- 1. Enzymatic preparation of silybin phase II metabolites: sulfation using aryl sulfotransferase from rat liver.
Aryl sulfotransferase IV (AstIV) from rat liver was overexpressed in Escherichia coli and purified to homogeneity. Using the produced mammalian liver enzyme, sulfation-the Phase II conjugation reaction-of optically pure silybin diastereoisomers (silybin A and B) was tested. As a result, silybin B was sulfated yielding 20-O-silybin B sulfate, whereas silybin A was completely resistant to the sulfation reaction. Milligram-scale sulfation of silybin B was optimized employing resting E. coli cells producing AstIV, thus avoiding the use of expensive 3'-phosphoadenosine-5'-phosphate cofactor and laborious enzyme purification. Using this approach, we were able to reach 48 % conversion of silybin B into its 20-sulfate within 24 h. The sulfated product was isolated by solid phase extraction and its structure was characterized by HRMS and NMR. Sulfation reaction of silybin appeared strictly stereoselective; only silybin B was sulfated by AstIV....(more)
Purchartová K, et al. Appl Microbiol Biotechnol 2013 Mar 14.
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- 2. The protective effect of silybin against lasalocid cytotoxic exposure on chicken and rat cell lines.
Lasalocid, an ionophore coccidiostat, extensive use implies a risk of toxicological impacts. Protective effects of silybin, a herbal compound of Silybum marianum, are reported elsewhere. The aim of this study was to compare effects of the combined use of lasalocid and silybin in chicken hepatoma cells (LMH) and rat myoblasts (L6) cell lines cultures. The cytoprotective effect resulting from an interaction of both pharmaceuticals was measured with the help of MTT reduction and, coomassie brilliant blue binding (CBB) and LDH release assays. Isobolography and the combination index (CI) estimated the nature and scale of interaction. In all performed tests, the lowest lasalocid EC50-values were obtained for chicken hepatocytes. In the rat myoblasts cultures, the lowest lasalocid EC50-values were found with LDH test. Simultaneously, a lack of silybin cytotoxic effect was proven for the studied cell lines. An interaction between both substances led to a considerable decrease of lasalocid cytotoxicity. The isobolograms and combination index showed a significant antagonistic nature of silybin effect in the course of lasalocid cytotoxicity. It is concluded that the mechanism of cytoprotection results from complex reaction at biochemical and biophysical endpoints during chicken hepatocytes and rat myoblasts cell lines exposure to silybin and lasalocid co-action....(more)
Radko L, et al. Biomed Res Int 2013;2013:783519.
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- 3. Anti-cancer efficacy of silybin derivatives - a structure-activity relationship.
Silybin or silibinin, a flavonolignan isolated from Milk thistle seeds, is one of the popular dietary supplements and has been extensively studied for its antioxidant, hepatoprotective and anti-cancer properties. We have envisioned that potency of silybin could be further enhanced through suitable modification/s in its chemical structure. Accordingly, here, we synthesized and characterized a series of silybin derivatives namely 2,3-dehydrosilybin (DHS), 7-O-methylsilybin (7OM), 7-O-galloylsilybin (7OG), 7,23-disulphatesilybin (DSS), 7-O-palmitoylsilybin (7OP), and 23-O-palmitoylsilybin (23OP); and compared their anti-cancer efficacy using human bladder cancer HTB9, colon cancer HCT116 and prostate carcinoma PC3 cells. In all the 3 cell lines, DHS, 7OM and 7OG demonstrated better growth inhibitory effects and compared to silybin, while other silybin derivatives showed lesser or no efficacy. Next, we prepared the optical isomers (A and B) of silybin, DHS, 7OM and 7OG, and compared their anti-cancer efficacy. Isomers of these three silybin derivatives also showed better efficacy compared with respective silybin isomers, but in each, there was no clear cut silybin A versus B isomer activity preference. Further studies in HTB cells found that DHS, 7OM and 7OG exert better apoptotic activity than silibinin. Clonogenic assays in HTB9 cells further confirmed that both the racemic mixtures as well as pure optical isomers of DHS, 7OM and 7OG were more effective than silybin. Overall, these results clearly suggest that the anti-cancer efficacy of silybin could be significantly enhanced through structural modifications, and identify strong anti-cancer efficacy of silybin derivatives, namely DHS, 7OM, and 7OG, signifying that their efficacy and toxicity should be evaluated in relevant pre-clinical cancer models in rodents....(more)
Agarwal C, et al. PLoS One 2013;8(3):e60074.
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- 4. Sinomenine hydrochloride enhancement of the inhibitory effects of anti-transferrin receptor antibody-dependent on the COX-2 pathway in human hepatoma cells.
Transferrin receptor (TfR) has been used as a target for the antibody-based therapy of cancer due to its higher expression in tumors relative to normal tissues. Great potential has been shown by anti-TfR antibodies combined with chemotherapeutic drugs as a possible cancer therapeutic strategy. In our study, we investigated the anti-tumor effects of anti-TfR monoclonal antibody (mAb) alone or in combination with sinomenine hydrochloride in vitro. Results suggested that anti-TfR mAb or sinomenine hydrochloride could induce apoptosis, inhibit proliferation, and affect the cell cycle. A synergistic effect was found in relation to tumor growth inhibition and the induction of apoptosis when anti-TfR mAb and sinomenine hydrochloride were used simultaneously. The expression of COX-2 and VEGF protein in HepG2 cells treated with anti-TfR mAb alone was increased in line with increasing dosage of the agent. In contrast, COX-2 expression was dramatically decreased in HepG2 cells treated with sinomenine hydrochloride alone. Furthermore, we demonstrated that the inhibitory effects of sinomenine hydrochloride and anti-TfR mAb administered in combination were more prominent than when the agents were administered singly. To sum up, these results showed that the combined use of sinomenine hydrochloride and anti-TfR mAb may exert synergistic inhibitory effects on human hepatoma HepG2 cells in a COX-2-dependent manner. This finding provides new insight into how tumor cells overcome the interference of iron intake to survive and forms the basis of a new therapeutic strategy involving the development of anti-TfR mAb combined with sinomenine hydrochloride for liver cancer....(more)
Hong Y, et al. Cancer Immunol Immunother 2013 Mar;62(3):447-54.
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- 5. Effect of sinomenine on vascular smooth muscle cell dedifferentiation and neointima formation after vascular injury in mice.
Sinomenine, a pure alkaloid extract from Sinomenium acutum, has anti-inflammatory and immunoregulatory functions. This study investigated the efficiency and the signalling pathways involved in the effect of sinomenine on vascular smooth muscle cell (VSMC) dedifferentiation in response to platelet-derived growth factor (PDGF)-BB stimulation and vascular injury. VSMCs were isolated from rat aorta and preincubated with sinomenine before being stimulated with PDGF-BB. WST and BrdU incorporation assays were used to evaluate VSMC proliferation. Flow cytometric analysis was performed for testing the cell cycle progression. The cell migration of VSMCs were analysed using a Transwell system. The expression of VSMC specific genes and signalling proteins were tested by Western blot. For the animal study, C57/BL6 mice were fed either normal rodent chow diets or sinomenine chow diets that supplemented with 0.09 % sinomenine (w/w) in the normal chows for 14 days before carotid artery wire injury. PDGF-BB activated the dedifferentiation of VSMCs characterised by decreased expression of SMA, Smoothelin and SM22α. However, sinomenine treatment preserved the dedifferentiation in response to PDGF-BB. The activations of mitogen-activated protein kinase extracellular signal-regulated kinases, Akt, GSK3β and STAT3 induced by PDGF-BB were also inhibited in sinomenine-treated VSMCs. In vivo evidence with wire-injured mice exhibited a reduction in neointimal area and an increase in smooth muscle-specific gene expression in the sinomenine-treated group. In this study, we found that sinomenine-suppressed VSMC phenotype switching induced by PDGF-BB in vitro and neointimal formation in vivo. Therefore, sinomenine is a potential candidate to be used in the treatment of vascular proliferative disease....(more)
Zhu L, et al. Mol Cell Biochem 2013 Jan;373(1-2):53-62.
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- 6. Sinomenine hydrochloride inhibits human hepatocellular carcinoma cell growth in vitro and in vivo: involvement of cell cycle arrest and apoptosis induction.
Hepatocellular carcinoma (HCC) is one of the most common malignancies worldwide. However, therapies against HCC to date have not been completely effective. Sinomenine hydrochloride (SH), an antiarthritis drug applied in clinical practice, has been reported to have in vitro antineoplastic activity in various cancer cells. Whether SH inhibits HCC remains unknown. For this purpose, in this study, MTT assay was used to determine cell growth. Flow cytometry, Hoechst staining, DNA fragmentation, western blot analysis, immunohistochemisty and TUNEL staining were performed to investigate the mechanisms involved. The in vivo activity of SH was determined using a mouse xenograft model. SH inhibited the growth of various types of human HCC cells in vitro. We found that SH promoted cell cycle arrest in the G1 phase and subG1 formation, associated with the increased p21/WAF1/Cip1 expression. Additionally, SH induced caspasedependent apoptosis, which involved the disruption of mitochondrial membrane potential, the increased release of cytochrome c and Omi/HtrA2 from the mitochondria into the cytoplasm, the downregulation of Bcl2 and the upregulation of Bax, the activation of a caspase cascade (caspase8, -10, -9 and -3) and PARP, as well as the decreased expression of survivin. The SHsuppressed growth of human HCC xenografts in vivo occurred due to the decrease in proliferation and the induction of apoptosis, implicating the activation of caspase3, the upregulation of p21 and the downregulation of survivin. These findings suggest that SH exhibits anticancer efficacy in vitro and in vivo involving cell cycle and caspasedependent apoptosis and may serve as a potential drug candidate against HCC....(more)
Lu XL, et al. Int J Oncol 2013 Jan;42(1):229-38.
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- 7. Analysis of active alkaloids in the Menispermaceae family by nonaqueous capillary electrophoresis-ion trap mass spectrometry.
A nonaqueous CE-IT MS with a nanospray ionization interface method was developed for the identification and quantification of tetrandrine (TET), fangchinoline (FAN), and sinomenine (SIN) using berberine as internal standard. The TET, FAN, and SIN standard solutions were directly infused into IT-MS for collecting MS(1-3) spectra. The major fragment ions of analytes were confirmed and possible main cleavage pathways of fragment ions were studied. A bare fused-silica capillary was used for separation of the analytes. A sheath liquid (50% aqueous methanol containing 0.2% acetic acid) to the capillary effluent with a nanoelectrospray ionization interface was added. Separation buffer comprised 80 mM solution of ammonium acetate, in a mixture of 70% methanol, 20% ACN, and 10% water, which also contained 1% acetic acid. The CE-MS method was validated for linearity, sensitivity, accuracy, and precision, and then used to determine the content of the above components. The detection limits of TET, FAN, and SIN are 0.05, 0.08, and 0.15 μg/mL, respectively. The precision was no more than 4.67% and the mean recovery of the analytes were 95.36-99.24%. This method was successfully applied to determine TET, FAN, and SIN in real samples radix Stephaniae tetrandrae and rhizomes of Menispermum dauricum....(more)
Chen Q, et al. J Sep Sci 2013 Jan;36(2):341-9.
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- 8. Microfluidics assisted synthesis and bioevaluation of sinomenine derivatives as antiinflammatory agents.
Sinomenine (1) is currently used for the treatment of rheumatoid arthritis (RA) in China and there is still room for the improvement of its efficacy. In present study, capillary based microfluidic system was effectively applied for the syntheses of two novel series of sinomenine derivatives. The Heck reactions in microreactor gave much higher conversions compared to the batch ones. The two-step synthesis of the isoxazoline in microreactor greatly shortened the reaction time without any isolation of intermediates. The inhibitory activity of synthesized compounds on the TNF-α-induced nuclear factor kappa B (NF-κB) activation was evaluated in vitro. Among the compounds, 3c and 3g showed the potent inhibitory activity. Furthermore, 3g exhibited the antiinflammatory effect in vivo....(more)
Jin J, et al. Eur J Med Chem 2013 Apr;62:280-8.
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- 9. Sinomenine inhibits the expression of PD?L1 in the peripheral blood mononuclear cells of mesangial proliferative nephritis patients.
Sinomenine has been used to treat autoimmune diseases for centuries. However, little is known about its exact mechanisms of action. Whether sinomenine has an effect on programmed death1 (PD1) ligands (PDLs) in vivo remains unclear. The present study aimed to determine the effect of sinomenine on the expression of PDL1 and PDL2 in peripheral blood mononuclear cells (PBMCs). A total of 25 patients with mesangial proliferative nephritis (MsPGN) were treated with sinomenine and followed up for 3 months. The expression of PDL1 and PDL2 was studied by using realtime RTPCR and flow cytometric analysis, and recorded at months 0, 1 and 3 within the PBMCs. The intrarenal expression of PDL1 and PDL2 was studied by immunohistochemistry. The results revealed that the PBMCs from the MsPGN patients expressed high levels of PDL1 at the mRNA and protein levels compared with the healthy donors. Immunohistochemistry revealed an increased PDL1 expression in the renal tissues from the MsPGN patients. Sinomenine was observed to have a significant effect in decreasing the PDL1 expression in the PBMCs. The present study therefore suggests a novel mechanism for the therapeutic effects of sinomenine on MsPGN in vivo....(more)
Cheng Y, et al. Mol Med Rep 2013 Apr;7(4):1223-8.
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- 10. Determination of alkaloids in Sinomenium acutum by field-amplified sample stacking in capillary electrophoresis with chemiluminescene detection.
A simple and rapid capillary electrophoresis (CE) with an acidic potassium permanganate chemiluminescence (CL) detection method was developed to determine three alkaloids (curine, sinomenine and magnoflorine) simultaneously. A laboratory-built CE-CL detection interface was used. The field-amplified sample stacking technique was applied to the online concentration of alkaloids. Experimental conditions for CE separation and CL detection were investigated in detail to acquire optimum conditions. Under optimal conditions, the three alkaloids were baseline separated within 6 min, and the detection limits (S/N = 3) ranged from 0.03 µg/mL to 0.49 µg/mL. This method was successfully applied to determine the above three alkaloids in Sinomenium acutum, and the result of the determination of sinomenine was in good agreement with those given by high-performance liquid chromatography and CE methods. In addition, a possible CL reaction mechanism of sinomenine-KMnO(4) -H(2) SO(4) was proposed. Copyright © 2013 John Wiley & Sons, Ltd....(more)
Shi G, et al. Luminescence 2013 Feb 7.
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- 11. Pharmacological characteristics of Kampo medicine as a mixture of constituents and ingredients.
Herbal medicine in Japan is termed as Kampo medicine, which is derived from traditional Chinese medicine. Shakuyakukanzoto (Shao-Yao-Gan-Cao-Tang) as a kind of Kampo formulations is composed of just two components; Paeoniae Radix and Glycyrrhizae Radix, which produced marked relaxation of intestinal tract. Mokuboito (Mu-Fang-Ji-Tang) inhibited cardiac ionic channel currents, and as a mixture also produced great vasodilatation. Sinomenine (a main ingredient of Mokuboito) as a single compound also caused the vasodilatation, but decreased it along with ageing. Gypsum containing in Mokuboito and Chotosan (Diao-Teng-San) caused more marked effects, as compared with those without Gypsum. On the other hand, Rokumigan (Liu-Wei-Wan), Hachimijiogan (Ba-Wei-Di-Huang-Wan) and Goshajinkigan (Niu-Che-Shen-Qi-Wan) increase in order the number of contained ingredients. The formulations with more herbs (ingredients) produced much more effective actions on rat aorta, presumably due to compensation of the decline of pharmacological sensitivity with ageing. Thus, there are some important differences between single chemical drugs and mixture drugs with many ingredients. The effects of Kampo medicine (mixture) are never just a sum of each effect induced by a lot of ingredients. For elder persons, furthermore, Kampo medicine exerts more effective actions....(more)
Satoh H. J Integr Med 2013 Jan;11(1):11-6.
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- 12. Sinomenine Protects against Lipopolysaccharide-Induced Acute Lung Injury in Mice via Adenosine A2A Receptor Signaling.
Sinomenine (SIN) is a bioactive alkaloid extracted from the Chinese medicinal plant Sinomenium acutum, which is widely used in the clinical treatment of rheumatoid arthritis (RA). However, its role in acute lung injury (ALI) is unclear. In this study, we investigate the role of SIN in lipopolysaccharide (LPS)-induced ALI in mice. After ALI, lung water content and histological signs of pulmonary injury were attenuated, whereas the PaO2/FIO2 (P/F) ratios were elevated significantly in the mice pretreated with SIN. Additionally, SIN markedly inhibited inflammatory cytokine TNF-α and IL-1β expression levels as well as neutrophil infiltration in the lung tissues of the mice. Microarray analysis and real-time PCR showed that SIN treatment upregulated adenosine A2A receptor (A2AR) expression, and the protective effect of SIN was abolished in A2AR knockout mice. Further investigation in isolated mouse neutrophils confirmed the upregulation of A2AR by SIN and showed that A2AR-cAMP-PKA signaling was involved in the anti-inflammatory effect of SIN. Taken together, these findings demonstrate an A2AR-associated anti-inflammatory effect and the protective role of SIN in ALI, which suggests a potential novel approach to treat ALI....(more)
Li J, et al. PLoS One 2013;8(3):e59257.
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- 13. Sinomenine Decreases MyD88 Expression and Improves Inflammation-Induced Joint Damage Progression and Symptoms in Rat Adjuvant-Induced Arthritis.
Sinomenine (SIN) is the active principle of the Chinese medical plant Sinomenium acutum which is widely used for the treatment of rheumatoid arthritis (RA) in China. Recently, several groups indicated that myeloid differentiation primary response protein 88 (MyD88) might be associated with disease progression of RA. Here, we observed the effect of SIN on MyD88 expression and showed its therapeutic role in RA. First, immunohistochemical staining in clinical specimens showed that MyD88 was mainly located in characteristic pathological structures of RA synovial tissues. Second, we found that MyD88 was overexpressed in the synovial tissues of the rats with adjuvant-induced arthritis (AIA). Treatment with SIN markedly decreased the expression of MyD88 in AIA rats. Finally, we provided evidences that SIN suppressed inflammation response and inflammation-induced joint destructive progression and arthritis symptoms in AIA rats. Therefore, SIN is an effective therapeutic agent for RA. Targeting MyD88 signaling may provide new methods for the treatment of RA....(more)
Mu H, et al. Inflammation 2013 Apr 21.
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- 14. Second-Hand Tobacco Smoke Exposure in Open and Semi-Open Settings: A Systematic Review.
BACKGROUND:
Some countries have recently extended smoke-free policies to particular outdoor settings; however, there is controversy regarding whether this is scientifically and ethically justifiable.
OBJECTIVES:
The objective of the present study is to review research on second-hand smoke (SHS) exposure in outdoor settings.
DATA SOURCES:
We conducted different searches in PubMed for the period prior to September 2012. We checked the references of the identified papers, and conducted a similar search in Google Scholar.
STUDY SELECTION:
We included combinations of secondhand smoke, environmental tobacco smoke, passive smoking OR tobacco smoke pollution AND outdoors AND PM, PM2.5, RSP, particulate matter, nicotine, CO, cotinine, marker, biomarker OR airborne marker. In total, 18 articles and reports met the inclusion criteria.
RESULTS:
Almost all studies used PM2.5 concentration as an SHS marker. Mean PM2.5 concentrations reported for outdoor smoking areas when smokers were present ranged from 8.32 µg/m<sup>3</sup> to 124 µg/m<sup>3</sup> at hospitality venues, and 4.60 µg/m<sup>3</sup> to 17.80 µg/m<sup>3</sup> at other locations. Mean PM2.5 concentrations in smoke-free indoor settings near outdoor smoking areas ranged from 4 µg/m<sup>3</sup> to 120.51 µg/m<sup>3</sup>. SHS levels were increased when smokers were present, and outdoor and indoor SHS levels were related. Most studies reported a positive association between SHS measures and smoker density, enclosure of outdoor locations, wind conditions, and proximity to smokers.
CONCLUSIONS:
The available evidence indicates high SHS levels at some outdoor smoking areas, and at adjacent smoke-free indoor areas. Further research and standardization of methodology is needed to determine whether smoke-free legislation should be extended to outdoor settings....(more)
Sureda X, et al. Environ Health Perspect 2013 May 7.
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- 15. The role of anti-smoking legislation on cigarette and alcohol consumption habits in Italy.
The short-term effects of public smoking bans on individual smoking and drinking habits were investigated in this paper. In 2005, a smoking ban was introduced in Italy, and we exploited this exogenous variation to measure the effect on both smoking participation and intensity and the indirect effect on alcohol consumption. Using data from the Everyday Life Aspects survey, for the period 2001-2007, we show that the introduction of smoke-free legislation in Italy significantly affected smoking behavior. We also document significant indirect effects on alcohol consumption for the main alcoholic beverage categories. A robustness analysis is also performed, to test the extent to which unobservable variables may bias our estimated parameters. Our results are then used to perform a cost-effectiveness analysis of the anti-smoking legislation in Italy.
Copyright © 2013 Elsevier Ireland Ltd. All rights reserved....(more)
Pieroni L, et al. Health Policy 2013 Apr 30.
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- 16. Tobacco control efforts in Europe.
Smoking is prevalent across Europe, but the severity and stage of the smoking epidemic, and policy responses to it, vary substantially between countries. Much progress is now being made in prohibition of paid-for advertising and in promotion of smoke-free policies, but mass media campaigns are widely underused, provision of services for smokers trying to quit is generally poor, and price policies are undermined by licit and illicit cheap supplies. Monitoring of prevalence is inadequate in many countries, as is investment in research and capacity to address this largest avoidable cause of death and disability across Europe. However, grounds for optimism are provided by progress in implementation of the WHO Framework Convention on Tobacco Control, and in the development of a new generation of nicotine-containing devices that could enable more widespread adoption of harm-reduction strategies. The effect of commercial vested interests has been and remains a major barrier to progress.
Copyright © 2013 Elsevier Ltd. All rights reserved....(more)
Britton J, et al. Lancet 2013 May 4;381(9877):1588-95.
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- 17. Understanding the Tobacco Control Act: efforts by the US Food and Drug Administration to make tobacco-related morbidity and mortality part of the USA's past, not its future.
The USA has a rich history of public health efforts to reduce morbidity and mortality from tobacco use. Comprehensive tobacco-prevention programmes, when robustly implemented, reduce the prevalence of youth and adult smoking, decrease cigarette consumption, accelerate declines in tobacco-related deaths, and diminish health-care costs from tobacco-related diseases. Effective public health interventions include raising the price of tobacco products, smoke-free policies, counter-marketing campaigns, advertising restrictions, augmenting access to treatment for tobacco use through insurance coverage and telephone help lines, and comprehensive approaches to prevent children and adolescents from accessing tobacco products. The US Food and Drug Administration (FDA) has six major areas of regulatory authority: regulation of tobacco products; regulation of the advertising, marketing, and promotion of tobacco products; regulation of the distribution and sales of tobacco products; enforcement of the provisions of the Tobacco Control Act and tobacco regulations; regulatory science to support FDA authorities and activities; and public education about the harms of tobacco products and to support FDA regulatory actions. With passing of the Family Smoking Prevention and Tobacco Control Act (Tobacco Control Act) in June, 2009, important new regulatory approaches were added to the tobacco prevention and control arsenal.
Copyright © 2013 Elsevier Ltd. All rights reserved....(more)
Husten CG, et al. Lancet 2013 May 4;381(9877):1570-80.
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- 18. Environmental factors and unhealthy lifestyle influence oxidative stress in humans-an overview.
Oxygen is the most essential molecule for life; since it is a strong oxidizing agent, it can aggravate the damage within the cell by a series of oxidative events including the generation of free radicals. Antioxidative agents are the only defense mechanism to neutralize these free radicals. Free radicals are not only generated internally in our body system but also trough external sources like environmental pollution, toxic metals, cigarette smoke, pesticides, etc., which add damage to our body system. Inhaling these toxic chemicals in the environment has become unavoidable in modern civilization. Antioxidants of plant origin with free radical scavenging properties could have great importance as therapeutic agents in several diseases caused by environmental pollution. This review summarizes the generation of reactive oxygen species and damage to cells by exposure to external factors, unhealthy lifestyle, and role of herbal plants in scavenging these reactive oxygen species....(more)
Aseervatham GS, et al. Environ Sci Pollut Res Int 2013 May 1.
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- 19. [Preventive measures against minor's smoking].
Adolescents are unique for tobacco control. They are easy to become tobacco-addicted and more than 70 % of adult smokers start to smoke tobacco during adolescence. Therefore, they are good targets for sales campaign by tobacco industry to secure their profit by making a large reservoir of smokers. Tobacco industry's tactics are very ingenious. It conducts many kinds of hidden advertisement. It supports many activities of youth and nonprofit organizations. Therefore, our effort should also put targets on adolescents. Adolescence is a unique stage of development and it is important to know its characteristics for effective approach to prevent starting and to facilitate quitting smoking. It is important to make tobacco-free environment surrounding adolescents, such as school campuses and other public places....(more)
Bessho F. Nihon Rinsho 2013 Mar;71(3):540-4. Japanese.
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- 20. [Anti-smoking education for tobacco-free society].
The Science Council of Japan handed a proposal entitled "For the establishment of tobacco-free society" to the Japanese government in 2008, demanding stronger policy implementation. Among the 7 demands, top priority was placed on"education for improvement of knowledge on health risks of smoking". Ample scientific evidences have proven the health hazards that smoking causes directly and indirectly, which, however, are not well acknowledged among Japanese people, leaving Japan an underdeveloped country in terms of smoke-free society. More education is indispensable in schools and by mass media such as TV. The government must allocate more budgets for the education and advertisements, and, if unsuccessful, should request NHK, which collects mandatory TV reception fees akin to broadcast tax, to assume this task....(more)
Ohno R. Nihon Rinsho 2013 Mar;71(3):527-32. Japanese.
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- 21. [Diagnosis and treatment strategy of diseases due to passive smoking].
Passive smoking causes a wide range of diseases from membrane irritation such as sore throat or nasal symptom, to fatal diseases such as lung cancer or heart attack. Extensive epidemiological studies have revealed that passive smoking at home or at workplaces raises the all cause mortality of nonsmoking family members by 14-75%. Moreover, many people in Japan are suffered from chemical hypersensitivity due to chronic persistent passive smoking at workplaces. Most critical diagnostic clue of passive smoking caused disease is the temporal relationship of tobacco smoke exposure and disease onset. One hundred percent smoke free workplace or environment is the only effective measure for curing and preventing illnesses caused by passive smoke exposure....(more)
Matsuzaki M. Nihon Rinsho 2013 Mar;71(3):469-72. Japanese.
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- 22. [Health risks induced by secondhand smoke and declines of risks after comprehensive smoke-free legislation].
Secondhand smoke is the major health risk among non-smokers. It is estimated that more than 6,800 non-smokers who are exposed to secondhand smoke die every year in Japan. WHO Framework Convention on Tobacco Control requires all the governments to implement comprehensive smoking ban in order to protect non-smokers' health. Many countries and municipal offices implemented comprehensive smoking ban in workplaces and public spaces including restaurants and bars. The number of patients of acute coronary syndrome and respiratory disease rapidly decreased in those countries. These facts should be announced to the people and policy makers where comprehensive smoking ban has not implemented yet in order to protect non-smokers' health....(more)
Yamato H. Nihon Rinsho 2013 Mar;71(3):464-8. Japanese.
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- 23. Cytokinesis-blocked micronucleus cytome assay and spectral karyotyping as methods for identifying chromosome damage in a lung cancer case-control population.
Lung cancer is the leading cause of all cancer-related deaths in the US. The need to develop more accurate cancer risk assessment tools is imperative to improve the ability to identify individuals at greatest risk of developing disease. The Cytokinesis-Blocked Micronucleus Cytome Assay (CBMNcyt) presents a sensitive and specific method of assessing DNA damage. We have previously reported that this assay is sensitive to genetic damage caused by the tobacco-specific nitrosamine 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK), and that binucleated cells with micronuclei, nucleoplasmic bridges and nuclear buds are strong predictors of lung cancer risk. The current study confirmed our previous findings and sought to identify the specific chromosomes involved in lung carcinogenesis. Spectral karyotyping was conducted on a subset of lung cancer cases [n = 116] and cancer-free controls [n = 126] with the highest CBMNcyt endpoints, on baseline and NNK-treated blood lymphocytes. After adjusting for age, gender, race/ethnicity, smoking status, and pack and smoke years, consistent significant associations between chromosome: 9, 19, 22, X, at baseline; chromosome: 3, 4, and 16 after NNK-induction; and chromosome: 1, 13, and 17 at both baseline and NNK-induction; and lung cancer risk (all P ≤ 0.05) were observed. Several of these chromosomes harbor critical genes involved in lung carcinogenesis, such as the FHIT gene, CDKN2A, PADPRP, and TP53. Our results indicate that the CBMNcyt assay when used in conjunction with other cytogenetic methodologies can increase our ability to identify specific chromosomal regions associated with DNA damage, thereby improving our understanding of the underlying mechanisms involved in individual cancer predisposition. © 2013 Wiley Periodicals, Inc.
Copyright © 2013 Wiley Periodicals, Inc....(more)
Lloyd SM, et al. Genes Chromosomes Cancer 2013 Apr 30.
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- 24. Immuno-suppressive effects of aqueous extract of soapnut Sapindus emarginatus on the larvae and pupae of vector mosquito, Aedes aegypti.
We recently reported the presence of potent anti-mosquito activity in aqueous kernel extract of the soapnut, Sapindus emarginatus, and demonstrated its impact on marker enzymes in larvae and pupae of the vector mosquito, Aedes aegypti. As a sequel to these findings, the present study elucidates immunotoxicity of this extract with respect to hemocyte-mediated cellular immune responses in fourth instar larvae and pupae as well as cuticular melanization reaction in the larvae of A. aegypti. The exposure of these two developmental stages of the mosquito to the soapnut extract at a lethal threshold concentration neither affected hemocyte viability tested up to 3h in vitro nor did it influence the hemocyte count. By contrast, exposure of the mosquito larvae and pupae to this extract significantly reduced the ability of their hemocytes to bind yeast cells, an important early event in the process of non-self recognition by immune cells. Consequently, the phagocytic activity of these hemocytes against yeast cells was also found to be adversely affected upon exposure of larvae and pupae to the extract. Besides, a perceptible initial delay in melanization reaction at the injured site of the cuticle in the extract-exposed larvae was observed. All these findings demonstrate, for the first time, the immuno-suppressive potential of a botanical biocide in the vector mosquito....(more)
Koodalingam A, et al. Acta Trop 2013 Jun;126(3):249-55.
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- 25. Zinc Lactate and Sapindin Act Synergistically with Lactocin 160 Against Gardnerella vaginalis.
Lactocin 160 is a vaginal probiotic-derived bacteriocin shown to selectively inhibit the growth of Gardenerella vaginalis and some other pathogens commonly associated with bacterial vaginosis. The natural origin of this peptide, its safety, and selective antimicrobial properties make it a promising candidate for successful treatment and prophylaxis of bacterial vaginosis (BV). This study evaluated interactions between lactocin 160 and four other natural antimicrobials in the ability to inhibit G. vaginalis. We report that zinc lactate and soapnut extract act synergistically with lactocin 160 against this pathogen and therefore have a potential to be successfully used as the components of the multiple-hurdle antimicrobial formulation for the treatment of BV....(more)
Turovskiy Y, et al. Probiotics Antimicrob Proteins 2011 Jun 1;3(2):144-149.
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- 26. Antimosquito activity of aqueous kernel extract of soapnut Sapindus emarginatus: impact on various developmental stages of three vector mosquito species and nontarget aquatic insects.
Aqueous (physiological saline) extracts of seed kernel from seven indigenous plants were initially screened for their antimosquito activity against eggs, larvae of all instars, and pupae of Aedes aegypti. Among various seed kernels tested, the soapnut Sapindus emarginatus (Sapindaceae) extract was found to exhibit, for the first time, a strong antimosquito activity as evident from its ability to inflict 100% mortality of all the developmental stages of A. aegypti. Furthermore, the kernel extract of S. emarginatus also exerted ovicidal, larvicidal, and pupicidal activity against two other important vector mosquitoes, namely, Anopheles stephensi and Culex quinquefasciatus. Differential susceptibility of the various developmental stages of the three mosquito species exposed to soapnut extract was also noticed. The kernel extract was found to be safe for two nontarget aquatic insects tested: the larvae of Chironomus costatus and the nymphs of Diplonychus rusticus. Lethal concentration values of soapnut extract to these nontarget insects were always threefold or fivefold higher than those that produced 100% mortality of the larvae of the three mosquito species examined. The findings of this study clearly demonstrate that the aqueous kernel extract of S. emarginatus has potent antimosquito activity detectable against all the developmental stages of three important vector mosquito species as well as it is safe for nontarget aquatic organisms, and thus this new botanical resource could be used as an eco-friendly alternative biocidal agent in control of mosquitoes....(more)
Koodalingam A, et al. Parasitol Res 2009 Oct;105(5):1425-34.
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- 27. Enhanced dissolution and oral bioavailability of tanshinone IIA base by solid dispersion system with low-molecular-weight chitosan.
OBJECTIVES:
The aim of this study is to improve the dissolution and oral bioavailability of tanshinone IIA (TAN).
METHODS:
Solid dispersions of TAN with low-molecular-weight chitosan (LMC) were prepared and the in-vitro dissolution and in-vivo performance were evaluated.
KEY FINDINGS:
At 1 h, the extent of dissolution of TAN from the LMC-TAN system (weight ratio 9 : 1) increased about 368.2% compared with the pure drug. Increasing the LMC content from 9 : 1 to 12 : 1 in this system did not significantly increase the rate and the extent of dissolution. Differential scanning calorimetry, X-ray diffraction and scanning electron microscopy demonstrated the formation of amorphous tanshinone IIA and the absence of crystallinity in the solid dispersion. Fourier transform infrared spectroscopy revealed that there was no interaction between drug and carrier. In-vivo test showed that LMC-TAN solid dispersion system presented significantly larger AUC0-t , which was 0.67 times that of physical mixtures and 1.17 times that of TAN. Additionally, the solid dispersion generated obviously higher Cmax and shortened Tmax compared with TAN and physical mixtures.
CONCLUSIONS:
In conclusion, the LMC -based solid dispersions could achieve complete dissolution, accelerated absorption rate and superior oral bioavailability.
© 2013 Royal Pharmaceutical Society....(more)
Liu QY, et al. J Pharm Pharmacol 2013 Jun;65(6):839-46.
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- 28. [Effect of tanshinone II A to B7H3 expression in human nasopharyngeal carcinoma CNE1 cell lines].
OBJECTIVE:
To explore the proliferation of human nasopharyngeal carcinoma CNE1 cell and B7H3 experation after treating by Tanshinone II A (Tan II A).
METHOD:
The CNE1 cell was cultured in vitro and treated by Tan II A with different concentrations; Cell proliferation was valuated by MTT; Apoptotic rate and cell cycle were investigated by flow cytometry; Bcl2 and B7H3 experation were detected by direct immunofluorescence assay.
RESULT:
The CNE1 cell's proliferation has been significantly inhibited by Tan II A, the inhibition was in dose and time effect with Tan II A, with significant difference (P<0.01); IC50 value in 24, 48 and 72 hours was respective 12.5 micromol/L, 4.8 micromol/L and 3.0 micromol/L; Comparing with the control group, Tan II A group increased apoptosis rate (P<0.01); Cell cycle was blocked in G2/M phase; Bcl2 and B7H3 expression were more decreased in Tan II A group than in control group with significant difference (P<0.05);
CONCLUSION:
Tan II A caused obviously growth inhibitory effect and induced apoptosis in CNE1 cells and the mechanisms might be related to down regulation of Bcl2 and B7H3....(more)
Zhao J, et al. Lin Chung Er Bi Yan Hou Tou Jing Wai Ke Za Zhi 2013 Feb;27(4):199-202. Chinese.
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- 29. Nanovesicles system for rapid-onset sublingual delivery containing sodium tanshinone IIA sulfonate: In vitro and in vivo evaluation.
A novel formulation based on nanovesicles system for rapid-onset sublingual delivery of hydrophilic drug (sodium tanshinone IIA sulfonate, STS) was investigated. The nanovesicles system was composed of 1.5% soybean lecithin, 6% propylene glycol, and penetration enhancers (1% sodium dodecyl sulfate and 0.03% hyaluronan acid). The STS-loaded nanovesicles with an average diameter of 133 ± 9.04 nm and high entrapment efficiency of 85.65 ± 3.89% were characterized. The effects of permeation enhancers on the penetration of STS formulations were investigated using Franz diffusion cells in vitro, showing 86.1-235.8 times higher permeation rate than that of normal STS solution. The rapid symptom relief effect of the nanovesicles system on acute myocardial infarction rabbits was evaluated by in vivo study, ST-segment deviation(S and T wave abnormality in electrocardiogram) was attenuated markedly and rapidly within 5 min, infarct size of heart was significantly reduced and the biochemical indicators were substantially decreased, compared with the control groups (p < 0.05). This study provided a promising tool for the future sublingual delivery of hydrophilic compounds with the noninvasive and rapid onset clinical effect. © 2013 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci.
Copyright © 2013 Wiley Periodicals, Inc....(more)
Zhu H, et al. J Pharm Sci 2013 Apr 23.
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- 30. Effects of sodium tanshinone IIA sulfonate against Marek's disease virus in experimentally infected chickens.
Chickens experimentally infected with Marek's disease virus J-1 strain were used to evaluate the anti-Marek's disease virus (MDV) activity of sodium tanshinone IIA sulfonate (STS) in vivo. Chickens in same group were kept in one pen and control group chickens were housed in negative pressure isolator. Chickens were treated with different dose of STS or ABOB for 21 consecutive days. Peripheral T lymphocyte proliferation, expression level of IFN-γ and IL-10 in serum, and MDV load in spleen were determined. The results showed that the treatments with STS and ABOB could significantly increase stimulating index (SI) of peripheral T lymphocytes while the SI is dropping due to the MDV infection, SI of chickens in STS prevention groups were significantly higher than that in STS treatment group and ABOB group (P<0.05 or P<0.01); IFN-γ and IL-10 level of chickens in STS groups were higher than that in other groups (P<0.05 or P<0.01). The results of qPCR demonstrated that STS could inhibit the virus replication in spleen of chickens infected with MDV. These findings indicated that STS can be potentially applied as an anti-MDV drug and set a solid basis for further investigating the antiviral mechanisms of STS.
Copyright © 2013. Published by Elsevier B.V....(more)
Zhang JQ, et al. Int J Biol Macromol 2013 Apr 18.
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- 31. Promising therapeutic effects of sodium tanshinone IIA sulfonate towards pulmonary arterial hypertension in patients.
BACKGROUND:
Pulmonary hypertension (PH) is a lethal disease with no cure currently available. Sodium Tanshinone IIA sulfonate (STS) is a water-soluble derivative of tanshinone IIA isolated as the major active component from salvia miltiorrhiza, a kind of Chinese herbal medicine. We investigate the efficacy of STS towards treatment of PH patients.
METHODS AND RESULTS:
Five hospitalized patients were randomly enrolled for this study. These patients were suffering from various types of serious PH without getting sufficient benefits from sildenafil treatment (20 mg tid) for at least three months. The efficacy of STS on PH was evaluated by measuring the pulmonary arterial systolic pressure (PASP), RV size by echocardiography, 6-minute walking distance (6MWD), Borg dyspnea score, and WHO functional class of PH. Patients aged from 17 to 46 (average 33±11) years old, pulmonary arterial systolic pressure (PASP) ranged from 60 to 140 mmHg, RV size ranged from 25 to 39 mm were included in study. At the endpoint of observation for 8 weeks of STS infusion, they obtained reduction of PASP in the range of 14-45 (average 28.6±12.5) mmHg, RV size in the range of 0-10 (average 4.2±1.6). All patients exhibited improved exercise capacity with an increase of 6MWD from 63 to 268 (average 138.4±40.7) meters, significantly reduced Borg dyspnea score from maximum 9 down to 1 or 0, and reduced WHO functional class of PH from III or IV down to II.
CONCLUSIONS:
These results indicate that STS exhibits remarkable beneficiary effects on treating PH patients either alone or in concert with sildenafil....(more)
Wang J, et al. J Thorac Dis 2013 Apr;5(2):169-72.
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- 32. Sodium tanshinone IIA sulfonate for pulmonary arterial hypertension: emerging therapeutic option.
Pulmonary arterial hypertension (PAH) is a rare disease characterised by a progressive increase of pulmonary vascular resistance and pulmonary arterial pressure, leading to right ventricle hypertrophy and death (1,2). The last decade has seen major advances in the understanding of the pathobiology of PAH along with discovery of several therapeutic options. Pharmacological agents targeting the endothelin (ET)-1 (ET-1 receptor antagonists, such as bosentan or sitaxentan), the nitric oxide (sildenafil, type 5 phosphodiesterase inhibitor), or the prostacyclin (epoprostenol, iloprost) pathways have shown benefits for patients with PAH (3). However, despite symptomatic improvement these treatments failed to improve the long-term survival and their use is hampered by either side-effects or inconvenient drug administration routes (4). Indeed, none of the currently available therapies is curative, so the search for novel therapeutic strategies continues....(more)
Raja SG. J Thorac Dis 2013 Apr;5(2):114-5.
Related Products: Sodium Tanshinone IIA Silate
- 33. Tanshinone II A inhibits breast cancer stem cells growth in vitro and in vivo through attenuation of IL-6/STAT3/NF-kB signaling pathways.
Cancer stem cells (CSCs) are maintained by inflammatory cytokines and signaling pathways. Tanshinone II A (Tan-IIA) possesses anti-cancer and anti-inflammatory activities. The purpose of this study is to confirm the growth inhibition effect of Tan-IIA on human breast CSCs growth in vitro and in vivo and to explore the possible mechanism of its activity. Human breast CSCs were enriched and expanded under serum-free mammosphere culture condition, and identified through mammosphere formation, toluidine blue staining, immunofluorescence staining and flow cytometry analysis of stemness markers of CD44/CD24 and ALDH, and tumorigenecity in vivo; the growth inhibition effect of Tan-IIA on human breast CSCs in vitro were tested by cell proliferation and mammosphere formation assays; inflammatory signaling pathway related protein expression in response to Tan-IIA, IL-6, STAT3, phospho-STAT3 (Tyr705), NF-κBp65 in cytoplasm and nucleus and cyclin D1 were evaluated with Western blotting; the growth inhibition effect of Tan-IIA on human breast CSCs growth were tested in vivo. A useful model of human breast CSCs for researching and developing the agents targeting CSCs was established. After Tan-IIA treatment, cell proliferation and mammosphere formation of CSCs were decreased significantly; the expression levels of IL-6, STAT3, phospho-STAT3 (Tyr705), NF-κBp65 in nucleus and cyclin D1 proteins were decreased significantly; the tumor growth and mean tumor weight were reduced significantly. Tan-IIA has the potential to target and kill CSCs, and can inhibit human breast CSCs growth both in vitro and in vivo through attenuation of IL-6/STAT3/NF-kB signaling pathways. J. Cell. Biochem. © 2013 Wiley Periodicals, Inc.
Copyright © 2013 Wiley Periodicals, Inc....(more)
Lin C, et al. J Cell Biochem 2013 Mar 28.
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- 34. Tanshinone IIA, a constituent of Danshen, inhibits the release of glutamate in rat cerebrocortical nerve terminals.
ETHNOPHARMACOLOGICAL RELEVANCE:
Danshen is a commonly used traditional Chinese medicine and has received considerable attention due to their beneficial effects on the health, including prevention of cardiovascular disease, and cancer. Tanshinone IIA, a major active constituent of Danshen, has been reported to have a neuroprotective profile.
AIM OF THE STUDY:
An excessive release of glutamate is considered to be related to neuropathology of several neurological diseases. In this study, we investigated whether tanshinone IIA could affect endogenous glutamate release and explored the possible mechanism.
MATERIALS AND METHODS:
The experimental model was the isolated nerve terminals (synaptosomes) purified from the rat cerebral cortex. The release of glutamate was evoked by the K(+) channel blocker 4-aminopyridine (4-AP) and measured by one-line enzyme-coupled fluorometric assay. We also used a membrane potential-sensitive dye to assay nerve terminal excitability and depolarization, and a Ca(2+) indicator, Fura-2-acetoxymethyl ester, to monitor cytosolic Ca(2+) concentrations ([Ca(2+)]C).
RESULTS:
Tanshinone IIA inhibited the release of glutamate evoked by 4-AP in a concentration-dependent manner. Inhibition of glutamate release by tanshinone IIA was prevented by the chelating the extracellular Ca(2+) ions, and by the vesicular transporter inhibitor bafilomycin A1. However, the glutamate transporter inhibitor DL-threo-beta-benzyl-oxyaspartate did not have any effect on the action of tanshinone IIA. Tanshinone IIA decreased the depolarization-induced increase in [Ca(2+)]C, whereas it did not alter the resting synaptosomal membrane potential or 4-AP-mediated depolarization. Furthermore, the effect of tanshinone IIA on evoked glutamate release was prevented by the Cav2.2 (N-type) and Cav2.1 (P/Q-type) channel blocker ω-conotoxin MVIIC, but not by the ryanodine receptor blocker dantrolene or the mitochondrial Na(+)/Ca(2+) exchanger blocker CGP37157. Mitogen-activated protein kinase (MEK) inhibition also prevented the inhibitory effect of tanshinone IIA on evoked glutamate release.
CONCLUSION:
These results show that tanshinone IIA inhibits glutamate release from cortical synaptosomes in rats through the suppression of presynaptic voltage-dependent Ca(2+) entry and MEK signaling cascade.
Copyright © 2013 Elsevier Ireland Ltd. All rights reserved....(more)
Lin TY, et al. J Ethnopharmacol 2013 May 20;147(2):488-96.
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- 35. Tanshinone IIA reverses the malignant phenotype of SGC7901 gastric cancer cells.
BACKGROUNDS:
Tanshinone IIA (TIIA), a phenanthrenequinone derivative extracted from Salvia miltiorrhiza BUNGE, has been reported to be a natural anti-cancer agent in a variety of tumor cells. However, the effect of TIIA on gastric cancer cells remains unknown. In the present study, we investigated the influence of TIIA on the malignant phenotype of SGC7901 gastric cancer cells.
METHODS:
Cells cultured in vitro were treated with TIIA (0, 1, 5, 10 μg/ml) and after incubation for different periods, cell proliferation was measured by MTT method and cell apoptosis and cell cycling were assessed by flow cytometry (FCM). The sensitivity of SGC7901 gastric cancer cells to anticancer chemotherapy was investigated with the MTT method, while cell migration and invasion were examined by wound-healing and transwell assays, respectively.
RESULTS:
TIIA (1, 5, 10 μg/ml) exerted powerful inhibitory effects on cell proliferation (P < 0.05, and P < 0.01), and this effect was time- and dose-dependent. FCM results showed that TIIA induced apoptosis of SGC7901 cells, reduced the number of cells in S phase and increased those in G0/G1 phase. TIIA also significantly increased the sensitivity of SGC7901 gastric cancer cells to ADR and Fu. Moreover, wound-healing and transwell assays showed that TIIA markedly decreased migratory and invasive abilities of SGC7901 cells.
CONCLUSIONS:
TIIA can reverse the malignant phenotype of SGC7901 gastric cancer cells, indicating that it may be a promising therapeutic agent....(more)
Xu M, et al. Asian Pac J Cancer Prev 2013;14(1):173-7.
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