Mechanism of action of Orthosiphon stamineus against non-alcoholic fatty liver disease: Insights from systems pharmacology and molecular docking approaches

Non-alcoholic fatty liver disease (NAFLD) is one of the most common complications of a metabolic syndrome caused by excessive accumulation of fat in the liver. Orthosiphon stamineus also known as Orthosiphon aristatus is a medicinal plant with possible potential beneficial effects on various metabolic disorders. This study aims to investigate the in vitro inhibitory effects of O. stamineus on hepatic fat accumulation and to further use the computational systems pharmacology approach to identify the pharmacokinetic properties of the bioactive compounds of O. stamineus and to predict their molecular mechanisms against NAFLD. Methods: The effects of an ethanolic extract of O. stamineus leaves on cytotoxicity, fat accumulation and antioxidant activity were assessed using HepG2 cells. The bioactive compounds of O. stamineus were identified using LC/MS and two bioinformatics databases, namely the Traditional Chinese Medicine Integrated Database (TCMID) and the Bioinformatics Analysis Tool for the Molecular Mechanism of Traditional Chinese Medicine (BATMAN-TCM). Pathway enrichment analysis was performed on the predicted targets of the bioactive compounds to provide a systematic overview of the molecular mechanism of action, while molecular docking was used to validate the predicted targets. Results: A total of 27 bioactive compounds corresponding to 50 potential NAFLD-related targets were identified. O. stamineus exerts its anti-NAFLD effects by modulating a variety of cellular processes, including oxidative stress, mitochondrial β-oxidation, inflammatory signalling pathways, insulin signalling, and fatty acid homeostasis pathways. O. stamineus is significantly targeting many oxidative stress regulators, including JNK, mammalian target of rapamycin (mTOR), NFKB1, PPAR, and AKT1. Molecular docking analysis confirmed the expected high affinity for the potential targets, while the in vitro assay indicates the ability of O. stamineus to inhibit hepatic fat accumulation. Conclusion: Using the computational systems pharmacology approach, the potentially beneficial effect of O. stamineus in NAFLD was indicated through the combination of multiple compounds, multiple targets, and multicellular components.     

A systematic review of antiglycation medicinal plants

Background and objectivesThe present review shows a list of anti-glycation plants with their anti-glycation activity mechanisms that can attract the attention of pharmacologist for further scientific research towards finding better remedy for diabetic complications.MaterialsGoogle scholar, Pubmed, Web of Science and Scopus were searched. The terms were advanced glycation end products (AGEs), medicinal plants, antiglycation products.Resultsplants that studied in this review inhibit glycation in several possible mechanisms. Some of these plants inhibit the production of shiff base and amadori products. The others inhibit the generation of amadori products in the advanced phase. Some others blocked the aggregation of AGEs and some plants have antioxidant activity and reduce AGEs formation by preventing oxidation of amadori product and metal-catalyzed glucoxidation.ConclusionThis review can help pharmacologist to find antiglycation natural substance that can be useful in treatment of diabetic complications.     

至阳八阵穴隔附子饼灸治疗糖尿病胃轻瘫临床研究

目的观察至阳八阵穴隔附子饼灸治疗脾胃气虚型糖尿病胃轻瘫的疗效及对胃泌素(GAS)、胃动素(MTL)和血管活性肠肽(VIP)水平的影响。方法86例脾胃气虚型糖尿病胃轻瘫患者随机分为对照组和治疗组,每组43例。治疗组给予至阳八阵穴隔附子饼灸;对照组口服枸橼酸莫沙必利片。治疗12周后观察胃轻瘫主要症状指数量表症状积分改善情况、胃排空率及血清GAS、MTL、VIP水平。结果治疗组治疗后在胃轻瘫主要症状指数量表症状积分及胃排空率方面明显高于对照组,差异均有统计学意义(P<0.05)。治疗组治疗后血清GAS、MTL水平明显高于对照组,血清VIP水平明显低于对照组,差异均有统计学意义(P<0.05)。治疗组总有效率为90.7%,明显高于对照组的72.1%(P<0.05)。结论采用至阳八阵穴隔附子饼灸能快速促进糖尿病胃轻瘫患者胃功能的恢复,改善症状和体征,其作用机制可能与升高患者血清GAS和MTL水平,降低VIP水平有关。     

Fighting the global pest problem: preface to the special Toxicon issue on insecticidal toxins and their potential for insect pest control.

Arthropod pests are responsible for major crop devastation and are vectors for the transmission of new and re-emerging diseases in humans and livestock. Despite many years of effective control by conventional agrochemical insecticides, a number of factors are threatening the effectiveness and continued use of these agents. These include the development of insecticide resistance and use-cancellation or de-registration of some insecticides due to human health and environmental concerns. Several approaches are being investigated for the design of new (bio)pesticides. These include the development of transgenic plants and recombinant baculoviruses as delivery systems for a variety of insect-selective toxins. Additional approaches for the development of foliar sprays include the rational design of peptidomimetics based on the key residues of these toxins that interact with the insect target. This special issue provides an overview of these phyletically selective animal, plant and microbial toxins and their diverse mechanisms of action to paralyze or kill arthropods. In addition, it reviews their potential for biopesticide discovery and validation of novel insecticide targets and provides an overview of the strengths and weaknesses of biopesticides in the global control of arthropod pests.     

芪月降脂片制剂处方的优化

[目的 ]优化芪月降脂片的制剂处方 .[方法 ]采用正交设计和多指标综合评分法对已筛选出的药剂辅料进行处方优化 .[结果 ]最佳制剂处方为糖粉 50 g ,辅料X 50g ,微晶纤维素 75g .[结论 ]该处方合理 ,成型性好     

姬松茸多糖的抗炎作用

[目的 ]观察姬松茸多糖的抗炎作用 .[方法 ]制作二甲苯所致小鼠耳急性炎症模型、角叉菜胶所致大鼠关节肿胀模型、小鼠棉球肉芽肿亚急性炎症模型和大鼠佐剂关节炎模型 ,给予 4 0 ,80 ,16 0mg/kg的姬松茸多糖 .[结果 ]姬松茸多糖明显抑制上述各类型炎症反应 .[结论 ]姬松茸多糖具有抗炎作用 .     

反相高效液相色谱法测定丹参中丹参酮工和丹参酮ⅡA的含量

[目的]用反相高效液相色谱法(RP-HPLC)同时测定丹参药材中丹参酮Ⅰ和丹参酮ⅡA的含量．[方法]选用mightysil RP-18(H)GP250-4．6(5μm)．流动相为甲醇-水(75：25)，检测波长为270nm，流速为1mL／min，温度为35℃．[结果]丹参酮Ⅰ和丹参酮ⅡA含量分别在0．0952～0．9520μg和0．1222～0．2850μg内呈线性关系；丹参酮Ⅰ和丹参酮ⅡA的平均回收率分另4为99．90％和99．69％．[结论]此方法快速、简便、可靠，为丹参及其制剂质量控制的科学方法。