Natural 2,5-bisaryltetrahydrofuran lignans: Platelet-activating factor antagonists

Lignans are a class of naturally occurring compounds characterized by bonding of two aryl propanoids at the 2-position. Recently, an increasing significance of the biological activities of these compounds has been recognized. Members of 2,5-bisaryltetrahydrofuran class of lignans are antagonists of the potent bioactive phospholipid, platelet activating factor (PAF). In this review, a survey of the occurrence, physical properties of all known bisaryltetrahydrofurans and reported biological activities as PAF antagonists is given.     

银杏萜内酯的研究概况

银杏萜内酯是血小板活化因子的强拮抗剂,对心脑血管疾病具有显著的疗效。本文对近10年银杏萜内酯在提取分离、含量测定、药理活性、药代动力学、组织培养以及生物合成等方面的研究概况作了综述。     

银杏萜内酯的研究概况

银杏萜内酯是血小板活化因子的强拮抗剂，对心脑血管疾病具有显著的疗效。本文对近10年银杏萜内酯在提取分离，含量测定，药理活性，药代动力学，组织培养以及生物合成等方面的研究概况作了综述。     

脑卒中与血小板活化因子及其受体拮抗剂

脑卒中是一种急性脑血管疾病,具有发病率高、致残率和致死率高的特点。全球脑卒中防治形势严峻,抗血小板聚集治疗能够有效防治脑卒中。血小板活化因子(PAF)是介导血小板聚集的另一重要介质,在脑卒中病理过程中起着重要作用。近年来,PAF受体拮抗剂在脑卒中防治领域逐渐引起国际关注。该文对PAF受体拮抗剂的分类、作用机制及药物特征进行综述,以期对临床用药及新药研发提供有价值的指导和方向。     

银杏二萜内酯葡胺注射液联合氯吡格雷治疗冠心病合并脑梗死的疗效分析

目的探究银杏二萜内酯葡胺注射液联合氯吡格雷对冠心病合并脑梗死的疗效。方法选取2018年8月—2020年8月医院收治的冠心病合并脑梗死患者214例,采用随机数字表法分为联合组和对照组各107例。对照组患者采用氯吡格雷治疗,联合组采用银杏二萜内酯葡胺注射液联合氯吡格雷治疗,持续治疗7个疗程后,评估两组总有效率,治疗前后中医证候积分、简易智力状况检查评分(MMSE)及血小板聚集率,不良反应发生率。结果联合组临床治疗总有效率显著高于对照组(P<0.05);治疗后,两组中医证候积分与治疗前比较显著下降,对照组中医证候积分明显高于联合组(P<0.05);二磷酸腺苷(ADP)诱导下,两组血小板聚集率在治疗后均显著降低(P<0.05),血小板活化因子(PAF)诱导下,联合组治疗后血小板聚集率较治疗前显著降低(P<0.05),而对照组无显著差异(P>0.05);治疗后4周、12周,两组MMSE评分较治疗前显著上升(P<0.05)且两组组间比较差异有统计学意义(P<0.05);两组均无严重不良反应发生。结论银杏二萜内酯葡胺注射液联合氯吡格雷治疗冠心病合并脑梗死疗效...     

银杏内酯对体外PC12细胞拟缺血缺氧损伤及缺血继发性凋亡的作用

目的：研究银杏内酯对缺血缺氧损伤情况下体外培养PC12细胞的保护作用及其对该细胞凋亡的影响，并探讨其作用机制。方法：在离体培养的PC12细胞，用NaCN无糖培养造成拟缺血损伤模型，用H2O2模拟氧自由基损伤，分别通过形态学观察、MTT微量比色等方法研究药物对上述模型的保护作用。另将PC12细胞在无血清条件下培养96h，通过琼脂糖凝胶电泳检测其凋亡情况，并用流式细胞术检测细胞的凋亡程度及凋亡相关基因bcl-2在其中的作用。结果：银杏内酯终浓度10^-5、10^-6、10^-7mol/L能抑制NaCN无糖和H2O2培养造成的细胞损伤，明显增强细胞活力。凝胶电泳可见到明显的梯型条带，流式细胞术检测凋亡情况发现模型组凋亡率为10．40％，银杏内酯10^-5mol/L组的凋亡率为3．96％。同时发现药物组和模型组细胞中的bcl-2基因表达没有显著差异。结论：银杏内酯具有神经保护作用，且该作用与药物的抗凋亡能力有关，但这种抗凋亡作用似乎并不是通过bcl-2基因的调控实现的。     

Antiinflammatory,Antioxidant, and Immunological Effects of Carum copticum L. and Some of Its Constituents

Carum copticum L. has been used traditionally for its various therapeutic effects. The plant contains various components such as thymol and carvacrol. Different therapeutic effects such as antifungal, antioxidant, antibacterial, antiparasitic, and antilipidemic were described for the plant and its constituents. Therefore, antiinflammatory, antioxidant, and immunological effects of C. copticum and its constituents, thymol and carvacrol, were discussed in the present review. Previous studies have shown potent antiinflammatory, antioxidant, and immunological effects for C. copticum and its constituents, thymol and carvacrol. Therefore, the plant and its constituents have therapeutic values in several inflammatory and immunological disorders as well as in the oxidative stress conditions. Copyright © 2014 John Wiley & Sons, Ltd.     

Pharmacokinetic and pharmacodynamic drug interactions with Kava (Piper methysticum Forst. f.)

Kava kava, a beverage or extract prepared from the rhizome of the kava plant (Piper methysticum Forst. f.), was used for many centuries as a traditional beverage in the Pacific Islands. During the past few decades, kava has also gained popularity in Western countries as well, due to its anxiolytic and sedative properties. However, in recent years, kava has been implicated in several liver failure cases which led to its ban in many countries and this has prompted wide discussion on its relative benefits and risks as a social beverage and a herbal remedy. Recently, it has been shown that several kavalactones, the assumed active principles of kava extracts, are potent inhibitors of several enzymes of the CYP 450 system (CYP1A2, 2C9, 2C19, 2D6, 3A4 and 4A9/11). This indicates that kava has a high potential for causing pharmacokinetic drug interactions with other herbal products or drugs, which are metabolised by the CYP 450 enzymes. In addition, several pharmacodynamic interactions have been postulated and indeed observed. Nevertheless, evidence of true pharmacokinetic and/or pharmacodynamic interactions remains unsubstantiated, and only few investigations of the potential of kava preparations to interact with specific drugs have been carried out. This review provides a critical overview of the existing data on interactions of kava with other drugs and concludes that there is an urgent need for further in vitro and in vivo investigations to fully understand clinically significant interactions with kava that have the potential to cause adverse effects or toxicity in kava users.     

The neuroprotective properties of the Ginkgo biloba leaf: a review of the possible relationship to platelet-activating factor (PAF)

Ginkgo biloba (Ginkgoaceae) is an ancient Chinese tree which has been cultivated and held sacred for its health-promoting properties. There is substantial experimental evidence to support the view that Ginkgo biloba extracts have neuroprotective properties under conditions such as hypoxia/ischemia, seizure activity and peripheral nerve damage. Research on the biochemical effects of Ginkgo biloba extracts is still at a very early stage. One of the components of Ginkgo biloba, ginkgolide B, is a potent platelet-activating factor (PAF) antagonist. Although the terpene fraction of Ginkgo biloba, which contains the ginkgolides, may contribute to the neuroprotective properties of the Ginkgo biloba leaf, it is also likely that the flavonoid fraction, containing free radical scavengers, is important in this respect. Taken together, the evidence suggests that Ginkgo biloba extracts are worthy of further investigation as potential neuroprotectant agents.     

CNS depressant effects,anti-inflammatory activity and anti-cholinergic actions of Santolina chamaecyparissus extracts

The pharmacological activity of several extracts together with the lyophilized infusion of S. chamaecyparissus ssp. squarrosa were investigated. The lethal dose 50% (LD₅₀), effect on animal metabolism, mechanical and thermic analgesia and spontaneous, anti-inflammatory, and anti-ulcer activity have been determined. Studies on isolated organs (rat duodenum and rat uterus) were also carried out. The hexanic and chloroformic extracts were potent antagonists of the thermic analgesia test; the former extract was also active in the mechanical analgesia test. The chloroformic extract and, to a lesser extent, the ethyl acetate extract and lyophilized infusion demonstrated noteworthy activity as anti-inflammatory agents. No extract produced an ulcerogenic effect. The hexanic extract had the highest inhibitory effect on ACh induced contraction of rat duodenum and the ethyl acetate extract of oxytocin induced contraction of rat uterus.     

Antioxidant approach to disease management and the role of 'Rasayana' herbs of Ayurveda

The disease preventive and health promotive approach of 'Ayurveda', which takes into consideration the whole body, mind and spirit while dealing with the maintenance of health, promotion of health and treating ailments is holistic and finds increasing acceptability in many regions of the world. Ancient Ayurvedic physicians had developed certain dietary and therapeutic measures to arrest/delay ageing and rejuvenating whole functional dynamics of the body system. This revitalization and rejuvenation is known as the 'Rasayan chikitsa' (rejuvenation therapy). Traditionally, Rasayana drugs are used against a plethora of seemingly diverse disorders with no pathophysiological connections according to modern medicine. Though, this group of plants generally possesses strong antioxidant activity, only a few have been investigated in detail. Over about 100 disorders like rheumatoid arthritis, hemorrhagic shock, CVS disorders, cystic fibrosis, metabolic disorders, neurodegenerative diseases, gastrointestinal ulcerogenesis and AIDS have been reported as reactive oxygen species mediated. In this review, the role of free radicals in these diseases has been briefly reviewed. 'Rasayana' plants with potent antioxidant activity have been reviewed for their traditional uses, and mechanism of antioxidant action. Fifteen such plants have been dealt with in detail and some more plants with less work have also been reviewed briefly.     

银杏二萜内酯葡胺注射液与中性硼硅玻璃安瓿的药物相容性试验研究

目的：通过对银杏二萜内酯葡胺注射液与中性硼硅玻璃安瓿的药物相容性试验研究,确定中性硼硅玻璃安瓿作为银杏二萜内酯葡胺注射液内包装材料的可行性。方法：根据《药品包装材料与药物相容性试验指导原则》,进行以中性硼硅玻璃安瓿为包装材料的银杏二萜内酯葡胺注射液相容性研究。结果：中性硼硅玻璃安瓿与银杏二萜内酯葡胺注射液之间无迁移及吸附等质量变化,中性硼硅玻璃安瓿与银杏二萜内酯葡胺注射液具有较好的药物相容性。结论：中性硼硅玻璃安瓿可以作为银杏二萜内酯葡胺注射液的包装材料。     

基于中药有效成分族的方剂物质基础研究

本文以血管紧张素转化酶（Angiotensin Converting Enzyme，ACE）抑制剂、3-羟基-3-甲基戊二酰辅酶A还原酶（3-Hydroxy-3-Methylglutaryl Coenzyme A Reductase，HMG—CoAR）抑制剂和血管紧张素Ⅱ（AngiotensinⅡ，AngⅡ）、血小板活化因子（Platelet Activating Factor，PAF）受体拮抗剂三维药效团为辨识模型，以三维数据库柔性搜索技术为辨识算法，发现了18首活血化瘀方剂及其所合20味中药可能具有的ACE、AngⅡ、PAF和HMG—CoAR受体活性的物质基础。结果表明，中药有效成分族的研究将为从分子层次上揭示方剂物质基础提供方法学支撑。     

天然产物中的抗补体活性成分

补体系统的非正常激活会引发类风湿性关节炎、老年性痴呆、急性呼吸窘迫综合征以及系统性红斑狼疮等多种疾病。目前临床上尚无高效、低毒、专一的补体抑制剂。国内外已完成部分天然产物的筛选,发现自然界中广泛存在的某些多糖、黄酮、甾类和萜类化合物具有显著的抗补体活性。本文对天然产物类抗补体活性成分的研究方法、已发现活性化合物的化学结构以及体内外药理研究概况进行综述,并分析了天然产物类补体抑制剂的应用前景。     

Studies on the anti-allergic activity of Mikania glomerata.

A fraction (MG1) obtained from the ethanolic extract of Mikania glomerata Sprengel (Compositae), popularly known as 'guaco' and used as 'an' anti-allergic and anti-inflammatory agent, was evaluated for these properties on ovalbumin-induced allergic pleurisy and in models of local inflammation induced by biogenic amines, carrageenan and PAF. Plasma exudation as well as neutrophil and eosinophil infiltration evoked by the intrapleural injection of the antigen were significantly reduced by the fraction. Likewise, PAF-induced pleural neutrophil migration was inhibited by the treatment with MG1. On the other hand, pre-treatment of the animals with MG1 failed to modify the pleurisy induced by histamine, serotonin or carrageenan. These results suggest that MG1 is effective in inhibiting immunologic inflammation but did not affect acute inflammatory response caused by other agents.     

Glycogen synthase kinase-3 (GSK-3) inhibitory activity and structure-activity relationship (SAR) studies of the manzamine alkaloids. Potential for Alzheimer's disease

Manzamine A and related derivatives isolated from a common Indonesian sponge, Acanthostrongylophora, have been identified as a new class of GSK-3beta inhibitors. The semisynthesis of new analogues and the first structure-activity relationship studies with GSK-3beta are also reported. Moreover, manzamine A proved to be effective in decreasing tau hyperphosphorylation in human neuroblastoma cell lines, a demonstration of its ability to enter cells and interfere with tau pathology. Inhibition studies of manzamine A against a selected panel of five different kinases related to GSK-3beta, specifically CDK-1, PKA, CDK-5, MAPK, and GSK-3alpha, show the specific inhibition of manzamine A on GSK-3beta and CDK-5, the two kinases involved in tau pathological hyperphosphorylation. These results suggest that manzamine A constitutes a promising scaffold from which more potent and selective GSK-3 inhibitors could be designed as potential therapeutic agents for Alzheimer's disease.     

Clinical and experimental studies on polyherbal formulations for diabetes: current status and future prospective

Diabetes is a leading cause of morbidity and mortality in the world. There is currently an active search for antidiabetic drugs with greater effectiveness with fewer and less adverse side effects. Although numerous individual herbs have been experimentally or clinically reported to possess antidiabetic effects, considerably less research has been conducted on polyherbal compounds. It is believed that herbal compounds containing multiple plant products have synergistic antidiabetic effects and could enhance the desired actions. Several polyherbal formulations have been studied as therapeutic agents in diabetes management. To describe the current state of research on polyherbal compounds in the treatment of diabetes, an extensive review of literature was undertaken on several major databases. This paper presents what is known about the efficacy of these polyherbal formulations and compare their antidiabetic effects with those of current oral hypoglycemic drugs as reference. The percent decrease in blood glucose, lipids and other biochemical parameters achieved by each product in diabetic animals and patients is reported. Also, the possible mechanisms responsible for hypoglycemic action of polyherbal formulations are discussed.     

Pharmacological activity of Mentha longifolia and its phytoconstituents

Current paper reviews the pharmacological activities, therapeutic indications and phytochemicals of M. longifolia. This herb has been consumed traditionally for the treatment of various diseases, including gastrointestinal disorders, respiratory disorders, infectious diseases, inflammatory diseases, as well as menstrual disorders. In the modern era, various pharmacological activities have been confirmed for M. longifolia, such as anti-parasitic, antimicrobial, anti-insect, antimutagenic, antinociceptive, anti-inflammatory, antioxidant, keratoprotective, hepatoprotective, anti-diarrhea, and spasmolytic effects. The plant showed therapeutic benefits in irritable bowel syndrome, amenorrhea and oligomenorrhea, and oxidative stress-associated diseases as well. A vast variety of natural components such as flavonoids, phenolic acids, cinnamates, ceramides, sesquiterpenes, terpenes, and terpenoids have been suggested to be responsible for the pharmacological action of M. longifolia. These natural products can be considered as novel medicinal sources for developing new drugs. Further investigations to explore therapeutic efficacy, tolerability,and pharmaceutical properties of M. longifolia phytochemical agents are recommended.     

Traditional antimalarials and the development of novel antimalarial drugs

Malaria continues to be a major cause of mortality and morbidity especially throughout the developing world. In the last 25 years or so a number of significant advances have been made that have the potential to make a major contribution to the control of this disease. The discovery of artemisinin and its analogues as potent antimalarial agents have been of immense importance and the latter, as well as some other selected developments are outlined in this brief review.