车前子临床应用拾偶

车前子,为车前科植物车前的成熟种子.车前子属甘寒之品,人肝、肾、肺、小肠、膀胱经,具有利水通淋,渗湿止泻,清肝明目,清肺祛痰止咳之功,可治小便不利,淋漓涩痛,湿热泄泻,目赤肿痛,眼目昏花,咳嗽痰多等症.     

附子的常用临床配伍

附子首载于<神农本草经>列为下品.为毛茛科多年生草本植物乌头的旁生块根.其味辛,性大热,有毒,归心、脾、肾经.主要功效为回阳救逆、助火补阳、温经散寒、除湿止痛,是治疗亡阳证、阳虚诸证、寒凝痛证之要药.因附子为纯阳燥烈之品,有毒,作用峻猛,且临床医生多缺乏其配伍及中毒防治知识,故多不敢用或用而不敢重用,致贻误病情.笔者总结了附子的常用临床配伍情况,现报道如下.     

车前子与马钱子

车前子与马钱子都是中医临床常用中药。从名称上看仅差一个字，但其药性、药效与配伍应用、剂量等均有着明显而严格的区分。文中所述之事就是去年河南发生的惨痛事实，我们特邀河南中医学院段振离教授撰写此文，希望能引起读者及有关人士们的注意与重视。     

车前子与伪品车前子的鉴别

车前子来源于车前科植物车前Plantago assatiala或Plantago depressa willd的干燥成熟种子。近年来，在市场上发现几种车前子的伪品，与正品车前子外观很相似，为保证用药安全有效，现将车前子及其几种伪品鉴别总结如下：     

浅析车前子在五子衍宗丸中的配伍意义

五子衍宗丸是治疗男性不育症的常用方剂,从古至今广为流传,被誉为"古今种子第一方",然而补肾填精的五子衍宗丸中为何配伍性偏通利的车前子。从方剂组成角度对五子衍宗丸中配伍车前子进行分析,旨在对五子衍宗丸有一个深入的了解,并初步探讨男性不育症方药治疗配伍理法,以便在临床中更好地运用。     

黄芪的不同配伍应用体会

为探索黄芪的配伍机制及临床意义,用黄芪配党参、白术、山药治疗慢性腹泻;配伍白术、防己、薏苡仁治疗水肿;配伍当归、赤芍、川芎治疗中风后遗症;配伍白术、防风、煅牡蛎治疗自汗。观察黄芪不同配伍的临床疗效。结果黄芪由于配伍不同,可以治疗多种疾病,从而确定了黄芪在临床中不同配伍的药效及机制。黄芪的不同配伍机理及作用,对临床具有重要的指导意义。     

浅议中药葛根的临床配伍运用

目的:探讨葛根的临床配伍运用,为使其在更广泛的医疗实践中发挥作用提供参考。方法:将近年来有关报道及临床经验加以总结,将传统理论与现代药理相结合。结果:巧妙配伍使葛根的临床应用更为广泛且疗效显著。结论:中药葛根来源丰富且临床应用广泛。     

浅谈龙胆草在皮肤科临床配伍运用

龙胆草性寒味苦,其主要功效为泻肝胆实火,清下焦湿热。它在中医内科临床有着较为广泛的运用,且疗效卓著。著名方剂龙胆泻肝汤（丸）,当归龙荟丸等堪称龙胆草在内科临床配伍运用之典范,兹就该药在皮肤科临床的配伍运用谈一点粗浅的认识。１脂溢性皮炎、痤疮脂溢性皮炎...     

Immunomodulatory activity of the seeds of Plantago asiatica L.

Ethnopharmacological relevance

The seeds of Plantago asiatica L. were often used as a traditional Chinese medicine for some immunologically weak patients suffering from chronic illness. These uses could be related to immunomodulatory properties of the plant.

Aim of the study

In this study, effects of extract of the seeds of Plantago asiatica L. (ES-PL) were investigated on the maturation of dendritic cells (DCs), which play significant role in primary immune system.

Materials and methods

The phenotypes of DCs were analyzed by using flow cytometry while phagocytosis was assessed by the uptake of FITC-dextran. Antigen presenting ability to allogeneically naïve or syngeneically primed T lymphocytes was examined by the lymphocyte proliferation of mixed lymphocyte reaction (MLR). In addition, the level of chemokine receptor CCR7 mRNA was determined by RT-PCR.

Results

DCs treated with ES-PL expressed higher levels of MHC class II molecules and major costimulatory molecules such as CD80 and CD86. Functional maturation of DCs treated with ES-PL was confirmed by decreased mannose receptor-mediated endocytosis and increased antigen presenting abilities to allogeneically naïve or syngeneically primed T lymphocytes. The CCR7 mRNA expression in DCs treated with ES-PL was also enhanced.

Conclusions

These results indicated that ES-PL could induce the maturation of murine DCs.     

山药和麦冬的配伍机制及其临床运用

目的:探索山药和麦冬配伍机制及临床意义,了解配伍在临床应用中的重要性.方法:山药和麦冬均为临床常用中药,基于药对配伍的原则、药对配伍组合特点及现代研究认识等,笔者通过研究历代及近现代文献,对山药和麦冬配伍组成的现代科学内涵及其临床运用进行了分析与探讨.结果:山药和麦冬配伍主要运用于润肺滋阴、补肺美肤、延年益寿3个方面.结论:山药和麦冬的配伍机制灵活,临床运用广泛,为临床用药提供一些新的思路.     

飞龙掌血乙醇提取物对白色念珠菌抑菌作用的研究

目的:研究飞龙掌血乙醇提取物体外抑制白色念珠菌生长作用,为进一步开发根管消毒新药提供理论依据.方法:微量肉汤稀释法确定飞龙掌血乙醇提取物体外抑制白色念珠菌生长的最小抑菌浓度(MIC)及最小杀菌浓度(MBC);常规扫描电镜制样,观察细菌细胞形态的变化;采用RT-PCR技术获得互补DNA,PCR技术扩增白色念珠菌毒力因子SNF2和PDE2基因片段,产物进行电泳分析.结果:飞龙掌血乙醇提取物对白色念珠菌的最小抑菌浓度为7.5 g·L-1,最小杀菌浓度为15.0 g·L-1;扫描电镜观察药物作用后菌体呈现不规则形态,表面有明显的凹陷、裂痕;随着药物浓度增加,毒力因子SNF2和PDE2的表达量呈明显下降趋势.结论:飞龙掌血乙醇提取物对白色念珠菌有较好的抑菌活性;推断该药物是通过抑制或干扰毒力因子SNF2和PDE2转录过程的表达,从而抑制致病性菌丝形态的形成及破坏细菌细胞壁的完整性,达到抑菌作用.     

通关藤抗肿瘤作用机制研究进展

归纳整理近年来各期刊报道的通关藤抗肿瘤作用机制研究方面的文献.查阅万方,中国知网等大型数据库及国外数据库,查阅近年来各专家学者对通关藤及其制剂抗肿瘤作用机制的研究论文.通关藤提取物及消癌平系列制剂,在体内外均有一定的活性,对多种肿瘤细胞有抑制作用,通过多种途径发挥抗肿瘤作用:干扰DNA的合成,抑制肿瘤细胞的增殖、改变细胞跨膜电位、调控基因表达、抑制肿瘤血管生成,调节机体免疫系统等.近年来学者专家们对通关藤进行了大量的药理作用及作用机制研究,但对具体起效成分作用机制研究较少.因此有必要对起效成分进行深入研究.     

Antimalarial and safety evaluation of extracts from Toddalia asiatica (L) Lam. (Rutaceae)

Ethnopharmacological relevance

Toddalia asiatica (L) Lam. (Rutaceae) is a medicinal plant traditionally used in Kenya by many communities for the treatment of malaria and other ailments. All parts of the plant are claimed to have medicinal value, but the root bark in particular is believed to be more potent. Decoctions or infusions of the roots are taken orally to treat malaria, fever and stomach ache.

Aim of the study

To evaluate antimalarial activity of aqueous and organic extracts prepared from Toddalia asiatica and determine in vitro and in vivo safety of the extracts.

Materials and methods

Aqueous, ethyl acetate, hexane and methanol extracts were obtained from Toddalia asiatica root bark, fruits and leaves. In vitro antiplasmodial activity was done using chloroquine-sensitive (D6) and chloroquine-resistant (W2) Plasmodium falciparum strains and the concentration causing 50% inhibition of radioisotope incorporation (IC₅₀) was determined. In vivo assay was done by administering mice infected with Plasmodium berghei four consecutive daily doses of the extracts through oral route following Peters 4-Day suppressive test. The percentage suppression of parasitaemia was calculated for each dose level by comparing the parasitaemia in untreated control with those of treated mice. Quinine hydrochloride was used as positive control while double distilled water or 20% Tween-80 was used as a negative control. In vivo acute toxicity was determined in mice using standard procedures. In vitro cytotoxicity assay was carried out using actively dividing sub-confluent Vero cells.

Results

Inhibitory concentrations of ethyl acetate extract of Toddalia asiatica fruits showed high activity against chloroquine resistant (W2) strains of Plasmodium falciparum (IC₅₀=1.87 μg/ml), followed by root bark aqueous extract (IC₅₀=2.43 μg/ml). Tested in vivo against Plasmodium berghei, the fruit ethyl acetate extract (500 mg/kg) and root bark aqueous extract (250 mg/kg) reduced malaria parasitaemia by 81.34% and 56.8% respectively. Higher doses were found to be less effective in vivo. Acute toxicity and cytotoxictiy of the tested extracts, with the exception of hexane extract from the roots, showed LD₅₀>1000 mg/kg and CC₅₀>100 μg/ml respectively.

Conclusions

The results obtained contribute to the validation of traditional use of Toddalia asiatica and provides in vivo and safety data of the plant extracts tested for the first time. Ethyl acetate extract of the fruits was active against chloroquine resistant Plasmodium falciparum as well as against Plasmodium berghei. These findings confirm the suitability of Toddalia asiatica as a good candidate for further tests to obtain a prototype for antimalarial medicine.     

In vitro modulatory effects on three major human cytochrome P450 enzymes by multiple active constituents and extracts of Centella asiatica

Ethnopharmacological relevance

Centella asiatica (CA) has been widely cultivated as a vegetable or spice in China, Southeast Asia, India, Sri Lanka, Africa, and Oceanic countries and traditionally used for wound healing and maintaining normal blood pressure.

Aim of the study

The present study was carried out to examine the potential modulatory effects of three commercially available active components (asiaticoside, asiatic acid and madecassic acid) and four extracts (aqueous, ethanol, dichloromethane and hexane) of CA on three major cDNA-expressed human cytochrome P450 (CYP) isoforms.

Materials and methods

High-performance liquid chromatography (HPLC)-based enzyme assays, namely tolbutamide 4-methyhydroxylase, dextromethorphan O-demethylase and testosterone 6β-hydroxylase assays were developed to probe activities of CYP2C9, CYP2D6 and CYP3A4, respectively. Probe substrates were incubated with or without each active component and extract for each isoform, followed by examination of the kinetics parameters, IC₅₀ and K_i, to characterize modulatory effects.

Results

CYP2C9 was more susceptible to inhibitory effects by CA extracts compared to CYP2D6 and CYP3A4. Moderate degree of inhibition was observed in ethanol (K_i = 39.1 μg/ml) and dichloromethane (K_i = 26.6 μg/ml) extracts implying potential risk of interaction when CYP2C9 substrates are consumed with CA products. The two extracts however showed negligible inhibition towards CYP2D6 and CYP3A4 (IC₅₀'s of 123.3 μg/ml and above). Similarly CA aqueous and hexane extracts did not significantly inhibit all three isoforms investigated (IC₅₀'s of 117.9 μg/ml and above). Among the active constituents investigated, asiatic acid and madecassic acid appeared to selectively inhibit CYP2C9 and CYP2D6 more than CYP3A4. Of particular interest is the potent inhibitory effect of asiatic acid on CYP2C9 (K_i = 9.1 μg/ml). This signifies potential risk of interaction when substrates for this isoform are taken together with CA products with high asiatic acid content. Inhibitions of asiatic acid with the other isoforms and that of madecassic acid with all isoforms were only moderate (K_i's ranged from 17.2 to 84.4 μg/ml). On the other hand, the IC₅₀ values for asiaticoside were high (1070.2 μg/ml or above) for all three isoforms, indicating negligible or low potential of this compound to modulate CYP enzymatic activity.

Conclusion

Centella asiatica extracts and active constituents inhibited CYP2C9, CYP2D6 and CYP3A4 activities with varying potency with CYP2C9 being the most susceptible isoform to inhibition. Significant inhibition was observed for asiatic acid and CA ethanol and dichloromethane extracts, implying involvement of semipolar constituents from CA in the effect. This study suggested that CA could cause drug–herb interactions through CYP2C9 inhibition.     

Antibacterial and antifungal activity of Flindersine isolated from the traditional medicinal plant, Toddalia asiatica (L.) Lam.

Aim of the study

The leaves and root of Toddalia asiatica (L.) Lam. (Rutaceae) are widely used as a folk medicine in India. Hexane, chloroform, ethyl acetate, methanol and water extracts of Toddalia asiatica leaves and isolated compound Flindersine were tested against bacteria and fungi.

Materials and methods

Antibacterial and antifungal activities were tested against bacteria and fungi using disc-diffusion method and minimum inhibitory concentrations (MICs). The compound was confirmed using X-ray crystallography technique.

Results

Antibacterial and antifungal activities were observed in ethyl acetate extract. One active principle Flindersine (2,6-dihydro-2,2-dimethyl-5H-pyrano [3,2-c] quinoline-5-one-9cl) was isolated from the ethyl acetate extract. The MIC values of the compound against bacteria Bacillus subtilis (31.25 μg/ml), Staphylococcus aureus (62.5 μg/ml), Staphylococcus epidermidis (62.5 μg/ml), Enterococcus faecalis (31.25 μg/ml), Pseudomonas aeruginosa (250 μg/ml), Acinetobacter baumannii (125 μg/ml) and fungi Trichophyton rubrum 57 (62.5 μg/ml), Trichophyton mentagrophytes (62.5 μg/ml), Trichophyton simii (62.5 μg/ml), Epidermophyton floccosum (62.5 μg/ml), Magnaporthe grisea (250 μg/ml) and Candida albicans (250 μg/ml) were determined.

Conclusions

Ethyl acetate extract showed promising antibacterial and antifungal activity and isolated compound Flindersine showed moderate activity against bacteria and fungi.     

香附提取物的抗抑郁活性及其作用机制研究

目的:筛选香附抗抑郁活性部位并初步探讨其抗抑郁作用机制.方法:小鼠ig香附各提取物给药量均为10 g?kg -1,阳性对照药氟西汀(0.08 g?kg-1),连续给药15 d后进行测试,采用小鼠强迫游泳实验和小鼠尾悬挂实验对香附醇提物及其各极性部位进行抗抑郁活性筛选,继而采用反相高效液相色谱法测定大脑额叶皮质中单胺类神经递质含量变化,探讨香附抗抑郁作用机制.结果:香附醇提取物的乙酸乙酯萃取部位和正丁醇萃取部位与对照品氟西汀类似,均能显著缩短小鼠游泳和悬尾的不动时间,乙酸乙酯萃取部位活性强于正丁醇萃取部位.乙酸乙酯萃取部位和正丁醇萃取部位可明显升高小鼠大脑额叶皮质5-羟色胺(5-HT)和多巴胺(DA)含量(P＜0.01),去甲肾上腺素(NE)含量无明显改变.结论:香附醇提物乙酸乙酯萃取部位和正丁醇萃取部位对“行为绝望”动物模型有较明显的抗抑郁作用,其作用机制可能与调节脑内单胺类神经递质5-HT和DA的含量有关.     

锡叶藤种质资源调查

目的:开展锡叶藤种质资源调查,为锡叶藤种质资源的综合评价及筛选优良种质奠定基础。方法:采用走访、实地调查及文献查阅相结合的方法,对锡叶藤种质资源的地理分布及生境、生物学特性、群落特征和伴生植物等进行调查。结果:锡叶藤主要分布的区域是广东、广西、海南,间断分布于海拔0~681 m的区域,平均海拔179 m,在中国的水平分布范围主要是N 18°01'~23°75',垂直分布在E 101°37'~118°05',超出此范围的分布比较少或无分布。适宜的生境为亚热带常绿阔叶林和南亚热带季风常绿阔叶林下,喜欢生长在潮湿炎热的地区的阴湿沟谷或山坡林下或灌木丛中,湿度70%~91%。生长地的年均气温18.3~25.4℃,降雨量1 112.1~2 996.8 mm。结论:该调查初步明确锡叶藤的地理分布特点、生物学特性、伴生植物群落种类,热量因子及湿度是锡叶藤分布的主要限制指标。通过对其种质资源调查及主要有效成分分析发现,锡叶藤种质资源丰富,尤其生长在广东、香港一带的植被保护较好、药材质量好。同时对锡叶藤的应用前景做了分析,为锡叶藤资源的保护、开发、利用提供了参考依据。