蛹虫草化学成分及药理作用研究进展

蛹虫草作为传统的中药,是一种能寄生在鳞翅目昆虫蛹及幼虫上的菌虫复合体。化学成分和药理研究表明,其含有包括核苷类、多糖类、糖醇、甾醇类以及SOD酶在内的多种有效成分,在免疫调节、抗肿瘤、抑菌抗炎、抗氧化衰老等方面有很强的活性,具有重要的研究和开发价值。文章从蛹虫草的化学成分及药理作用方面展开综述。     

蛹虫草化学成分及药理作用研究进展

综述近年蛹虫草化学成分及药理作用研究进展。蛹虫草的化学成分有核苷类、多糖类、虫草酸、虫草素、甾醇类以及氨基酸和微量元素等,其药理作用广泛,主要对神经系统、循环系统以及免疫系统等多种疾病疗效显著。     

蛹虫草的化学成分、药理作用及产业化研究进展

蛹虫草Cordyceps militaris是食药两用真菌,在传统医学中应用广泛,并于2009年被我国卫生部批准为新资源食品。已有研究表明,蛹虫草提取物及其活性成分（虫草多糖、虫草素等）具有多种药理作用。从化学成分、体内/体外药理作用和产业化现状3个方面对蛹虫草相关文献进行梳理,对其调节免疫、抗肿瘤、调血脂、神经保护等药理作用及其相关大健康产品进行综述,并指出蛹虫草在药效物质基础发现、大健康产品研发方面存在的问题及解决思路,以期充分发掘其菌种资源,创造更大的医药价值、经济价值和社会价值。     

北虫草的化学成分及药理作用

北虫草是一种药食两用真菌,在保健食品和药品行业日益成为热点。近10年研究表明,北虫草主要含有虫草素、腺苷、乙酰基虫草素等多种核苷、虫草多糖、氨基酸和无机元素的化学成分;药理研究显示北虫草中核苷和多糖类成分在抗肿瘤、抗炎、抗老化、免疫调节等方面有较为明显的作用。但有效成分的分离纯化制约着产业化的发展,北虫草有效成分药理作用机制研究也有待补足。     

蛹虫草有效成分及药理作用研究进展

蛹虫草是传统的中药,化学成分和药理研究表明,其含有包括核苷类、多糖类、糖醇、甾醇类以及SOD酶在内的多种有效成分,具有镇静催眠、提高机体免疫力、抗肿瘤、防止衰老、保护心肺组织等多种药理作用,因此对蛹虫草的有效成分和药理作用进行了综述.     

蛹虫草化学成分研究

从蛹虫草菌丝中分离出六种化学成分。经结构鉴定为β-谷甾醇,麦角甾醇,D-甘露醇,腺嘌呤,腺苷及虫草素(3′-脱氧腺苷)。从蛹虫草菌丝中分离出虫草素、腺嘌呤及麦角甾醇尚属首次。     

虫草素的药理作用研究进展

虫草素是从蛹虫草Cordyceps militari中分离的核苷类抗生素,并已成功地从人工培育的蛹虫草子实体中提取到,质量分数98％以上.虫草素不仅具有抗肿瘤、抗白血病、免疫调节等作用,还具有抗菌、消炎、抗病毒、降血糖、降血脂、抗衰老等多种生物活性和药理作用.近年来虫草素已引起国内外研究人员的极大关注,主要对虫草素的生物活性和药理作用研究概况进行综述.     

人工蛹虫草化学成分研究

人工蛹虫草Cordyceps militaris(L.)Link又称北冬虫夏草，与冬虫夏草同属麦角菌科虫草属。北方民间曾把蛹虫草作为冬虫夏草应用。《新华本草纲要》记载其“性平，味甘，有益肺肾，补精髓，止血化痰”等功效，用于肺结核及老人虚弱和贫血等症,为珍贵的中药材。目前由于人们疯狂搜寻挖掘冬虫     

蛹虫草研究进展

概述了蛹虫草的化学成分、药理作用,并讨论其不良反应与可能的物质基础。     

复方蛹虫草制剂对C57BL/6荷瘤小鼠免疫功能的影响

目的:研究蛹虫草复方制剂(CCM)对C57BL/6荷瘤小鼠免疫功能影响.方法:C57 BL/6雄性小鼠腋下皮下注入Lewis肺癌小鼠移植瘤动物模型,将荷瘤鼠分为模型组、阳性对照组以环磷酰胺ip 20 mg· kg-,复方蛹虫草制剂低、中、高剂量组(1.2,2.5,7.5)g·kg-1ig给药,连续给药14 d,以抑瘤率为指标考察CCM的体内抗肿瘤活性,分别测定其抑瘤率、T淋巴细胞亚群CD4 +/CD8+;荷瘤小鼠血清中白细胞介素-2(IL-2)、白细胞介素-12(IL-12)、肿瘤坏死因子-α(TNF-α)水平;抗体生成细胞数以及力竭游泳时间.结果:CCM高剂量组(7.5 g·kg-1对肿瘤生长有明显的抑制作用(P＜0.05),其抑瘤率为40.3％,CCM高剂量组T淋巴细胞亚群CD3+,CD4+,CD4+/CD8+均高于模型对照组;同时中、高剂量组能显著提高荷瘤小鼠血清TNF-α,IL-2,IL-12的水平;抗体生成细胞数和力竭游泳时间也均高于荷瘤对照组(P＜0.05).结论:CCM具有提高荷瘤小鼠免疫功能的作用.     

Comparisons on enhancing the immunity of fresh and dry Cordyceps militaris in vivo and in vitro

Ethnopharmacological relevance

The immunomodulatory capacities of fresh Cordyceps militaris (FCM) and dry Cordyceps militaris (DCM) were compared.

Materials and methods

In vivo immunomodulatory assay, different doses of FCM and DCM were orally administrated over a period of 15 days in a cyclophosphamide (CY) induced immunosuppression mice; in vitro testing, the spleen cells were extracted from healthy mice and treaded with CY, then cultured with different dose of FCM or DCM; the contents of Cordyceps militaris polysaccharide (CMP), cordycepin, adenosine, total polyphenol (TP) and total flavonoids (TF) in FCM and DCM were measured.

Results

Our studys indicated that, FCM was significantly stronger than DCM on increasing the spleen and thymus indexes, spleen lymphocyte activity, macrophage function, and promoting the levels of IL-2, IFN-γ in vivo and in vitro. The contents of immunomodulatory CMP and TF in FCM were markedly higher than in DCM.

Conclusion

All these results suggested that FCM was superior to DCM on enhancing immunity.     

Constituents isolated from Cordyceps militaris suppress enhanced inflammatory mediator's production and human cancer cell proliferation

Aim of the study

The purpose of this study is to isolate the pure compounds from the extracts of Cordyceps militaris obtained through solid-state cultivation process, and evaluate their anti-inflammatory and anticancer properties.

Materials and methods

Silica gel column chromatographic purification of Cordyceps militaris extracts resulted in the isolation of 10 pure compounds (1-10). The compounds 1-10 were examined for their growth inhibitory properties against nitric oxide (NO), tumor necrosis factor (TNF)-α and interleukin (IL)-12 enhanced production from LPS/IFN-γ-stimulated macrophages. Additionally, the anti-proliferation effects of 1-10 on human cancer cell lines, colon (colon 205), prostate (PC-3), and hepatoma (HepG2) cells were also analyzed.

Results

Compound 8 displayed potent growth inhibition on NO, TNF-α and IL-12 production with an IC₅₀ value of 7.5, 6.3, and 7.6 μg/ml, respectively. A similar inhibitory trend on these inflammatory mediators was observed for 3, 7, 9 and 10 with an IC₅₀ values ranging from 10.8 to 17.2 μg/ml. On the other hand, compounds 3 and 8 were potent anti-proliferative agents with an IC₅₀ value of 35.6 and 32.6 μg/ml toward PC-3 and colon 205 cell lines, respectively. The compounds 1 and 2 showed potent anti-proliferation in PC-3 and colon 205 cells, while only 3 displayed such effect in HepG2 cells.

Conclusion

The present study provides scientific supporting information for the ethnopharmacological use of Cordyceps militaris as an anti-inflammatory and anticancer agent.     

Effect of Cordyceps militaris extract and active constituents on metabolic parameters of obesity induced by high-fat diet in C58BL/6J mice

Ethnopharmacological relevance

Cordyceps species which is well-known as ‘winter worm summer grass’ has long been used as tonics and stimulants to enhance energy, exhibiting a potential for energy metabolism. Clinical trials have suggested their beneficial effect on lipid metabolic disorders such as hyperlipidemia.

Materials and methods

The effect of Cordyceps militaris on metabolic parameters was investigated using C58BL/6J mice induced by high-fat diet (HFD). The effect was first determined by assessing the body and organ weight. For further investigation, sections of epididymal adipose tissue were stained with hematoxylin and eosin and the size of epididymal adipocyte was measured by Image analysis system. Fat accumulation in frozen liver sections was assessed by the Oil Red O staining and the plasma biochemical parameters were also assessed. Active constituents were characterized using chromatographic and spectroscopic analysis.

Results

The administration of Cordyceps militaris extract (CE) at the dose of 100 mg/kg and 300 mg/kg reduced body weight gain and food efficiency ratio induced by HFD. The amount of epididymal fat and size of adipocytes were also decreased by CE treatment. In addition, liver weight and fat deposition in liver were dramatically reduced in CE-treated group. The treatment of CE also showed beneficial effects on plasma parameters related to lipid profiles. Further study for the characterization of active constituents of Cordyceps resulted in the isolation of two new compounds such as cordyrroles A (1) and B (7) together with 12 known compounds including pyrrole alkaloids and nucleotide derivatives. Among the isolated compounds, cordyrrole A significantly inhibited adipocyte differentiation and pancreatic lipase activity, whereas cordyrrole B was more effective at inhibiting pancreatic lipase. Cordycepin, a characteristic compound of Cordyceps militaris, decreased the rate of adipocyte differentiation.

Conclusion

Treatment of CE inhibited HFD-induced metabolic disorders, mainly by improvement in metabolic parameters. As active constituents, pyrrole alkaloids and nucleotide derivatives were characterized. These results suggested that Cordyceps militaris might be beneficial for the treatment of metabolic disorders obesity through the combined actions of diverse constituents.     

冬虫夏草用药部位描述的商榷

对国家药典所载冬虫夏草用药部位的描述进行商榷。建议描述为:冬虫夏草为麦角菌科真菌冬虫夏草菌Cordyceps sinensis(Berk.)Sacc.侵染了蝙蝠蛾科昆虫幼虫而形成的成熟菌体及幼虫尸体的干燥复合体,对冬虫夏草的基原描述提出新的观点,为其描述的准确性提供新的参考。     

蛹虫草多糖的分离纯化及促胆固醇逆向转运研究

对蛹虫草子实体多糖进行分离纯化、相对分子质量测定、单糖组成分析和体内胆固醇逆向转运活性研究。采用阴离子交换色谱、分子排阻色谱分离纯化多糖,高效凝胶渗透色谱法测定相对分子质量,高效液相色谱结合柱前衍生法测定单糖组成,同位素示踪技术评价胆固醇转运活性。最终获得3种纯多糖组分CMBW1,CMBW2和CMYW1,糖含量依次为87%,89%,95%,蛋白含量依次为6.5%,1.3%,2.8%,相对分子质量依次为772.1,20.9,13.2 kDa;CMBW1由Man,GlcN,Rha,GlcUA,Glc,Gal和Ara构成,摩尔比例为7.25:0.17:1.29:0.23:6.30:11.08:0.79;CMBW2由Man,GlcN,Gal和Ara组成,摩尔比例为2.40:0.16:2.92:0.24;CMYW1由Man,GlcN,GlcUA和Glc组成,摩尔比例为0.59:0.57:0.45:25.61;蛹虫草多糖50 mg·kg^-1即可显著促进³H-胆固醇向小鼠血液转运和经由粪便排出。所得3种蛹虫草多糖组分均为杂多糖,所得蛹虫草多糖具有促胆固醇逆向转运功能。     

绵枣儿属药用植物化学成分和药理活性研究进展

绵枣儿属Scilla植物是百合科多年生草本,约90种,广布于欧洲、亚洲和非洲的温带地区,少数也见于热带山地。我国产1种和1变种,即绵枣儿和白绿绵枣儿。该属中多种植物可以药用,常被用于治疗跌打损伤,腰腿疼痛、筋骨痛等。该属植物的化学成分主要是尤可甾醇衍生的三萜及其糖苷、蟾蜍甾、高异黄酮、生物碱、二苯乙烯及少量的木脂素等。药理活性主要表现在抗菌、抗炎、抗氧化、抗肿瘤和糖苷酶抑制等方面。为了更好地开发利用本属药用植物,该文综述了其化学成分与药理活性的研究进展。     

虫草属EST-SSR标记系统的建立研究

目的:通过球孢虫草、蛹虫草EST设计EST-SSR引物,建立虫草属EST-SSR标记系统.方法:从NCBI公共数据库下载获得虫草EST,利用Sequece Seiners 1.2软件去除冗余序列并设计引物,进行PAGE电泳.结果:通过去除EST总序列中低质量的和冗余的序列后,得到全长为2 953 173 bp的4 556条无冗余球孢虫草EST.从中发掘出718个EST-SSR,分布于616条EST中,出现频率是15.8％.平均分布频率是每4 096 bp出现1个,三核苷酸重复序列有419个,是出现最多的重复类型.蛹虫草EST去冗余后得到1 363条无冗余EST,共含有1 117个EST-SSR,出现频率为81.95％,出现最多的重复类型是A核苷酸重复.根据球孢虫草EST-SSR序列,设计合成50对引物,有扩增产物的引物为34对,占总设计引物数的68％.根据蛹虫草EST-SSR,设计合成40对引物,有扩增产物的引物为39对,占总设计引物数的97.5％.基于SSR标记进行聚类分析,7种虫草无性型均能分开,且分为4支.结论:虫草属EST-SSR出现频率较高、类型较丰富、多态性潜能较高,具有较高的利用价值.球孢虫草和蛹虫草EST开发的SSR标记在虫草属有较好的转移性与通用性,可以很好的应用于虫草种间遗传关系的研究.应用虫草物种EST建立分子标记是一条简便而又有效的途径.     

Mycelia glycoproteins from Cordyceps sobolifera ameliorate cyclosporine-induced renal tubule dysfunction in rats

Ethnopharmacological relevance

Cordyceps sorbolifera has been used in Traditional Chinese Medicine for improving the renal function. Cyclosporine A (CsA) is an important immunosuppressive agent in the prevention of renal allograft rejection, but long-term usage of CsA could lead to chronic nephrotoxicity and renal graft failure. The study was aimed to investigate whether the mycelia glycoproteins of Cordyceps sobolifera (CSP) exert prevention effects on CsA-induced nephrotoxicity.

Materials and methods

Sprague-Dawley (SD) rats were randomly assigned into four groups (n=6 per group): normal saline (control group), CSP group, CsA group, and CSP-CsA group (CsA combined treatment with CSP). Glomerular and tubular functions were assessed and histological studies were performed.

Results

CSP, prepared by hot water extraction, ethanol precipitation and membrane dialysis, was found to be composed of three glycoproteins with average molecular weights of 543, 31, and 6.3 kDa, respectively. CsA impaired urea clearance and creatinine clearance were significantly improved by concomitant administration of CSP. TUNEL histochemical stain revealed that CSP significantly decreased CsA-induced apoptosis in renal tubular cells. The reducing effect of caspase-3 activation by CSP was suggested through the over-expression of the anti-apoptosis protein Bcl-2 in renal tubule cells. In assessment of CSP protection of renal tubule function, we found that CSP restored CsA induced magnesium wasting by increasing the magnesium reabsorption channels TRMP6 and TRMP7.

Conclusion

The results suggested that CSP had a significant suppressive activity on CsA-induced apoptosis and protective activity against nephron loss possibly via its restoring activity by increasing the magnesium reabsorption channels TRMP6 and TRMP7 on CsA induced magnesium wasting.