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...     

3种虫草抗氧化活性的研究

目的研究蒙山虫草、蛹虫草、冬虫夏草等 3种虫草水提液的抗氧化活性 ,并考察实验条件对结果的影响。方法采用邻苯三酚自氧化法测定 3种虫草的抗氧化活性。结果 3种虫草的抗氧化活性都较强 ,且比较接近。结论 3种虫草具有较强的抗氧化活性 ,具有延缓衰老的功效。     

苯酚-硫酸法测定蛹虫草中多糖含量

蛹虫草(Cordyceps militaris),别名北冬虫夏草、北虫草。野生蛹虫草具有多种药用价值、滋补功能,可与人参、鹿茸相媲美。其所含的虫草素、甘露醇、SOD等成分,均达到或超过名贵中药冬虫夏草。具有抗疲劳、抗衰老、增强免疫和性功能等作用,可杀灭喉癌细胞,能补肺益肾壮阳,有扶虚损、益精气、止血、化痰、镇静、免疫等多种功能。其有效活性成分虫草多糖(CMPS)被认为是非特异性免疫调节剂,可激活肌体的免疫活性细胞。本文通过苯酚-硫酸法,测定蛹虫草中多含量,此方法简便、结果准确、重现性好、颜色稳定。因此,可采用苯酚-硫酸法测定蛹虫草中…     

蛹虫草富锗胞外多糖对大鼠长期毒性研究

<正>蛹虫草(Cordyceps militaris)含有虫草多糖和虫草素等重要的生物活性成分,具有抗真菌、抗病毒、抗肿瘤、抗衰老、增强免疫力等多方面的药理作用[1-3]。有机锗是一种生物活性很高的物质,具有诱发自身干扰素,增加NK细胞活性,活化巨噬细胞,抗脂质过氧化,抗肿瘤,抗病毒,降血脂,清除自由基等多重医疗保健功能;同时对骨质疏松、高血压、糖尿病等也有一定疗效,含锗食物和药物被认为是治疗癌症和艾滋病的主要药品之一[4-8]。     

北冬虫夏草粉剂的亚慢性毒性试验

冬虫夏草(Cordyceps sinensis)简称虫草,是一种虫生真菌,常用作为传统的名贵药材。现代药物研究表明虫草中含有甘露醇、腺苷、腺嘌呤和尿苷等多种成分,具有多种药理作用[1]。药理研究表明,人工培育的北冬虫夏草,又称蛹虫草,毒性低,与天然冬虫夏草具有相似的作用[2]。目前蛹虫草的研究多限于药理作用等方面的探讨,而针对蛹虫草的毒理学研究则少有报道。本试验通过大鼠90 d喂养试验,阐明蛹虫草的亚慢性毒性,为蛹虫草的开发利用提供安全性参考。1材料与方法1·1受试物北冬虫夏草粉剂,黄色粉末,按照《食品安全性毒理学评价程序和检验方法》采用…     

略述北冬虫夏草生物活性物质的应用(临床)试验研究

冬虫夏草(虫草)是具有多种用途的生物资源,在其频临灭绝,用量大增的情况下,人工培育的北冬虫夏草(蛹虫草)是代替虫草的较佳新品种,新资源。据研究发现,蛹虫草有多种生物活性物质,大致可分为腺苷类、多糖类、环状肽类、酶类等等,与虫草基本相同。多种实验研究表明,蛹虫草内含的生物活性物质,具有1.抗细菌和真菌、病毒、癌和杀虫;2.调节免疫,3.抗幅射等;作用与虫草相同。     

蛹虫草液体发酵产物冻干粉的抗氧化活性及保肝作用

目的 研究蛹虫草液体发酵产物冻干粉的抗氧化活性及保肝作用。方法 采用真空冷冻干燥的方法将蛹虫草液体发酵产物制成干粉并对冻干粉主要成分进行分析测定,通过DPPH自由基清除实验和衰老小鼠模型验证蛹虫草发酵产物冻干粉的抗氧化活性,通过小鼠急性肝损伤实验研究冻干粉的保肝作用,采用急性毒性试验验证冻干粉的安全性。结果 蛹虫草发酵产物冻干粉含丰富的粗纤维、粗多糖、粗三萜及黄酮类物质。蛹虫草发酵产物冻干粉对DPPH自由基的半数有效浓度（EC₅₀）为8.12 mg/mL,在16 mg/mL时对DPPH自由基的清除率为61.56%,与0.02 mg/mL的维生素C（Vc）清除能力相当;蛹虫草发酵产物能显著提高衰老模型小鼠血清和肝脏中的总超氧化物歧化酶（T-SOD）、谷胱甘肽过氧化物酶（GSH-px）活力水平,降低丙二醛（MDA）含量,高剂量组的抗衰老效果与阳性药Vc组的抗氧化能力相当。小鼠急性肝损伤试验结果显示,冻干粉能有效降低模型组小鼠血液中门冬氨酸氨基转移酶（AST）与丙氨酸氨基转移酶（ALT）水平（P＜0.05）。冻干粉的半数致死量（LD₅₀）远大于国家无毒标准15 g/kg,属于无毒级别。结论 蛹虫草发酵产物具有良好的抗氧化活性和保肝作用,且安全无毒。     

蛹虫草提取物对内毒素引起小鼠急性肺损伤的保护作用

目的 :观察蛹虫草提取物对内毒素引起小鼠急性肺损伤的保护作用。方法 :建立内毒素急性损伤小鼠肺病理模型 ,造模 4和 8h后 ,用蛹虫草提取物治疗 ,造模 2 4h后 ,对血细胞和肺灌洗液中细胞进行计数并测定肺灌洗液中蛋白酶的活性和蛋白的含量。结果 :蛹虫草提取物对血液成分没有明显影响 ,但可以使肺灌洗液中白细胞、粒细胞的含量有所降低 ,而淋巴细胞和单核细胞的数量有所增加 ,蛋白酶活性降低。结论 :蛹虫草提取物可调节机体组织的免疫功能 ,可以缓解由于内毒素或类似物质造成的肺部炎症 ,具有一定的肺保护作用。     

蛹虫草液体发酵产物冻干粉的抗氧化活性及保肝作用

目的研究蛹虫草液体发酵产物冻干粉的抗氧化活性及保肝作用。方法采用真空冷冻干燥的方法将蛹虫草液体发酵产物制成干粉并对冻干粉主要成分进行分析测定,通过DPPH自由基清除实验和衰老小鼠模型验证蛹虫草发酵产物冻干粉的抗氧化活性,通过小鼠急性肝损伤实验研究冻干粉的保肝作用,采用急性毒性试验验证冻干粉的安全性。结果蛹虫草发酵产物冻干粉含丰富的粗纤维、粗多糖、粗三萜及黄酮类物质。蛹虫草发酵产物冻干粉对DPPH自由基的半数有效浓度（EC50）为8．12mg／mL,在16mg／mL时对DPPH自由基的清除率为61．56％,与0．02mg／mL的维生素C（Vc）清除能力相当;蛹虫草发酵产物能显著提高衰老模型小鼠血清和肝脏中的总超氧化物歧化酶（T-SOD）、谷胱甘肽过氧化物酶（GSH-px）活力水平,降低丙二醛（MDA）含量,高剂量组的抗衰老效果与阳性药Vc组的抗氧化能力相当。小鼠急性肝损伤试验结果显示,冻干粉能有效降低模型组小鼠血液中门冬氨酸氨基转移酶（AST）与丙氨酸氨基转移酶（ALT）水平（P〈0．05）。冻干粉的半数致死量（LD50）远大于国家无毒标准15g／kg,属于无毒级别。结论蛹虫草发酵产物具有良好的抗氧化活性和保肝作用,且安全无毒。     

冬虫夏草多糖的药理学研究进展

虫草多糖（Cordyceps．Polysacchride，CP）是冬虫夏草的主要活性成分之一，具有抗肝纤维化、免疫调节、抗肿瘤、降血糖等多方面的作用。本文对CP的生物学活性及其可能的药理机制进行综述。     

Synthesis,Cytotoxicity and Antileishmanial Activity of Some N-(2-(indol-3-yl)ethyl)-7-chloroquinolin-4-amines

We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3) . Hydrolysis of the methyl ester adduct (5) yielded the free acid (6) . The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.     

Lung disease and PKCs

The lung offers a rich opportunity for development of therapeutic strategies focused on isozymes of protein kinase C (PKCs). PKCs are important in many cellular responses in the lung, and existing therapies for pulmonary disorders are inadequate. The lung poses unique challenges as it interfaces with air and blood, contains a pulmonary and systemic circulation, and consists of many cell types. Key structures are bronchial and pulmonary vessels, branching airways, and distal air sacs defined by alveolar walls containing capillaries and interstitial space. The cellular composition of each vessel, airway, and alveolar wall is heterogeneous. Injurious environmental stimuli signal through PKCs and cause a variety of disorders. Edema formation and pulmonary hypertension (PHTN) result from derangements in endothelial, smooth muscle (SM), and/or adventitial fibroblast cell phenotype. Asthma, chronic obstructive pulmonary disease (COPD), and lung cancer are characterized by distinctive pathological changes in airway epithelial, SM, and mucous-generating cells. Acute and chronic pneumonitis and fibrosis occur in the alveolar space and interstitium with type 2 pneumocytes and interstitial fibroblasts/myofibroblasts playing a prominent role. At each site, inflammatory, immune, and vascular progenitor cells contribute to the injury and repair process. Many strategies have been used to investigate PKCs in lung injury. Isolated organ preparations and whole animal studies are powerful approaches especially when genetically engineered mice are used. More analysis of PKC isozymes in normal and diseased human lung tissue and cells is needed to complement this work. Since opposing or counter-regulatory effects of selected PKCs in the same cell or tissue have been found, it may be desirable to target more than one PKC isozyme and potentially in different directions. Because multiple signaling pathways contribute to the key cellular responses important in lung biology, therapeutic strategies targeting PKCs may be more effective if combined with inhibitors of other pathways for additive or synergistic effect. Mechanisms that regulate PKC activity, including phosphorylation and interaction with isozyme-specific binding proteins, are also potential therapeutic targets. Key isotypes of PKC involved in lung pathophysiology are summarized and current and evolving therapeutic approaches to target them are identified.     

Gender-related symptoms and correlates of alcohol dependence among men and women with a lifetime diagnosis of alcohol use disorders

This study explored gender-related symptoms and correlates of alcohol dependence in a crosssectional study of 150 men and 150 women with a lifetime diagnosis of alcohol use disorders (AUD). Participants were recruited in equal numbers from treatment settings, correctional centres and the general community. Standardized measures were used to determine participants' use of substances, history of psychiatric disorders and psychosocial stress, their sensation seeking and family history of substance use and mental health disorders. Multivariate analyses were used to detect patterns of variables associated with gender and the lifetime severity of AUD. Men had a longer history of severe AUD than women. Women had similar levels of alcohol dependence and medical and psychological sequelae as men, despite 6 fewer years of AUD. More women than men had a history of severe psychosocial stress, severe dependence on other substances and antecedent mental health problems, especially mood and anxiety disorders. There were differences in family history of alcohol-related problems approximating same-gender aggregation. The severity of a lifetime AUD was predicted by its earlier age at onset and the occurrence of other disorders, especially anxiety, among both men and women. The limitations in the generalizability of these findings due to sample idiosyncrasies are discussed.     

Biochemical and molecular characterisation of cubozoan protein toxins

Class Cubozoa includes several species of box jellyfish that are harmful to humans. The venoms of box jellyfish are stored and discharged by nematocysts and contain a variety of bioactive proteins that are cytolytic, cytotoxic, inflammatory or lethal. Although cubozoan venoms generally share similar biological activities, the diverse range and severity of effects caused by different species indicate that their venoms vary in protein composition, activity and potency. To date, few individual venom proteins have been thoroughly characterised, however, accumulating evidence suggests that cubozoan jellyfish produce at least one group of homologous bioactive proteins that are labile, basic, haemolytic and similar in molecular mass (42-46 kDa). The novel box jellyfish toxins are also potentially lethal and the cause of cutaneous pain, inflammation and necrosis, similar to that observed in envenomed humans. Secondary structure analysis and remote protein homology predictions suggest that the box jellyfish toxins may act as α-pore-forming toxins. However, more research is required to elucidate their structures and investigate their mechanism(s) of action. The biological, biochemical and molecular characteristics of cubozoan venoms and their bioactive protein components are reviewed, with particular focus on cubozoan cytolysins and the newly emerging family of box jellyfish toxins.     

Dose tolerability of chronically inhaled voriconazole solution in rodents

Invasive pulmonary aspergillosis (IPA) is a fungal disease of the lung associated with high mortality rates in immunosuppressed patients despite treatment. Targeted drug delivery of aqueous voriconazole solutions has been shown in previous studies to produce high tissue and plasma drug concentrations as well as improved survival in a murine model of IPA. In the present study, rats were exposed to 20 min nebulizations of normal saline (control group) or aerosolized aqueous solutions of voriconazole at 15.625 mg (low dose group) or 31.25 mg (high dose group). Peak voriconazole concentrations in rat lung tissue and plasma after 3 days of twice daily dosing in the high dose group were 0.85 ± 0.63 μg/g wet lung weight and 0.58 ± 0.30 μg/mL, with low dose group lung and plasma concentrations of 0.38 ± 0.01 μg/g wet lung weight and 0.09 ± 0.06 μg/mL, respectively. Trough plasma concentrations were low but demonstrated some drug accumulation over 21 days of inhaled voriconazole administered twice daily. Following multiple inhaled doses, statistically significant but clinically irrelevant abnormalities in laboratory values were observed. Histopathology also revealed an increase in the number of alveolar macrophages but without inflammation or ulceration of the airway, interstitial changes, or edema. Inhaled voriconazole was well tolerated in a rat model of drug inhalation.