A comparison of human immunodeficiency virus type-1 protease inhibition activities by the aqueous and methanol extracts of Chinese medicinal herbs

The aqueous and methanol extracts of thirty-one herbs traditionally used as anti-fever remedies in China were screened for their in vitro inhibition on human immunodeficiency virus type-1 protease (HIV-1 PR). The activity of recombinant HIV-1 protease was determined by sequence-specific cleavage at the Tyr-Pro bond of the fluorogenic substrate (Arg-Glu(EDANS)-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-Lys(DABCYL)- Arg) or by HPLC anaylsis of the cleavage products after incubation of the enzyme with a synthetic peptide substrate (Acetyl-Ser-Gln-Asn-Tyr-Pro-Val-Val-amide). Among the herbal extracts examined, the aqueous extracts of Prunella vulgaris and Scutellaria baicalensis and the methanol extracts of Woodwardia unigemmata, Paeonica suffruticosa and Spatholobus suberectus elicited significant inhibition (>90%) at a concentration of 200 microg/ml.     

A comparison of HIV-1 integrase inhibition by aqueous and methanol extracts of Chinese medicinal herbs

The aqueous and methanol extracts of twenty herbs traditionally used in Chinese medicine were screened for anti-HIV-1 integrase activity in a non-radioactive ELISA-based HIV-1 integrase assay. The screening was performed at an herb extract concentration of 50 microg/ml. It was found that most of the aqueous and methanol herb extracts could elicit strong inhibition of HIV-I integrase activity. The inhibition was most likely due to tannins or polyphenolics in the herb extracts. In most of the herb extracts, 40-80% of the anti-HIV-1 integrase activity could be removed after passing through a minicolumn of polyamide resin. After removal of polyphenolic compounds, the methanol extract of Paeonia suffruticosa still exerted potent inhibition of HIV-1 integrase (EC50 = 15 microg/ml) and the aqueous extract of Prunella vulgaris caused moderate inhibition (EC50 = 45 microg/ml). The results support the view that herbs represent a rich source of anti-HIV compounds.     

内蒙古产柽柳和多枝柽柳α-葡萄糖苷酶抑制活性

首次利用体外α-葡萄糖苷酶抑制模型以96微孔板法,对内蒙古产2种柽柳属植物不同溶剂提取物进行活性评价,并与阳性对照Acarbose比较,发现6种提取物均有较好的α-葡萄糖苷酶抑制作用,远远强于阳性对照Acarbose(IC50=1103.01μg·mL-1)的抑制活性。结果显示,同一植物不同溶剂提取物相比较,两者石油醚提取物α-葡萄糖苷酶抑制活性不及乙酸乙酯和正丁醇提取物;不同植物同一溶剂的提取物抑制活性也不同,6种提取物中,多枝柽柳的正丁醇和柽柳的乙酸乙酯提取物抑制活性最高(IC50=13.36和17.35μg·mL-1)。所有提取物对α-葡萄糖苷酶活性的抑制效果均很好,且多枝柽柳抑制活性整体上较柽柳好,具有良好的潜在开发价值。     

Antitumor and antiviral activity of Colombian medicinal plant extracts.

Extracts of nine species of plants traditionally used in Colombia for the treatment of a variety of diseases were tested in vitro for their potential antitumor (cytotoxicity) and antiherpetic activity. MTT (Tetrazolium blue) and Neutral Red colorimetric assays were used to evaluate the reduction of viability of cell cultures in presence and absence of the extracts. MTT was also used to evaluate the effects of the extracts on the lytic activity of herpes simplex virus type 2 (HSV-2). The 50% cytotoxic concentration (CC50) and the 50% inhibitory concentration of the viral effect (EC50) for each extract were calculated by linear regression analysis. Extracts from Annona muricata, A. cherimolia and Rollinia membranacea, known for their cytotoxicity were used as positive controls. Likewise, acyclovir and heparin were used as positive controls of antiherpetic activity. Methanolic extract from Annona sp. on HEp-2 cells presented a CC50 value at 72 hr of 49.6x10(3)mg/ml. Neither of the other extracts examined showed a significant cytotoxicity. The aqueous extract from Beta vulgaris, the ethanol extract from Callisia grasilis and the methanol extract Annona sp. showed some antiherpetic activity with acceptable therapeutic indexes (the ratio of CC50 to EC50). These species are good candidates for further activity-monitored fractionation to identify active principles.     

Anthelmintic efficacy of Achillea millifolium against gastrointestinal nematodes of sheep: in vitro and in vivo studies

Achillea millifolium Linn., commonly called 'Pehl-ghasa', is used by farmers in traditional animal health care as a vermifuge. The objective of this study was to evaluate the anthelmintic efficacy of crude aqueous extracts and crude ethanolic extracts of entire A. millifolium against the gastrointestinal nematodes of sheep. The worm motility inhibition assay was used for in vitro studies and faecal egg count reduction assay was used for in vivo studies. In vitro studies revealed significant anthelmintic effects of aqueous extracts and ethanolic extracts on live Haemonchus contortus worms (P < 0.05) as evident from their paralysis and/or death at 8 h post exposure. Aqueous extracts of A. millifolium resulted in a mean worm motility inhibition of 94.44%, while ethanolic extracts resulted in mean worm motility inhibition of 88.88%. The mean mortality index of aqueous extracts was 0.95 while for ethanolic extracts it was 0.9. The lethal concentration 50 was 0.05 mg ml(-1) for aqueous extracts and 0.11 mg ml(-1) for ethanolic extracts. The in vivo anthelmintic activity of aqueous and ethanolic extracts of A. millifolium demonstrated a maximum (88.40%) nematode egg count reduction in sheep treated with aqueous extracts at 2 g kg(-1) body weight on day 15 after treatment. Ethanolic extracts resulted in a maximum of 76.53% reduction in faecal egg counts on day 15 after treatment with 2 g kg(-1) body weight. Thus, the aqueous extracts exhibited greater anthelmintic activity under both in vitro and in vivo conditions, and could be due to the presence of water-soluble active principle/s in A. millifolium. It is concluded that the entire plant of A. millifolium possesses significant anthelmintic activity and could be a potential alternative for treating cases of helminth infections in ruminants.     

Chemical composition and vasodilatation induced by Cuphea carthagenensis preparations

The aerial parts of Cuphea carthagenensis (Jacq.) J.F. Macbride (Lythraceae) are traditionally employed in Brazil to treat cardiovascular diseases. The aim of this study was to compare preparations of C. carthagenensis aerial parts (aqueous and ethanol extracts, together with derived fractions) with regard to their total phenolic contents and in vitro vasodilating activity. The main flavonoids found in the extracts were isolated and identified as quercetin derivatives. The extracts and fractions showed similar HPLC profiles with the presence of quercetin-5-O-β-glucopyranoside, quercetin-3-O-α-arabinofuranoside and quercetin-3-sulfate in all of them, but marked differences in the contents of flavonoids, proanthocyanidins, tannis and total phenolics. Excepting the aqueous extract, all assayed preparations elicited vasodilatation on pre-contracted rat aortic rings in the range of pIC(50) 4.53±0.03 to 4.98±0.06. Polynomial regression analysis demonstrated the relationship between vasodilating activity and the contents of flavonoids (r(2)=0.5190), proanthocyanidins (r(2)=0.8016), tannins (r(2)=0.8041) and total phenolics (r(2)=0.6226), suggesting the participation of these compounds in the pharmacological effect and their potential use as chemical markers for the species.     

中国水仙生物技术研究进展

中国水仙是我国传统名花,其栽培中一直存在三个问题:品种单一、繁殖速度有限、病毒积累严重。生物技术的发展为解决中国水仙目前存在的问题提供了新的途径,将成为中国水仙遗传改良、种质资源创新的重要手段。该文从四个方面综述了近年来中国水仙生物技术的研究进展:(1)离体培养;(2)基因工程;(3)离体突变体筛选;(4)分子标记。     

黄连提取物对α-葡萄糖苷酶抑制作用研究

利用体外α-葡萄糖苷酶抑制模型对黄连不同部位提取物进行活性评价,并与阳性对照Acarbose比较,发现黄连不同部位均有一定的α-葡萄糖苷酶抑制活性.其中,黄连根茎乙酸乙酯提取物的抑制活性最高(IC_(50)=20.72 μg/mL),黄连种子石油醚部位(IC_(50)=40.86 μg/mL)和黄连叶石油醚部位(IC_(50)=62.85 μg/mL)的活性次之.3个部位的提取物活性均远大于阳性对照Acarbose(IC_(50)=1081,27 μg/mL).不同部位比较,根茎对α-葡萄糖苷酶抑制活性最好,这3种提取物抑制活性均比阳性对照高;同一部位不同提取物比较,石油醚和甲醇提取物α-葡萄糖苷酶抑制活性一般要高于乙酸乙酯提取物.     

冷蒿对三种禾本科植物种子萌发和幼苗生长的化感作用

研究了冷蒿茎叶水浸提液及冷蒿斑块土壤对羊草草原3种禾本科植物(羊草、克氏针茅和糙隐子草)种子萌发及幼苗生长的影响.结果表明:冷蒿茎叶水浸提液使受试植物种子的发芽指数降低,平均发芽时间延长.羊草、克氏针茅和糙隐子草幼苗苗高及克氏针茅幼苗根长均受冷蒿茎叶水浸提液抑制;浸提液浓度≥0.075g.ml-1时显著抑制羊草幼苗根长生长,≤0.05g.ml-1时则无显著影响;而茎叶水浸提液对糙隐子草幼苗根长有"低促高抑"的作用.冷蒿斑块土壤抑制受试植物幼苗生长;3种植物对冷蒿化感效应的敏感性依次为克氏针茅羊草糙隐子草,且幼苗根长的敏感性均大于苗高.     

The effect of erythrodiol-3-acetate on the expressions of matrix metalloproteinase-1 and type-1 procollagen caused by ultraviolet irradiated cultured primary old aged human skin fibroblasts

Methanol and aqueous extracts of Styrax japonica used traditionally for the treatments of skin elastic materials were screened in vitro for the matrix metalloproteinase (MMP)-1 inhibitor actions. The methylene chloride soluble fraction of methanol extract from the stems of S. japonica showed significant MMP-1 inhibition in primary old aged human skin fibroblasts caused by ultraviolet (UV) irradiation. Main triterpenoids were isolated by repeated column chromatography. Among them, the triterpenoid erythrodiol-3-acetate reduced the expression of MMP-1 and induced the expression of type-1 procollagen at the protein levels in a dose-dependent manner caused by UV irradiated cultured old aged human skin fibroblasts. Taken together, our results suggest that erythrodiol-3-acetate plays an important role in the skin aging process caused by UV irradiation.     

Evaluation of anthelmintic activity of Iris hookeriana against gastrointestinal nematodes of sheep

The objective of this study was to evaluate the anthelmintic efficacy of Iris hookeriana Linn. rhizome against gastrointestinal nematodes of sheep. A worm motility inhibition assay was used for in vitro study and a faecal egg count reduction assay was used for an in vivo study. The in vitro study revealed anthelmintic effects of crude aqueous extracts and crude ethanolic extracts on live Trichuris ovis worms (P < or = 0.05) as evident from their paralysis and/or death at 8 h after exposure. The aqueous extracts of I. hookeriana resulted in a mean worm motility inhibition of 54.0%, while ethanolic extracts resulted in a mean worm motility inhibition of 84.6%. The mean mortality index of aqueous extracts was 0.55, while for ethanolic extracts it was 0.85. The lethal concentration 50 for aqueous extracts was 0.45 mg ml- 1 and for ethanolic extracts it was 0.15 mg ml- 1. The in vivo anthelmintic activity of aqueous and ethanolic extracts of I. hookeriana in sheep naturally infected with mixed species of gastrointestinal nematodes demonstrated a maximum (45.62%) egg count reduction in sheep treated with ethanolic extracts at 2 g kg- 1 body weight on day 10 after treatment, closely followed by ethanolic extracts at 1 g kg- 1 body weight on day 10 after treatment (43.54% egg count reduction). The aqueous extracts resulted in a maximum of 31.53% reduction in faecal egg counts on day 10 after treatment with 1 g kg- 1 body weight. Thus ethanolic extracts exhibited greater anthelmintic activity under both in vitro and in vivo conditions; this could be due to the presence of alcohol-soluble active ingredients in I. hookeriana. From the present study it can be suggested that I. hookeriana rhizome exhibited significant anthelmintic activity against gastrointestinal nematodes of sheep and has the potential to contribute to the control of gastrointestinal nematode parasites of small ruminants.     

七种中草药提取物抗肿瘤活性部位的筛选研究初报

选取叶下珠、珠子草、千里光、鸦胆子、使君子、冬青和猫爪藤等7种中草药进行提取和初步分离,筛选出有抗肿瘤效果的活性部位,并对其进行初步分析。采用MTT法,以7种中草药醇提物的不同分离部位分别对人肝癌、胃癌、卵巢癌等肿瘤细胞株进行体外增殖抑制作用研究,并以人正常肝细胞株为模型对照跟踪筛选活性部位。结果表明,从7种中草药醇提物中,均获得对肿瘤细胞株具有体外增殖抑制作用的化学分离部位,其中叶下珠和珠子草的乙酸乙酯层和正丁醇层的活性最显著,千里光的乙酸乙酯层、鸦胆子的正丁醇层、使君子和冬青的氯仿层活性次之,猫爪藤氯仿层和冬青的乙酸乙酯层活性较差,其他部位无活性。     

In vitro effects of four tropical plants on the activity and development of the parasitic nematode, Trichostrongylus colubriformis

The in vitro effects of extracts of four tropical plants (Zanthoxylum zanthoxyloides, Newbouldia laevis, Morinda lucida and Carica papaya) on the egg, infective larvae and adult worms of Trichostrongylus colubriformis were screened for potential anthelmintic properties. Significant effects were observed with the four plants on T. colubriformis but they differed depending on the stage of the parasite. Extracts of each plant induced a dose-dependent inhibition of egg hatching. Using a larval inhibition migration test, the effects on the infective larvae were also detected with the four plant extracts. In contrast, for adult worms, the effects were statistically significant only for N. laevis and C. papaya. No significant activity was shown for M. lucida and Z. zanthoxyloides. These in vitro results suggest the presence of some anthelmintic properties associated with these four plants, which are traditionally used by small farmers in western Africa. These effects need to be studied under in vivo conditions.     

Antibacterial activity of plant extracts on phytopathogenic Xanthomonas campestris pathovars

Aqueous extracts from leaves of 30 higher plants, collected from different localities, were screened in vitro for antibacterial activity against different pathovars of the phytopathogenic bacterium, Xanthomonas campestris. Eight plant species showed antibacterial activity, based on the zone of inhibition in a diffusion assay. Significant antibacterial activity was observed in the aqueous extracts of Prosopis juliflora , Oxalis corniculata and Lawsonia inermis. The susceptibility of different pathovars of X. campestris to these plant extracts varied. The antibacterial activity of extracts of a few plants was comparable with that of the synthetic antibiotics, bacterimycin and streptocycline. The study indicates the potential of these plant extracts in the management of diseases caused by X. campestris in several important crop plants.     

Screening of medicinal plant extracts for antioxidant activity

The methanol extracts of nine medicinal plants traditionally used in Chinese medicine were screened for antioxidant activity versus resveratrol, which has been shown to protect cells from oxidative damage [Toxicol. Lett. 102 (1998) 5]. Most of the plant extracts used in this study inhibited the H(2)O(2)-induced apoptosis of Chinese hamster lung fibroblast (V79-4) cells. The extracts of Areca catechu var. dulcissima, Paeonia suffruticosa, Alpinia officinarum, Glycyrrhiza uralensis and Cinnamomun cassia strongly enhanced viability against H(2)O(2)-induced oxidative damage in V79-4 cells. Relatively high levels of 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity were detected in extracts of Areca catechu var. dulcissima, Paeonia suffruticosa and Cinnamomun cassia (IC(50) < 6.0 microg/ml). The activities of superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPX) were dose-dependently enhanced in V79-4 cells treated with most of the plant extracts. The extracts of Areca catechu var. dulcissima showed higher antioxidant activity than resveratrol in all experiments. These results suggest that the plant extracts prevent oxidative damage in normal cells probably because of their antioxidant characteristics.     

Important Roles of Minor Peroxide Components in the Autoxidation of Methyl Linoleate

Superoxide dismutase (SOD)-like compounds and activators of SOD were screened for in the extracts of fruits, vegetables, and mushrooms by measuring their effects on pyrogallol autoxidation, which is catalyzed by superoxide anion. SOD-like activity was high in aqueous extract of nameko, garlic, broccoli, and oriental lettuce. Ethanolic extracts of onion and watermelon could enhance human SOD activity more than 40%.     

Phytopesticidal and repellent efficacy of Litsea salicifolia (Lauraceae) against Aedes aegypti and Culex quinquefasciatus

Litsea salicifolia is one of the many plants used as phytopesticide, traditionally by various tribes of Assam. Of the five extracts of L. salicifolia tested for the bioactivity against Aedes aegypti and Culex quinquefasciatus, the aqueous extract was more effective compared to other extracts exhibiting bioactivity at 72 ppm against A. aegypti. The hexane extract (2000 ppm) exhibited 70% repellent activity for 3 hr against A. aegypti and 46% activity for 3 hr against C. quinquefasciatus. This is the first report on the insecticidal properties of L. salicifolia which can be further developed as an eco-friendly biopesticides of the future.     

Antibacterial activity of aerial parts as well as in vitro raised calli of the medicinal plant Saraca asoca (Roxb.) de Wilde

Leaves, stem, and flowers of Saraca asoca, an endangered medicinal plant in India, and young explants cultivated on Murashige & Skoog's medium containing 6-benzylaminopurine were analyzed for antibacterial potential. Alcoholic and aqueous extracts from parent explants and their in vitro raised calli were tested by an agar well diffusion method. Minimal inhibitory concentrations (MICs) of the extracts were determined by broth microdilution method. Aqueous extracts showed antibacterial activity against limited bacterial species, whereas alcoholic extracts were active against a wider range of bacteria. Although the alcoholic extracts of all the explants and calli showed antibacterial activity, the extracts derived from flowers and their calli showed better results. Extracts derived from calli showed comparable results to the extracts from explants. Overall, the MICs of the extracts ranged from 0.039 to 1.25 mg/mL. MICs against gram-positive bacteria ranged from 0.078 to 1.25 mg/mL, whereas they ranged between 0.039 and 0.625 mg/mL against gram-negative bacteria. A MIC distribution plot showed that gram-negative bacteria were more susceptible to the extracts than gram-positive bacteria. It is concluded that extracts of S. asoca contain antibacterial agent, and as the calli gave good results, in vitro cultivation of the explants may be used to obtain antibacterial compounds. This is the first report on antibacterial activity of S. asoca, especially through in vitro raised calli.     

无叶假木贼和盐爪爪提取物的抗菌活性

无叶假木贼和盐爪爪地上部分乙醇提取物、不同溶剂萃取部分对供试病原细菌和真菌均表现出较好的抑制作用,其乙酸乙酯萃取部分和正丁醇萃取部分的抗菌活性明显强于石油醚萃取部分和水部分。结果表明,无叶假木贼中抗菌活性成分主要为极性中等的化合物,且很可能是具弱碱性、易与酸成盐的生物碱类。盐爪爪中抗菌活性成分同样为极性中等的化合物。