164种中药乙醇提取物抗真菌作用研究

目的：体外观察164种中药95％乙醇提取物对白色含珠菌、啤酒酵母和威克海姆原藻3种真菌的作用，并对其中抑菌效果明显的中药中的主要成分进行抗真菌药敏试验。方法：半固体药基混合法，微量稀释法。结果：22种中药乙醇提取物对1种或几种真菌显示较强的抑制作用，所试验的单体化合物对3种真菌无显著抑制作用。结论：首次对中药95％乙醇提取物应用半固体药基混合法进行抗真菌活性筛选，土槿皮、牡丹皮95％乙醇粗提物对3种真菌均有较强的抑制作用。     

Antimicrobial properties of heartwood,bark/sapwood and leaves of Juniperus species

Hexane and methanol extracts of heartwood, bark/sapwood and leaves of twelve taxa of Juniperus from the United States were assayed for antifungal and antibacterial activities. The hexane extract of the heartwood of several junipers appeared comparable in antibacterial activity to streptomycin. Antibacterial activity of the hexane extracts from the bark/sapwood of J. monosperma and J. californica were comparable to streptomycin. No appreciable antibacterial activities were found in the leaf extracts from any species examined. No antifungal activities comparable to amphotericin B were found in either hexane or methanol extracts of the heartwood nor from the bark/sapwood. Antifungal activity against Cryptococcus neoformans comparable to amphotericin B was found in the hexane extract of the leaves of J. occidentalis var. australis. The methanol extracts from the leaves of J. osteosperma and J. californica had antifungal activities comparable to amphotericin B against Trichophyton mentagrophytes.     

几种人参属中药提取物的制备及体外抗卵巢癌活性比较

目的:从人参、西洋参、竹节参、三七这4个人参属中药中提取成分,对其抗卵巢癌活性进行筛选、比较。方法:人参、西洋参、竹节参和三七分别用水和乙醇热回流提取制备相应的水提物和醇提物;上述药材70%乙醇水提取物经大孔树脂柱色谱分别制备得到总皂苷和相应的原人参二醇型皂苷和原人参三醇型皂苷部位。用噻唑蓝(MTT)法对这些提取物和部位在卵巢癌HEY细胞进行活性筛选,并用碘化丙啶(PI)染色检测提取物对细胞周期分布的影响,进一步用免疫印迹法(Western blot)检测了其对细胞周期蛋白表达的影响。划痕实验检测了提取物对细胞迁移能力的影响。结果:各提取物都表现出不同程度地抑制卵巢癌HEY细胞增殖活性,其中西洋原人参二醇型皂苷(PDSPQ)、竹节参总皂苷(TSPJ)、人参醇提物(EEPG)、人参总皂苷(TSPG)、人参原人参二醇型皂苷(PDSPG)对HEY细胞的增殖抑制比较明显,抑制率分别为45.59%,45.78%,50.48%,46.98%,64.36%,PDSPQ,TSPG,PDSPG可以不同程度的下调周期蛋白依赖性激酶(CDK)4,CDK6,细胞周期蛋白D1(cyclin D1)的表达,但对细胞迁移能力没有明显影响。结论:含有原人参二醇型皂苷的组分的抗卵巢癌HEY细胞活性比其他部位更明显,其机制可能与下调细胞周期相关蛋白CDK4,CDK6,cyclin D1的表达有关。     

Evaluation of antifungal activity of extracts of two Cameroonian Rutaceae: Zanthoxylum leprieurii Guill. et Perr. and Zanthoxylum xanthoxyloides Waterm.

Aqueous-ethanol 90% extracts of leaves, roots and stem barks of Zanthoxylum leprieurii and Zanthoxylum xanthoxyloides were examined for their antifungal properties against nine fungi by dilution methods on a solid medium and in a liquid medium. Our results indicate that these extracts, to varying extents, inhibit the in vitro growth of Candida albicans, Cryptococcus neoformans and seven filamentous fungi tested. Only the extracts obtained from the roots and stem barks of Z. xanthoxyloides showed antifungal activity on the germs studied, with minimal inhibitory concentration varying, respectively, from 0.5 to 1 mg/ml for the roots and from 0.125 to 1 mg/ml for the stem barks.     

五倍子有效部位抗病原微生物活性

目的:探讨五倍子抗细菌和抗白假丝酵母真菌的有效活性部位。方法:采用琼脂平板二倍稀释法测定了五倍子醇提物的石油醚、三氯甲烷、乙酸乙酯、正丁醇、乙醇和水6个有效部位对金黄色葡萄球菌、链球菌、大肠埃希菌等5个种属细菌和白假丝酵母真菌的最低抑菌浓度(MIC)。用单因素方差分析法、独立样本t检验比较分析不同活性部位对受试菌株抑菌活性的强弱。结果:五倍子石油醚、三氯甲烷和乙醇有效部位均无抗细菌和真菌活性,水部位仅对金黄色葡萄球菌有一定抗菌活性,MIC为733.69 g·L-1,正丁醇部位仅对5种细菌有较强的抗菌活性,MIC为2.06~32.96 g·L-1,而乙酸乙酯部位对受试细菌和白假丝酵母真菌均有强的抗菌活性,MIC分别为2.88~23.07 g·L-1和0.36~27.28 g·L-1。统计分析表明,乙酸乙酯和正丁醇部位对革兰阳性菌的抑菌活性强于对革兰阴性菌的抑菌活性(P<0.01,P<0.05),两者对同种属细菌的抑菌活性强弱相当,对耐药株和敏感株具有相似的抗菌活性。虽五倍子乙酸乙酯部位对白假丝酵母真菌临床分离株的MIC(95.15±96.34)mg·L-1明显高于克霉唑(8.00±8.92)mg·L-1(P<0.01),但克霉唑对临床分离株的耐药率为14.29%(2/14),而乙酸乙酯部位对所有临床分离株均有相似的抗菌活性(MIC为0.36~0.72 g·L-1)。结论:五倍子抗细菌和真菌的活性部位为乙酸乙酯部位。     

In vitro cytotoxic, antileishmanial and antifungal activities of ethnopharmacologically selected Gabonese plants

Seventy-seven crude extracts from leaves and stem barks of 15 Gabonese plants used in traditional medicine were evaluated for their cytotoxic, antileishmanial and antifungal activities. Most of the extracts exhibited cytotoxic activities toward human monocytes, and most particularly the hydromethanolic 50% (v/v) fraction of Ganophyllum giganteum leaves (IC(50)=1.3 microg/ml) as well as the methanolic extracts of Polyalthia suaveolens, Dioscorea preussii, Augouardia letestui leaves and Cola lizae stem barks (IC(50)<5 microg/ml). The methanolic extract of Polyalthia suaveolens displayed a strong antiproliferative activity against the promastigote form of Leishmania infantum parasites and presented a good antifungal activity on all the tested strains (IC(50)<1mg/ml). This extract was divided into six fractions: fraction F6 demonstrated a cytotoxic activity stronger than those of the crude extract (IC(50)=0.6 microg/ml), fractions F4 and F5 were devoid of cytotoxicity (IC(50)>100 microg/ml) and displayed interesting antileishmanial activity against the intracellular amastigote form of the parasite (IC(50)=5.6 and 12.4 microg/ml), respectively. However, the antifungal activity observed for the crude extract could not be recovered in the corresponding fractions.     

Pharmacological studies on the crude drug ‘Hwang-Jin-Guey’ from Taiwan (1)

Three different crude drugs take the same name ‘Hwang-jin-guey’ on the Taiwan market, they are (1) Cudrania cochinchinensis var. gerontogea (Moraceae), (2) Ventilago leiocarpa (Rhamnaceae) and (3) Viscum multinerve (Loranthaceae). To clarify and compare the pharmacological actions of these folk medicines, the antiinflammatory and liver-protective effects of their aqueous and ethanol extracts were investigated. The results showed that the aqueous extracts of C. cochinchinensis (300 mg/kg), V. leiocarpa (300 mg/kg) and ethanol extract of C. cochinchinensis (100 mg/kg) displayed marked antiinflammatory activity compared to indomethacin. An ethanol extract of V. leiocarpa (300 mg/kg) exhibited a comparable inhibitory effect to indomethacin in the paw oedema induced by carrageenan. As to the liver-protective effect, the statistical analysis (ANOVA) indicated that the aqueous (100 mg/kg) and ethanol (300 mg/kg) extracts of C. cochinchinensis presented pronounced activities against CCI₄-induced acute liver damage. However, treatment with V. multinerve offered no protection against CCI₄-induced hepatotoxicity, whether aqueous or ethanol extracts. These phenomena were also confirmed by histological observation.     

The role of the lignan constituents in the effect of Schisandra chinensis fruit extract on penile erection

The effect of the ethanol extract and active components of the fruit of Schisandra chinensis was evaluated on rabbit penile corpus cavernosum (PCC). PCC, pre‐contracted with 10^?5 m phenylephrine (Phe), was treated with extracts of S. chinensis at five different compositions of ethanol and water (95%, 70%, 50%, 30% and ethanol/water [v/v]) and three fractions (0.1, 0.5, 1 and 2 mg/mL). The effect of the extracts and active lignans (schisandrol A and schisandrol B) from S. chinensis on sildenafil citrate pre‐incubated PCC was also evaluated. The PCC relaxation induced by the 95% ethanol extraction and the n‐hexane fraction was concentration‐dependent and the ethanol extract enhanced sildenafil citrate‐induced PCC relaxation. The active components of S. chinensis (schisandrol A and schisandrol B) significantly enhanced sildenafil citrate‐induced relaxation >2‐fold; schisandrol A had the highest relaxant effect on sildenafil citrate pre‐incubated PCC. The lignans, schisandrol A and schisandrol B, isolated from the fruits of S. chinensis enhanced sildenafil citrate‐induced relaxation and may have synergistic action in patients who do not completely respond to sildenafil. Copyright © 2011 John Wiley & Sons, Ltd.     

绵马贯众不同萃取部位的抑菌活性

目的:研究绵马贯众不同萃取部位的抑菌活性。方法:以70%乙醇冷浸72 h制备绵马贯众粗提物,液-液分离法制备石油醚、三氯甲烷、乙酸乙酯、正丁醇和水5个部位萃取物,用K-B纸片扩散法对大肠埃希菌、金黄色葡萄球菌、枯草杆菌、酵母菌、黄曲霉和黑根霉6种供试菌株的抑菌活性进行研究。结果:绵马贯众5个萃取部位均表现出一定的抑菌效果,且随着用药量的增加其抑菌活性总体上呈现出增强的趋势,其中以三氯甲烷萃取部位和乙酸乙酯萃取部位的抑菌活性较大,水萃取部位的抑菌活性最小。结论:不同部位对供试菌株的抑菌活性不同。     

Screening of Malian medicinal plants for antifungal, larvicidal, molluscicidal, antioxidant and radical scavenging activities

A total of 78 different extracts from 20 medicinal plants belonging to 14 plant families from Mali were tested for their antifungal, larvicidal, molluscicidal, antioxidant and radical scavenging activities. Dichloromethane, methanol, water and ethanol extracts were used. TLC autobiography for antifungal activity was run with Cladosporium cucumerinum and Candida albicans. Extracts were also tested on the larvae of the mosquitoes Aedes aegypti, Anopheles gambiae and Culex quinquefasciatus. Molluscicidal activities were established with the snails Biomphalaria glabrata, Biomphalaria pfeifferi and Bulinus truncatus. β‐Carotene and DPPH solutions sprayed on TLC plates were used for antioxidant and radical scavenging assays. Of the extracts investigated, 20% were antioxidant and radical scavengers, 19% fungicidal, 30% were larvicidal and 11% were molluscicidal. Three of the plant extracts, from Cussonia barteri (Araliaceae), Glinus oppositifolius (Aïzoaceae) and Lannea velutina (Anacardiaceae) gave positive responses in all four tests. Copyright © 2001 John Wiley & Sons, Ltd.     

5种中药乙醇提取物的体外抗氧化活性研究

目的: 研究马尾松等5种中药的乙醇提取物的体外抗氧化活性。 方法: 采用乙醇超声提取法获得各中药提取物,并以抗坏血酸(VitC)为阳性对照来考察其对超氧阴离子(O₂^-·)、羟自由基(·OH)、1,1-二苯基-2-三硝基苯肼自由基(DPPH·)的清除效果。 结果: 甘草、丹参、马尾松、当归、罗汉松对O₂^-·的抑制率分别为(浓度相当于原药材100 g·L^-1):15.86%,11.68%,11.31%,7.88%,5.94%;在清除DPPH·的实验中各中药的IC₅₀(g·L^-1)分别为:丹参1.6,马尾松1.87,罗汉松3.11,甘草13.91,当归22.32;而在清除·OH的实验中各中药的IC₅₀(g·L^-1)则为:丹参1.6,罗汉松2.02,马尾松2.1,甘草2.77,当归4.03;而三大体系阳性对照的IC₅₀分别为0.047,0.93,0.21 g·L^-1。 结论: 5种中药乙醇超声提取物均具有一定的抗氧化活性,其中丹参、马尾松效果较好;但与阳性对照Vit C相比仍有一定差距。     

Antifungal Compounds from the Rhizome and Roots of Ferula hermonis

The antifungal activity of hexane, dichloromethane, methanol and aqueous extracts from the rhizome and root of Ferula hermonis was assayed in vitro by the agar disk diffusion method against a panel of human opportunistic and pathogenic fungi. Among them, the hexane and dichloromethane extracts showed the highest activity particularly against the dermatophytes Microsporum gypseum and Tricophyton mentagrophytes as well as the yeast Candida lactis‐condensi. Activity‐guided fractionation of both extracts using an agar overlay bioautographic method led to the isolation of two antifungal compounds which were identified as the daucane aryl esters jaeschkeanadiol p‐hydroxybenzoate (ferutinin) and jaeschkeanadiol benzoate (teferidin). Determination of minimal inhibitory concentration (MIC) and minimal fungicidal concentration (MFC) values of both compounds evidenced a stronger antifungal activity for ferutinin than for teferidin. Particularly, T. mentagrophytes was the most sensitive strain with MIC and MFC values ranging from 8 to 256 µg/mL. Copyright © 2012 John Wiley & Sons, Ltd.     

地锦草乙醇提取物对白色念珠菌性阴道炎大鼠模型的治疗作用

目的:观察地锦草乙醇提取物对大鼠白色念珠菌性阴道炎模型的治疗效果及其相关机制.方法:在卵巢切除加乙烯雌酚联合氢化可的松注射的基础上予白色念珠菌感染法制备大鼠白色念珠菌性阴道炎模型.并给予地锦草乙醇提取物治疗,连续7d.治疗结束后,取阴道分泌物进行真菌培养;行阴道灌洗,ELISA法测定灌洗液中单核细胞趋化蛋白-1(MCP-1)、巨噬细胞炎性蛋白-2(MIP-2)水平;切取阴道组织行组织病理学观察.结果:与正常组比较,模型组大鼠阴道分泌物培养出的白色念珠菌落数显著增多(P ＜0.001),地锦草乙醇提取物治疗组大鼠阴道分泌物培养出的白色念珠菌落数显著低于模型组(P＜0.01);ELISA检测显示模型组大鼠阴道灌洗液中MCP-1及MIP-2水平显著升高;(P ＜0.001);地锦草提乙醇取物治疗组大鼠阴道灌洗液中MCP-1及MIP-2水平显著低于模型组(P＜0.01);阴道组织病变在光镜下观察发现,实验动物造模成功后,阴道充血、分泌物增多.给地锦草乙醇提取物治疗7d后,阴道局部充血病变显著减轻,分泌物显著减少.结论:地锦草可以通过抑制真菌的生长,减少有关趋化因子的产生,从而发挥了对霉菌性阴道炎的治疗作用.     

In vitro cytotoxic,antiprotozoal and antimicrobial activities of medicinal plants from Vanuatu

Sixty‐three extracts obtained from 18 plants traditionally used in the South Pacific archipelago Vanuatu for the treatment of infectious diseases were screened for antimicrobial and antiprotozoal activities. In addition, the extracts were subjected to a detailed analysis on cytotoxic effects toward a panel of human cancer cell lines, designed as a smaller version of the NCI60 screen. Intriguingly, 15 plant extracts exhibited strong cytotoxic effects specific for only one cancer cell line. Extracts of the leaves of Acalypha grandis Benth . significantly affected Plasmodium falciparum without showing obvious effects against the other protozoa tested. The leaves of Gyrocarpus americanus Jacq . displayed significant activity against Trypanosoma b. brucei and the leaves of Tabernaemontana pandacaqui Lam . I as well as the stems of Macropiper latifolium (L.f .) against Trypanosoma cruzi. In contrast none of the extracts showed relevant antibacterial or antifungal activity. Copyright © 2009 John Wiley & Sons, Ltd.     

Antiviral activity of panamanian plant extracts

Panamanian tropical forest plants are potential sources of useful medicinal compounds including some with antiviral activities. Extracts prepared from the leaves of seven plants (Alseis blackiana Hemsl., Aspidosperma megalocarpon Muell, Arg., Hybanthus prunifolius (Humb. & Bonpl.) G. K. Schulze, Ouratea lucens Engl., Piper cordulatum C. DC., Trichilia cipo C. DC. and Tetragastris panamensis Kuntze) were screened for antiviral activity using three separate assay methods. The more polar (aqueous and ethanol) extracts of all plants demonstrated antiviral and virucidal activities. Good activities were found in the Ouratea lucens and Trichilia cipo ethanol and aqueous extracts which were further characterized for antiviral activity and cytotoxic effects. These extracts had direct virucidal activity as well as intracellular antiviral activity against both DNA and RNA viruses. Antiviral activity was achieved with extract concentrations significantly lower than those necessary to produce cytotoxic effects. Additionally, extracts were less toxic to normal cells than to the tumour cells tested.     

Effects of extracts of Olax subscorpioides and Aspilia africana on bovine red blood cells

Isosaline and ethanol extracts of Olax subscorpioides and Aspilia africana were investigated for their antiinflammatory properties. Both extracts exhibited antiinflammatory activity by stabilizing bovine red blood cell membranes against heat and hypotonic induced lyses. The ethanol extracts showed a biphasic effect on membrane stabilization at all the concentrations tested. The activities of the extracts were comparable to that of the standard drug indomethacin. © 1997 John Wiley & Sons, Ltd.     

Phytosynergy in some Hypoxis species and pharmacological properties of a Hypoxis-based phytopharmaceutical formula

Ethnopharmacology relevance

Hypoxis species are used extensively in traditional medicine in southern Africa for several ailments including tuberculosis, chest infections, and nervous and urinary disorders. Several other claims have been made for extracts emanating from Hypoxis species and have led to the production of several commercial products used as immunostimulants mostly for people living with HIV/AIDS and cancer. This study was aimed at investigating the biological activity of four Hypoxis species and a commercial herbal product, ‘African potato extract’ (APE).

Materials and methods

Antibacterial, antifungal, cyclooxygenase (COX) and acetylcholineasterase (AChE) inhibitory activities of four Hypoxis species (H. acuminata, H. colchicifolia, H. hemerocallidea and H. rigidula) and a popular Hypoxis-based herbal preparation, APE were tested. The phytoconstituents of the mixture were also profiled using TLC methods. Several combinations of the Hypoxis species were prepared and their synergism, additive, autonomic and antagonism effects investigated. As a quality control measure, batch to batch comparison in the phytoconstituents and biological activity of APE was carried out.

Results

The results confirmed H. colchicifolia and H. hemerocallidea as the phytoconstituents of APE. The extracts showed a broad spectrum of activities against the bacterial and fungal strains used. Of particular interest were the activities exhibited by the APE and combinations of H. colchicifolia and H. hemerocallidea. The APE mixture exhibited good antibacterial activity (MIC values of 0.78 mg/ml each) in all the tested batches against the bacterial strains used. The water extracts of all four Hypoxis species, three batches of APE and the combination (water extracts) of H. colchicifolia and H. hemerocallidea exhibited high COX-1 and moderate COX-2 inhibitory activity except for H. acuminata which showed low activity against COX-2. All the extract, batches of APE and combinations showed low to moderate AChE inhibitory activity. These results provided some evidence of phytosynergy in some extracts of H. hemerocallidea and H. colchicifolia except for a few extracts which act as additive, autonomous and antagonistic when used to inhibit some bacterial and fungal strains. However, this was not the case for COX and AChE inhibition, as only acetone extracts acted in a synergistic way to reduce the activity of the enzyme.

Conclusion

Even though the results give an indication of a positive interaction between some extracts of H. hemerocallidea and H. colchicifolia, the study was carried out on 1:1 v/v combinations only. It is therefore important to carry out isobologram studies, which considers more than one ratio of the combinations.     

阳荷提取物体外抗菌作用研究

目的:研究姜科姜属植物阳荷根茎乙醇提取物的体外抗菌活性.方法:运用乙醇渗漉法提取得到阳荷总提取物,依次用石油醚、氯仿、乙酸乙酯、正丁醇萃取,得到不同极性部位;用滤纸片法对乙醇提取物及各萃取物进行体外抗菌活性测定,有抑菌作用的萃取物进一步用微量肉汤稀释法测定其最低抑菌浓度(MIC)和最低杀菌浓度(MBC).结果:阳荷根茎乙醇提取物、石油醚和氯仿萃取物具有抑制金黄色葡萄球菌等3种革兰阳性菌和大肠埃希菌等3种革兰阴性菌生长繁殖的活性,MIC值在312.5 ～1250 mg·L-1.总提取物对地衣芽孢杆菌、无乳链球菌和大肠埃希菌的MBC均为1250 mg· L-;石油醚和氯仿萃取物对6种测试菌株均有杀灭作用,MBC值在625～1250 mg·L-1.结论:阳荷根茎乙醇提取物及石油醚和氯仿萃取物能显著抑制金黄色葡萄球菌、地衣芽孢杆菌、无乳链球菌、大肠埃希菌、肺炎克雷伯菌和铜绿假单胞菌的生长繁殖,具有明显的灭活作用.     

Antimicrobial activity of Polygonum equisetiforme extracts and flavonoids

Methanol, hexane, aqueous and petroleum ether extracts of the whole plant Polygonum equisetiforme did not show any activity against ten bacterial and four fungal species. The butanol crude extract and all the pooled groups of this exhibited variable patterns of antimicrobial activity. Quercetin (a flavonol) has been isolated and identified as the major constituent. The antifungal and antibacterial activity of quercetin was compared with the antibacterial drugs gentamycin, streptomycin and ampicillin and the antifungal drug miconazole nitrate. The antifungal activity of quercetin was limited to Candida tropicalis and it had a narrow antibacterial spectrum of activity. However, its activities against Enterobacter aerogenes and Escherichia coli were low grade compared with ampicillin, stretomycin and gentamycin. Quercetin-3-O-rhamnoside, quercetin-3-O-glucuronide, quercetin-3-O-arabinoside and isorhamnetin were also isolated in very low yield. They have not been reported previously in this species.     

In vitro anti‐adhesive activity of green tea extract against pathogen adhesion

Camellia sinensis polysaccharide has been reported to possess anti‐adhesive activity against pathogens. The present study was designed to investigate whether hot water extracts obtained from green tea leaves might inhibit pathogen adhesion to human or mouse cell lines. Green tea extract‐4 (CSI‐4) with the maximum yield of 4% (w/v) is composed of a major proportion of carbohydrates containing 40% uronic acids, but lack of catechins. It showed strong inhibitory activities against hemagglutination mediated by pathogens Helicobacter pylori, Propionibacterium acnes and Staphylococcus aureus with the minimum inhibitory concentrations of 0.01‐0.5 mg/mL. CSI‐4 further demonstrated an inhibitory effect on the adhesion of these pathogens to host cell lines with the IC₅₀ values (50% inhibition of adhesion) of 0.14–2.3 mg/mL. It exhibited the highest activity against P. acnes, but no inhibitory effects were observed against Lactobacillus acidophilus, Bifidobacterium bifidum, Escherichia coli, or Staphylococcus epidermidis. Our results suggest that CSI‐4 may exert a selective anti‐adhesive effect against certain pathogenic bacteria with no adverse effects against beneficial or commensal bacteria. Copyright © 2008 John Wiley & Sons, Ltd.