Klos M, van de Venter M, Milne P J, Traore H N, Meyer D, Oosthuizen V
Department of Pharmacy, Nelson Mandela Metropolitan University, PO Box 77000, Port Elizabeth 6031, South Africa.
J Ethnopharmacol. 2009 Jul 15;124(2):182-8. doi: 10.1016/j.jep.2009.04.043. Epub 2009 May 3.
Five South African medicinal plants, Bulbine alooides (L.) Willd. (Asphodelaceae), Crinummacowani Baker (Amaryllidaceae), Hypoxis sobolifera var. sobolifera (Jacq.) Nel (Hypoxidaceae), Leonotisleonurus (L.) R.Br. (Lamiaceae) and Tulbaghiaviolacea Harv (Liliaceae) used for the treatment of various ailments, including infectious diseases, were screened for activity against human immunodeficiency virus (HIV).
Aqueous and ethanol extracts were tested for inhibitory activity in HIV-1 infected CEM.NK(R)-CCR5 cells, and against HIV-1 reverse transcriptase (RT) and HIV-1 protease (PR).
In CEM.NK(R)-CCR5 cells, ethanol extracts of Leonotisleonurus inhibited HIV-1 significantly (33% reduction in HIV-1 p24, P<0.05). HIV-1 RT inhibition (> or =50%) was shown for extracts of Bulbine alooides (aqueous and ethanol), Hypoxis sobolifera (aqueous and ethanol) and Leonotisleonurus (aqueous), but inhibitory activity was lost upon dereplication for removal of non-specific tannins/polysaccharides. HIV-1 PR inhibition was observed for extracts of Hypoxis sobolifera (aqueous), Bulbine alooides (aqueous and ethanol) and Leonotisleonurus (ethanol). Only ethanolic extracts of Bulbine alooides and Leonotisleonurus retained HIV-1 PR inhibition after dereplication with IC50 of 94 microg/ml and 120 microg/ml, respectively.
The dereplicated ethanolic extracts of Leonotisleonurus and Bulbine alooides showed the greatest anti-HIV potential in this study through inhibition of HIV-1 PR.
对五种用于治疗包括传染病在内的各种疾病的南非药用植物进行筛选,检测其对人类免疫缺陷病毒(HIV)的活性。这五种植物分别是芦荟叶灯心草(百合科)、考氏海葱(石蒜科)、索氏小金梅草变种索氏小金梅(仙茅科)、益母草(唇形科)和紫花图尔巴吉花(百合科)。
检测水提取物和乙醇提取物对HIV-1感染的CEM.NK(R)-CCR5细胞的抑制活性,以及对HIV-1逆转录酶(RT)和HIV-1蛋白酶(PR)的抑制活性。
在CEM.NK(R)-CCR5细胞中,益母草的乙醇提取物对HIV-1有显著抑制作用(HIV-1 p24降低33%,P<0.05)。芦荟叶灯心草(水提取物和乙醇提取物)、索氏小金梅草(水提取物和乙醇提取物)和益母草(水提取物)的提取物显示出对HIV-1 RT的抑制作用(≥50%),但在去除非特异性单宁/多糖进行去重复处理后,抑制活性丧失。索氏小金梅草(水提取物)、芦荟叶灯心草(水提取物和乙醇提取物)和益母草(乙醇提取物)的提取物观察到对HIV-1 PR的抑制作用。去重复处理后,只有芦荟叶灯心草和益母草的乙醇提取物保留了对HIV-1 PR的抑制作用,IC50分别为94微克/毫升和120微克/毫升。
在本研究中,经去重复处理的益母草和芦荟叶灯心草乙醇提取物通过抑制HIV-1 PR显示出最大的抗HIV潜力。