Dyary H O, Arifah A K, Sukari M A, Sharma R S K
Faculty of Veterinary Medicine, Universiti Putra Malaysia, 43400 UPM Serdang, Selangor, Malaysia.
College of Veterinary Medicine, University of Sulaimani, Sulaymaniyah, Kurdistan Region, Iraq.
Trop Biomed. 2019 Mar 1;36(1):94-102.
Four carbazoles (girinimbine, mahanimbine, murrayafoline and murrayanine), isolated from Murraya koenigii, and one kavalactone (5,6-dehydrokawain) and one flavonoid (pinostrobin) isolated, from Alpinia mutica, were tested for their antitrypanosomal activity using in vitro cultured Trypanosoma evansi cell lines. The cytotoxic activities of these compounds were also investigated against mammalian Vero cells using the MTT (3-(4,5- Dimethylthiazol-2-yl) -2,5-diphenyltetrazolium bromide)-cell proliferation assay. Three carbazole compounds, namely mahanimbine, murrayafoline, and girinimbine, showed a potent antitrypanosomal activity, scoring a median inhibitory concentration (IC) of 3.13, 6.35 and 10.16 µg/ml, respectively. Girinimbine was the least toxic to Vero cells, and the mean cytotoxic concentration (CC) and the selectivity index (SI) of this compound were 745.58 ± 42.38 µg/ ml and 73.38, respectively. Girinimbine and the other carbazole compounds possess potential antitrypanosomal activity with comparably low toxicity against mammalian cells. Girinimbine, in particular, is a good candidate to be further investigated as a potential antitrypanosomal agent using in vivo models.
从九里香中分离出的四种咔唑类化合物（吉里宁宾、马汉宁宾、默里叶酸和默里宁），以及从少花山姜中分离出的一种卡瓦内酯（5,6-脱氢卡瓦因）和一种黄酮类化合物（松属素），利用体外培养的伊氏锥虫细胞系对其抗锥虫活性进行了测试。还使用MTT（3-(4,5-二甲基噻唑-2-基)-2,5-二苯基溴化四氮唑）细胞增殖试验研究了这些化合物对哺乳动物Vero细胞的细胞毒性活性。三种咔唑类化合物，即马汉宁宾、默里叶酸和吉里宁宾，显示出强大的抗锥虫活性，其半数抑制浓度（IC）分别为3.13、6.35和10.16µg/ml。吉里宁宾对Vero细胞的毒性最小，该化合物的平均细胞毒性浓度（CC）和选择性指数（SI）分别为745.58±42.38µg/ml和73.38。吉里宁宾和其他咔唑类化合物具有潜在的抗锥虫活性，对哺乳动物细胞的毒性相对较低。特别是吉里宁宾，作为一种潜在的抗锥虫药物，是使用体内模型进一步研究的良好候选物。
