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Bioactive diterpenes and sesquiterpenes from the rhizomes of Wild ginger (Siphonochilus aethiopicus (Schweinf) B.L Burtt)

机译:野生姜根茎的生物活性二萜和倍半萜(Siphonochilus aethiopicus(Schweinf)B.L Burtt)

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摘要

Wild ginger (Siphonochilus aethiopicus (Schweinf) B.L Burtt) is used in traditional medicines in the West and South of Africa. In the present study, the crude hexane extract of wild ginger was evaluated for in vitro bioactivity. The components isolated from the plant for the first time are: epi-curzerenone, furanodienone (sesquiterpenes), 8(17),12E-labdadiene-15,16-dial, 15-hydroxy-8(17),12E-labdadiene-16-al and 16-oxo-8(17),12E-labdadiene-15-oic acid (labdanes). Cytotoxicity determinations using five cell lines: SH-SY5Y (human, Caucasian, bone marrow, neuroblastoma), Jurkat (human, peripheral blood, leukaemia T cell), L929 (mouse, CH3/connective tissue, areolar and adipose tumour cells), Hep G2 (human, Caucasian, hepatocellular carcinoma) and Hs 27 (normal, human, foreskin cells) were carried out. Anti-trypanosomal activity against Trypanosoma brucei brucei (S427) blood stream forms and anti-bacterial activity against Mycobacterium aurum (CIP .104482) were also investigated. Activity against M. aurum was moderate and at 100μg/ml, the crude extract together with the labdanes showed specific cytotoxicity, indicating anti-cancer potency. Anti-trypanosomal activity was observed in the crude extract which increased with the pure components: 8(17),12E-labdadiene-15,16-dial (MIC = 5.3 μM) and the sesquiterpenoids (MIC = 6.9 μM) as compared to suramin activity (MIC = 10 μM). This anti-trypanosomal activity which is being reported for the first time indicates possible usage against sleeping sickness and nagana in cattle.
机译:野生姜(Siphonochilus aethiopicus(Schweinf)B.L Burtt)在非洲的西部和南部被用作传统药物。在本研究中,野姜的粗己烷提取物的体外生物活性进行了评估。首次从植物中分离出的成分是:表姜油酮,呋喃二烯酮(倍半萜),8(17),12E-拉巴二烯-15、16-拨号,15-羟基-8(17),12E-拉巴二烯-16 -al和16-oxo-8(17),12E-labdadiene-15-oic acid(labdanes)。使用五种细胞系进行细胞毒性测定:SH-SY5Y(人,高加索人,骨髓,神经母细胞瘤),Jurkat(人,外周血,白血病T细胞),L929(小鼠,CH3 /结缔组织,乳晕和脂肪肿瘤细胞),Hep进行了G2(人,白种人,肝细胞癌)和Hs 27(正常,人,包皮细胞)。还研究了对布鲁氏锥虫(S427)血流形式的抗锥虫活性和对金黄色分枝杆菌(CIP .104482)的抗菌活性。对金黄色葡萄球菌的活性中等,在100μg/ ml时,粗提物与拉丹脂一起显示出特定的细胞毒性,表明抗癌效力。与苏拉明相比,在粗提物中观察到的抗锥虫活性随以下纯组分的增加而增加:8(17),12E-labdadiene-15,16-dial(MIC = 5.3μM)和倍半萜类化合物(MIC = 6.9μM)活性(MIC = 10μM)。首次报道的这种抗锥虫活性表明可能在牛中用于抵抗昏睡病和长臂猿。

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