Mushi Novatus F, Innocent Ester, Kidukuli Abdul W
Department of Natural Products Formulation and Development, Institute of Traditional Medicine, Muhimbili University of Health and Allied Sciences Dar es Salaam, Tanzania.
Department of Biological and Preclinical Studies, Institute of Traditional Medicine, Muhimbili University of Health and Allied Sciences Dar es Salaam, Tanzania.
J Intercult Ethnopharmacol. 2015 Jan-Mar;4(1):52-6. doi: 10.5455/jice.20141025103405. Epub 2014 Nov 28.
The aim of this study was to isolate the bioactive compounds from the roots of Combretum adenogonium and assess for its antibacterial and cytotoxic properties.
The extract was obtained using 20% aqueous ethanol and further subjected to fractionation with 1:1 n-butanol/water. Chromatographic analyses of the n-butanol fraction led to the isolation of compounds (1-3). The compounds (1-3) were assayed for antibacterial activities using two-fold microdilution methods and cytotoxicity using brine shrimps lethality assay.
Following spectroscopic analyses the compounds were established as 2,3,8-trihydroxy-4,6-dimethoxyphenanthrene (1a) and 2,3,8-trihydroxy-4,6-dimethoxy-9,10-dihydrophenanthrene (1β). Compound 2 was derived from 2,3,8-trihydroxy-4,6-dimethoxyphenanthrene condensation with methyl acetate while Compound 3 was derived from 2,3,8-trihydroxy-4,6-dimethoxy-9,10-dihydrophenanthrene condensation with methyl propionate. These compounds (1-3) were active against Pseudomonas aeruginosa with minimal inhibitory concentration-value of 0.16 mg/ml. The compounds (1-3) also exhibited significant toxicity with LC50 (95% confidence interval [CI]) of 12.11 (7.32-20.05) µg/ml compared to standard anticancer drug, cyclophosphamide which had LC50 (95% CI) value of 16.37 (12.01-22.31) µg/ml.
These compounds add for a novel structure that can be synthesized, further screened for in vitro and in vivo models and clinical trials in order to evaluate its potential for further development as new anticancer agent.
本研究旨在从腺叶风车子根中分离生物活性化合物，并评估其抗菌和细胞毒性特性。
用20%乙醇水溶液提取提取物，再用正丁醇/水1:1进行分馏。对正丁醇馏分进行色谱分析，分离出化合物（1 - 3）。采用两倍稀释法测定化合物（1 - 3）的抗菌活性，采用卤虫致死试验测定其细胞毒性。
经光谱分析，确定化合物为2,3,8 - 三羟基 - 4,6 - 二甲氧基菲（1a）和2,3,8 - 三羟基 - 4,6 - 二甲氧基 - 9,10 - 二氢菲（1β）。化合物2由2,3,8 - 三羟基 - 4,6 - 二甲氧基菲与乙酸甲酯缩合而成，化合物3由2,3,8 - 三羟基 - 4,6 - 二甲氧基 - 9,10 - 二氢菲与丙酸甲酯缩合而成。这些化合物（1 - 3）对铜绿假单胞菌有活性，最低抑菌浓度值为0.16 mg/ml。与标准抗癌药物环磷酰胺相比，化合物（1 - 3）也表现出显著毒性，其半数致死浓度（LC50，95%置信区间[CI]）为12.11（7.32 - 20.05）μg/ml，而环磷酰胺的LC50（95% CI）值为16.37（12.01 - 22.31）μg/ml。
这些化合物增加了一种可合成的新结构，可进一步在体外和体内模型以及临床试验中进行筛选，以评估其作为新型抗癌药物进一步开发的潜力。
