Background

R. natalensis.Bernh ex C.Krauss (Anacardiaceae) is used by Traditional Health Practitioners (THPs) in Same district, north eastern Tanzania, for treatment of cancer and other diseases. The current study was done to determine its cytotoxic activity.

Methodology

Dried root powder was extracted by cold maceration with a 1:1 mixture of methanol and dichloromethane. Sequential VLC fractions (Petroleum ether, ethyl acetate, and methanol) of the extract were made and tested for toxicity against brine shrimp (Artemia salina) larvae. The ethyl acetate fraction, which exhibited the highest toxicity against brine shrimp larvae, was used for bioassay-guided isolation and to test for cytotoxic activity against HeLa cervical cancer cells and antioxidant activity.

Results

The ethyl acetate extract was the most toxic against the brine shrimp larvae with LC₅₀ 7.2 μg/mL at (95 % CI of 4.993/10.033), while the methanol fraction gave an LC₅₀ 346.8 μg/mL. The ethyl acetate extracts exhibited antioxidant activity in both the DPPH and FRAP with EC₅₀ = 83.05 ± 0.06 μg/mL and (58.75 ± 0.091 μmol Fe²⁺ /g dry weight respectively. It also revealed cytotoxic activity against HeLa cervical cancer cells with IC₅₀ of 17.2 ± 3.4 μg/mL. A new compound, 3-((Z)-heptadec-14-enyl) benzene -1-ol, isolated from the ethyl acetate extract exhibited a weak cytotoxic activity of 35.24 ± 3.5 μg/mL on HeLa cells. Cell cycle analysis showed that the ethyl acetate extract inhibited mitosis and induced apoptosis as evidenced by activation of caspase 3 and membrane phosphatidylserine translocation.

Conclusion

The present results provide initial evidence that the root extract of R.natalensis contains compounds with both cytotoxic and antioxidant activity. Further studies are needed to determine activity on other cancer cell lines and to further elucidate the mechanism of cytotoxic activity.

中文翻译：

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一个新的细胞毒性化合物的分离，3 - （（Z） -十七碳-14-烯基）苯-从-1-醇漆树纳塔尔根提取物

背景

坦桑尼亚东北部同一地区的传统卫生从业者（THPs）将纳塔尔伯纳河杆菌（Anacardiaceae）用作原发性念珠菌（R. natalensis），用于治疗癌症和其他疾病。进行了当前研究以确定其细胞毒性活性。

方法

用甲醇和二氯甲烷的1：1混合物进行冷浸法提取干燥的根粉。制备提取物的顺序VLC馏分（石油醚，乙酸乙酯和甲醇），并测试其对盐水虾（Artemia salina）幼虫的毒性。对盐水虾幼虫具有最高毒性的乙酸乙酯级分被用于生物测定指导的分离，并测试其对HeLa宫颈癌细胞的细胞毒性活性和抗氧化活性。

结果

乙酸乙酯萃取物对盐水虾幼虫的毒性最高，LC值为₅₀ 7.2μg/ mL（95％CI为4.993 / 10.033），而甲醇馏分的LC ₅₀值为₅₀ 346.8μg/ mL。乙酸乙酯提取物在DPPH和FRAP中均表现出抗氧化活性，EC ₅₀ = 83.05±0.06μg/ mL和（58.75±0.091μmolFe ²⁺ / g干重），并且还显示了对带有IC的HeLa宫颈癌细胞的细胞毒活性。₅₀ of 17.2±3.4μg/ mL。一种新化合物3-（（Z从乙酸乙酯提取物中分离得到的）-十七烷-14-烯基）苯-1-醇对HeLa细胞的细胞毒性较弱，为35.24±3.5μg/ mL。细胞周期分析表明，乙酸乙酯提取物抑制有丝分裂并诱导凋亡，这由caspase 3的激活和膜磷脂酰丝氨酸的转运所证实。

结论

目前的结果提供了初步的证据，即罗汉果的根提取物含有具有细胞毒性和抗氧化活性的化合物。需要进一步的研究来确定对其他癌细胞系的活性并进一步阐明细胞毒性活性的机制。