β-榄香烯对体外培养恶性疟原虫生长抑制作用的实验研究
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摘要
目的:研究从中药莪术中分离得到的新型非细胞毒性抗肿瘤药物β-榄香烯的体外抗疟活性,。方法:采用恶性疟原虫3D7株(氯喹敏感株)和Dd2株(氯喹抗性株)进行测试,恶性疟原虫经过同步化处理后添加β-榄香烯,40 h后涂片镜检,观察其细胞形态变化;采用SYBR Green I染料法检测两种虫株对β-榄香烯和氯喹的半数抑制浓度(IC_(50))。结果:与空白对照组相比,添加10μg/mL的β-榄香烯能抑制恶性疟原虫的生长,40μg/mL的β-榄香烯可以完全抑制恶性疟原虫的生长;3D7虫株和Dd2虫株对β-榄香烯的IC_(50)值分别为(13.60±0.540)μg/mL和(12.59±0.54)μg/mL。结论:β-榄香烯具有显著的体外抗疟活性,值得进一步深入研究。
Objective: To study the antimalarial activity of β-elemene in vitro, a novel non-cytotoxic antitumor drug isolated from the Traditional Chinese Medicinal herb Rhizoma Zedoariae. Methods: Chloroquine(CQ)-sensitive(3 D7)and CQ-resistant(Dd2) strains of Plasmodium falciparum were tested using β-elemene and the fluorescence-based SYBR Green I assay was used to calculate the growth inhibition. Results: Compared with non-treated control, β-elemene can arrest the parasites growth at 10 μg/mL,and the parasites could be significantly inhibited at 40 μg/mL. The 50% inhibitory concentration(IC_(50)) values of β-elemene were(13.60±0.540) μg/mL for 3 D7 and(12.59±0.54) μg/mL for Dd2,respectively. Conclusion: These results demonstrated that β-elemene showed good antimalarial effect, and the β-elemene seemed to be of special interest for further antimalarial studies.
Objective: To study the antimalarial activity of β-elemene in vitro, a novel non-cytotoxic antitumor drug isolated from the Traditional Chinese Medicinal herb Rhizoma Zedoariae. Methods: Chloroquine(CQ)-sensitive(3 D7)and CQ-resistant(Dd2) strains of Plasmodium falciparum were tested using β-elemene and the fluorescence-based SYBR Green I assay was used to calculate the growth inhibition. Results: Compared with non-treated control, β-elemene can arrest the parasites growth at 10 μg/mL,and the parasites could be significantly inhibited at 40 μg/mL. The 50% inhibitory concentration(IC_(50)) values of β-elemene were(13.60±0.540) μg/mL for 3 D7 and(12.59±0.54) μg/mL for Dd2,respectively. Conclusion: These results demonstrated that β-elemene showed good antimalarial effect, and the β-elemene seemed to be of special interest for further antimalarial studies.
引文
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[2]Fidock DA,Rosenthal PJ,Croft SL,et al.Antimalarial drug discovery:efficacy models for compound screening[J].Nat Rev Drug Discov,2004,3(6):509-520.
[3]Eastman RT,Fidock DA.Artemisinin-based combination therapies:a vital tool in efforts to eliminate malaria[J].Nat Rev Microbiol,2009,7(12):864-874.
[4]Dondorp AM,Nosten F,Yi P,et al.Artemisinin resistance in Plasmodium falciparum malaria[J].N Engl J Med,2009,361(5):455-467.
[5]Htut ZW.Artemisinin resistance in Plasmodium falciparum malaria[J].N Engl J Med,2009,361(18):1807-1808;author reply 1808.
[6]Noedl H,Se Y,Schaecher K,et al.Evidence of artemisinin-resistant malaria in western Cambodia[J].N Engl JMed,2008,359(24):2619-2620.
[7]Lu F,Culleton R,Zhang M,et al.Emergence of Indigenous Artemisinin-Resistant Plasmodium falciparum in Africa[J].N Engl J Med,2017,376(10):991-3
[8]Kozlov S,Waters NC,Chavchich M.Leveraging cell cycle analysis in anticancer drug discovery to identify novel plasmodial drug targets[J].Infect Disord Drug Targets,2010,10(3):165-190.
[9]Reynolds JM,El Bissati K.Antimalarial activity of the anticancer and proteasome inhibitor bortezomib and its analog ZL3B[J].BMC Clin Pharmacol,2007,7:13.
[10]朱琳芳,王秋岩,吴慧丽,等.榄香烯抗肿瘤活性机理及其衍生物活性研究进展[J].杭州师范大学学报:自然科学版,2018,17(2):170-176
[11]Trager W,Jensen JB.Human malaria parasites in continuous culture[J].Science,1976,193(4254):673-675.
[12]周洪昌,张慧,李小余,等.恶性疟原虫二氢乳清酸脱氢酶抑制剂体外诱导恶性疟原虫耐药的实验研究[J].中国寄生虫学与寄生虫病杂志,2017,35(4):317-321.
[13]Chong CR,Chen X,Shi L,et al.A clinical drug library screen identifies astemizole as an antimalarial agent[J].Nat Chem Biol,2006,2(8):415-416.
[14]Li X,Wang G,Zhao J,et al.Antiproliferative effect of beta-elemene in chemoresistant ovarian carcinoma cells is mediated through arrest of the cell cycle at the G2-Mphase[J].Cell Mol Life Sci,2005,62(7-8):894-904.