In vivo and in vitro antimalarial activity of bergenin

Liang,Jiao; Li,Yinghui; Liu,Xuewu; Huang,Yuxiao; Shen,Yan; Wang,Jun; Liu,Zhongxiang; Zhao,Ya

doi:10.3892/br.2013.207

In vivo and in vitro antimalarial activity of bergenin

Authors:
- Jiao Liang
- Yinghui Li
- Xuewu Liu
- Yuxiao Huang
- Yan Shen
- Jun Wang
- Zhongxiang Liu
- Ya Zhao
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Affiliations: Department of Microbiology and Parasitology, The Fourth Military Medical University, Xi'an, Shaanxi 710032, P.R. China
Published online on: November 25, 2013 https://doi.org/10.3892/br.2013.207
Pages: 260-264

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Abstract

Malaria is a potentially life-threatening protozoal parasitic disease transmitted by female Anopheles mosquitoes. Drug therapy is currently the most widely used method for the control and treatment of this disease. Several plants were found to contain substances possessing antimalarial properties. In this study, we investigated the antimalarial activity of bergenin, a sesquiterpene lactone compound derived from Rodgersia aesculifolia Batal. The results indicated that bergenin effectively inhibited Plasmodium falciparum growth in vitro (IC50, 14.1 µg̸ml, with ~100% inhibition at 50 µg/ml), without apparent cytotoxicity to erythrocytes or to mammalian HeLa and HepG2 cells. bergenin exhibited less cytotoxic activity and the selectivity index (SI) was 887 and 1,355 for HeLa and HepG2 cells, respectively. The administration of bergenin to Plasmodium berghei‑infected mice for 6 days significantly inhibited the growth of the parasites. Taken together, these findings provide evidence that bergenin may be a promising novel drug for antimalarial treatment.

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1	World Health Organization. World Malaria Report. 2011, http://www.who.int/malaria/world_malaria_report_2011/en/uri.
2	Ashley EA and White NJ: Artemisinin-based combinations. Curr Opin Infect Dis. 18:531–536. 2005. View Article : Google Scholar
3	World Health Organization. Guidelines for the treatment of malaria. http://www.who.int/malaria/docs/TreatmentGuidelines2006.pdfuri.
4	Phyo AP, Nkhoma S, Stepniewska K, et al: Emergence of artemisinin-resistant malaria on the western border of Thailand: a longitudinal study. Lancet. 379:1960–1966. 2012. View Article : Google Scholar : PubMed/NCBI
5	Noedl H, Se Y, Schaecher K, et al; Artemisinin Resistance in Cambodia 1 (ARC1) Study Consortium. Evidence of artemisinin-resistant malaria in western Cambodia. N Engl J Med. 359:2619–2620. 2008. View Article : Google Scholar : PubMed/NCBI
6	Dondorp AM, Nosten F, Yi P, et al: Artemisinin resistance in Plasmodium falciparum malaria. N Engl J Med. 361:455–467. 2009. View Article : Google Scholar
7	Willcox ML and Bodeker G: Traditional herbal medicines for malaria. BMJ. 329:1156–1159. 2004. View Article : Google Scholar : PubMed/NCBI
8	Saxena S, Pant N, Jain DC and Bhakuni RS: Antimalarial agents from plant sources. Curr Sci. 85:1314–1329. 2003.
9	Kaur K, Jain M, Kaur T and Jain R: Antimalarials from nature. Bioorg Med Chem. 17:3229–3256. 2009. View Article : Google Scholar : PubMed/NCBI
10	Raj MK, Duraipandiyan V, Agustin P and Ignacimuthu S: Antimicrobial activity of bergenin isolated from Peltophorum pterocarpum DC. flowers. Asian Pac J Trop Biomed. 2:S901–S904. 2012. View Article : Google Scholar
11	Nazir N, Koul S, Qurishi MA, Najar MH and Zargar MI: Evaluation of antioxidant and antimicrobial activities of bergenin and its derivatives obtained by chemoenzymatic synthesis. Eur J Med Chem. 46:2415–2420. 2011. View Article : Google Scholar : PubMed/NCBI
12	Da Silva SL, Oliveira VG, Yano T and Nunomura RCS: Antimicrobial activity of bergenin from Endopleura uchi(Huber) Cuatrec. Acta Amazonica. 39:187–192. 2009.
13	Piacente S, Pizza C, De Tommasi N and Mahmood N: Constituents of Ardisia japonica and their in vitro anti-HIV activity. J Nat Prod. 59:565–569. 1996.
14	Nunomura RCS, Oliveira VG, Da Silva SL and Nunomura SM: Characterization of bergenin in Endopleura uchi bark and its anti-inflammatory activity. J Brazil Chem Soc. 20:1060–1064. 2009.
15	Nazir N, Koul S, Qurishi MA, Taneja SC, Ahmad SF, Bani S and Qazi GN: Immunomodulatory effect of bergenin and norbergenin against adjuvant-induced arthritis - a flow cytometric study. J Ethnopharmacol. 112:401–405. 2007. View Article : Google Scholar : PubMed/NCBI
16	De Abreu HA, Aparecida Dos S, Lago I, Souza GP, Pilo-Veloso D, Duarte HA and de C Alcantara AF: Antioxidant activity of (+)-bergenin: a phytoconstituent isolated from the bark of Sacoglottis uchi Huber (Humireaceae). Org Biomol Chem. 6:2713–2718. 2008.
17	Lim HK, Kim HS, Choi HS, Oh S and Choi J: Hepatoprotective effects of bergenin, a major constituent of Mallotus japonicus, on carbon tetrachloride-intoxicated rats. J Ethnopharmacol. 72:469–474. 2000. View Article : Google Scholar : PubMed/NCBI
18	Takahashi H, Kosaka M, Watanabe Y, Nakade K and Fukuyama Y: Synthesis and neuroprotective activity of bergenin derivatives with antioxidant activity. Bioorg Med Chem. 11:1781–1788. 2003. View Article : Google Scholar : PubMed/NCBI
19	Goel RK, Maiti RN, Manickam M and Ray AB: Antiulcer activity of naturally occurring pyrano-coumarin and isocoumarins and their effect on prostanoid synthesis using human colonic mucosa. Indian J Exp Biol. 35:1080–1083. 1997.PubMed/NCBI
20	Trager W and Jensen JB: Human malaria parasites in continuous culture. Science. 193:673–675. 1976. View Article : Google Scholar : PubMed/NCBI
21	Arnot DE, Ronander E and Bengtsson DC: The progression of the intra-erythrocytic cell cycle of Plasmodium falciparum and the role of the centriolar plaques in asynchronous mitotic division during schizogony. Int J Parasitol. 41:71–80. 2011.PubMed/NCBI
22	Gamo FJ, Sanz LM, Vidal J, et al: Thousands of chemical starting points for antimalarial lead identification. Nature. 465:305–310. 2010. View Article : Google Scholar : PubMed/NCBI
23	Lazaro JE and Gay F: Plasmodium falciparum: in vitro cytotoxicity testing using MTT. J Biomol Screen. 3:49–53. 1998. View Article : Google Scholar
24	Saha S and Verma R: Inhibitory potential of traditional herbs on alpha-amylase activity. Pharm Biol. 50:326–331. 2012. View Article : Google Scholar : PubMed/NCBI
25	Mbatchi SF, Mbatchi B, Banzouzi JT, Bansimba T, Nsonde Ntandou GF, Ouamba JM, Berry A and Benoit-Vical F: In vitro antiplasmodial activity of 18 plants used in Congo Brazzaville traditional medicine. J Ethnopharmacol. 104:168–174. 2006. View Article : Google Scholar : PubMed/NCBI
26	Malebo HM, Tanja W, Cal M, Swaleh SA, Omolo MO, Hassanali A, Sequin U, Hamburger M, Brun R and Ndiege IO: Antiplasmodial, anti-trypanosomal, anti-leishmanial and cytotoxicity activity of selected Tanzanian medicinal plants. Tanzan J Health Res. 11:226–234. 2009.PubMed/NCBI
27	Newman DJ and Cragg GM: Natural products as sources of new drugs over the last 25 years. J Nat Prod. 70:461–477. 2007.PubMed/NCBI
28	Ginsburg H and Deharo E: A call for using natural compounds in the development of new antimalarial treatments - an introduction. Malar J. 10(Suppl 1): S12011. View Article : Google Scholar : PubMed/NCBI
29	Patel DK, Patel K, Kumar R, Gadewar M and Tahilyani V: Pharmacological and analytical aspects of bergenin: a concise report. Asian Pac J Trop Dis. 2:163–167. 2012. View Article : Google Scholar
30	Merisko-Liversidge EM and Liversidge GG: Drug nanoparticles: formulating poorly water-soluble compounds. Toxicol Pathol. 36:43–48. 2008. View Article : Google Scholar : PubMed/NCBI
31	Qin X, Yang Y, Fan TT, Gong T, Zhang XN and Huang Y: Preparation, characterization and in vivo evaluation of bergenin-phospholipid complex. Acta Pharmacol Sin. 31:127–136. 2010. View Article : Google Scholar : PubMed/NCBI
32	Upadhyay HC, Sisodia BS, Verma RK, Darokar MP and Srivastava SK: Antiplasmodial potential of extracts from two species of genus Blumea. Pharm Biol. 51:1326–1330. 2013. View Article : Google Scholar : PubMed/NCBI