Antimalarial activity of plumbagin in vitro and in animal models

BMC Complementary and Alternative Medicine

Kesara Na-Bangchang²  Juntra Karbwang¹  Vithoon Viyanant²  Wanna Chaijaroenkul²  Tullayakorn Plengsuriyakarn²  Wiriyaporn Sumsakul² 

[1] Department of Clinical Product Development, Nagasaki Institute of Tropical Medicine, Nagasaki, Japan;Chulabhorn International College of Medicine, Thammasat University (Rangsit Campus), Pathumtani 12121, Thailand

关键词: Plasmodium berghei;    Plasmodium falciparum;    Antimalarial;    Plumbagin;   

Others  :  1220346
DOI  :  10.1186/1472-6882-14-15

 received in 2013-08-22, accepted in 2014-01-08,  发布年份 2014

【 摘 要 】

Background

Plumbagin is the major active constituent in several plants including Plumbago indica Linn. (root). This compound has been shown to exhibit a wide spectrum of biological and pharmacological activities. The present study aimed to evaluate the in vitro and in vivo antimalarial activity of plumbagin including its acute and subacute toxicity in mice.

Methods

In vitro antimalarial activity of plumbagin against K1 and 3D7 Plasmodium falciparum clones were assessed using SYBR Green I based assay. In vivo antimalarial activity was investigated in Plasmodium berghei-infected mouse model (a 4-day suppressive test).

Results

Plumbagin exhibited promising antimalarial activity with in vitro IC₅₀ (concentration that inhibits parasite growth to 50%) against 3D7 chloroquine-sensitive P. falciparum and K1 chloroquine-resistant P. falciparum clones of 580 (270–640) and 370 (270–490) nM, respectively. Toxicity testing indicated relatively low toxicity at the dose levels up to 100 (single oral dose) and 25 (daily doses for 14 days) mg/kg body weight for acute and subacute toxicity, respectively. Chloroquine exhibited the most potent antimalarial activity in mice infected with P. berghei ANKA strain with respect to its activity on the reduction of parasitaemia on day 4 and the prolongation of survival time.

Conclusions

Plumbagin at the dose of 25 mg/kg body weight given for 4 days was safe and produced weak antimalarial activity. Chemical derivatization of the parent compound or preparation of modified formulation is required to improve its systemic bioavailability.

【 授权许可】

   
2014 Sumsakul et al.; licensee BioMed Central Ltd.

【 图 表 】

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