Antimalarial activity of plumbagin in vitro and in animal models

Sumsakul, Wiriyaporn; Plengsuriyakarn, Tullayakorn; Chai่jaroenkul, Wanna; Viyanant, Vithoon; Karbwang, Juntra; Na‐Bangchang, Kesara

doi:10.1186/1472-6882-14-15

Cited by 58 publications

(33 citation statements)

References 20 publications

(19 reference statements)

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“…Antimalarial activity of plumbagin was reported by Sumsakul et al (2014) by investigating In vitro antimalarial activity of plumbagin against K1 and 3D7 Plasmodium falciparum and In vivo antimalarial activity in Plasmodium bergheiinfected mouse model (a 4-day suppressive test). Their study concluded that plumbagin exhibited efficient antimalarial activity in both In vivo and In vitro experiments and displayed a fairly 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.…”

Section: Antimalarial Activitymentioning

confidence: 99%

A Comprehensive Review on the Genus Plumbago With Focus on Plumbago Auriculata (Plumbaginaceae)

Singh¹,

Naidoo²,

Baijnath³

2017

Afr J Tradit Complement Altern Med

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Background: The genus Plumbago distributed in warm tropical regions throughout the world is the largest genus in Plumbaginaceae. Medicinal plants are characteristic to the genus Plumbago and are cultivated and utilized worldwide. Plumbago auriculata Lam. is common in South Africa and is often cultivated for its ornamental and medicinal uses throughout the world. Materials and Methods: A comprehensive review of the genus Plumbago with focus on Plumbago auriculata was carried out and information was gathered using scientific publications, conference proceedings, the internet and books. Articles based on the morphology, pharmacological and medicinal uses of Plumbago auriculata was analysed thoroughly. Results: Plumbago auriculata plant parts posses a wide range of phytochemicals with plumbagin being the marker compound showing various pharmacological activities. Different plant parts are claimed to be used for the treatment of human and animal ailments, however they do exhibit toxic properties and need to be administered with caution. Salt secreting glands and trichomes are characteristic of Plumbaginaceae. Conclusion: This study reveals new insights on the genus Plumbago and the potential use of species in the genus as medicinal plants. Plumbago auriculata possess the bioactive compound plumbagin and secondary metabolites, thus, it is of high medicinal importance. P. auriculata is a poorly nor favourite studied species in the genus Plumbago and further research needs to be carried out to explore specific details of the species.

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Section: Antimalarial Activitymentioning

confidence: 99%

A Comprehensive Review on the Genus Plumbago With Focus on Plumbago Auriculata (Plumbaginaceae)

Singh¹,

Naidoo²,

Baijnath³

2017

Afr J Tradit Complement Altern Med

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“…Among the Plumbago species, only P. europaea propagates in Iran . Plumbagin, 5‐hydroxy‐2‐methyl‐1, 4‐napthoquinone (C 11 H 8 O 3 ), is a natural product found in the roots of this genus, which has many therapeutic utilities because of anticancer, antimalarial, antimicrobial, antiatherosclerosis, antioxidant, leishmanicidal properties . P. europaea is an endangered species due to severe grazing of animals and harvesting for folk medicine proposes.…”

Section: Introductionmentioning

confidence: 99%

Potential of the genetically transformed root cultures of Plumbago europaea for biomass and plumbagin production

Beigmohamadi

Movafeghi

Jafari

et al. 2019

Biotechnology Progress

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Plumbago europaea L. is the main source of plumbagin which is a well‐known pharmacological active compound. In this investigation, genetically transformed roots of P. europaea were obtained by improving some factors affecting the efficiency of Agrobacterium rhizoigenes‐mediated transformation such as explant type, A. rhizoigenes strain, bacterial infection period, co‐cultivation period and acetosyringone concentration. The leaf, hypocotyl and stem explants from in vitro grown plantlets were infected with bacterial strains (A4, ATCC15834, MSU440 and A13). The highest transformation rate of 69.3% was achieved after 7–9 days by inoculating A. rhizogenes MSU440 strain onto the 3‐week‐old stem explants followed by a co‐cultivation period of 2 days on a medium containing 100 μM acetosyringone. To investigate the existence of the rolB gene, polymerase chain reaction was carried out using specific primers. Effects of growth media (MS, 1/2 MS, MS‐B5 and ½ MS‐B5), different sucrose concentrations and illumination on biomass production and plumbagin biosynthesis in P. europaea hairy root cultures were analyzed using stem explants after infection with MSU440 strain. ½ MS‐B5 liquid medium containing 30 g L−1 sucrose incubated in the dark resulted in the efficient biomass production of transformed hairy roots (12.5 g fresh weight, 1.8 g dry weight) with 3.2 mg g−1 DW plumbagin accumulation. This procedure provides a framework for large‐scale cultivation of hairy roots for plumbagin production. This is the first report describing the establishment of P. europaea hairy root culture with special emphasis on plumbagin production.

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“…Promising antimalarial activities of both plumbagin and the crude ethanolic extract of Plumbago indica Linn. (root) have been demonstrated in vitro and in vivo [3, 4]. In the in vitro model, the extract exhibited good to moderate antimalarial activity (class III antimalarial activity) with IC 50 (concentration producing 50 % growth inhibition) of 3 and 6.2 μg/mL, against K1 chloroquine-resistant and 3D7 chloroquine-sensitive P. falciparum clones, respectively [3].…”

Section: Introductionmentioning

confidence: 99%

“…The activity against P. falciparum enzyme succinate dehydrogenanse (SDH) including parasite growth has been shown to be inhibited to 50 % by plumbagin at inhibitory concentrations of 5 and 0.27 mM, respectively [6]. In the in vivo model, plumbagin at the dose of 25 mg/kg body weight given for 4 days however, exhibited only weak to antimalarial activity with regard to the inhibitory activity on the reduction of parasitemia and the prolongation of survival time [4]. …”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics, toxicity, and cytochrome P450 modulatory activity of plumbagin

Sumsakul

Plengsuriyakarn

Na‐Bangchang

2016

BMC Pharmacol Toxicol

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BackgroundThe antimalarial activity of plumbagin (5-hydroxy-2-methyl-1,4-naphthoquinone), a naturally occurring naphthoquinone widely distributed in the Plumbaginaceae family has previously been demonstrated in vitro (good activity) and in vivo (weak activity). The aim of the study was to investigate the pharmacokinetic profile following a single oral dosing to explain inconsistency of results of the in vitro and in vivo antimalarial activities. In addition, toxicity profiles and potential of modulation of cytochrome P450 enzymes (CYP1A2 and CYP3A11) were also investigated.MethodsThe pharmacokinetics and toxicity of plumbagin were investigated in rats. The propensity of plumbagin to modulate the mRNA expression and activities of the two inducible forms of hepatic drug metabolizing enzyme cytochrome P450 (CYP450), i.e., CYP1A2 and CYP3A11, was investigated using microsomes prepared from mouse livers.ResultsAcute and subacute toxicity tests indicate low toxicity of plumbagin with maximum tolerated doses of 150 (single oral dose) and 25 (daily doses for 28 days) mg/kg body weight, respectively. The pharmacokinetic profile of plumbagin following a single oral dose of 100 mg/kg body weight suggests that delayed absorption and short residence time (median values of time to maximal concentration and elimination half-life = 9.63 and 5.0 h, respectively) in plasma. Plumbagin did not modulate mRNA expression and activities of CYP1A2 and CYP3A11.ConclusionsPlumbagin was well tolerated following oral dose administration in rats. Pharmacokinetic property of this compound may be a limiting factor that explains the weak antimalarial activity of plumbagin observed in animal models. Potential metabolic interaction with co-administered drugs that are metabolized by CYP1A2 or CYP3A11 are unlikely.

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Antimalarial activity of plumbagin in vitro and in animal models

Cited by 58 publications

References 20 publications

A Comprehensive Review on the Genus Plumbago With Focus on Plumbago Auriculata (Plumbaginaceae)

A Comprehensive Review on the Genus Plumbago With Focus on Plumbago Auriculata (Plumbaginaceae)

Potential of the genetically transformed root cultures of Plumbago europaea for biomass and plumbagin production

Pharmacokinetics, toxicity, and cytochrome P450 modulatory activity of plumbagin

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