Cytotoxic and Antiplasmodial Compounds from the Roots of <i>Strophioblachia fimbricalyx</i>

Seephonkai, Prapairat; Sangdee, Aphidech; Bunchalee, Pasakorn; Pyne, Stephen G.

doi:10.1021/np900352n

Cited by 19 publications

(34 citation statements)

References 8 publications

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“…Seephonkai et al [ 46 ] studied the Thai traditional medicinal plant Strophioblachia fimbricalyx , and isolated 9- O -demethyltrigonostemone ( 87 ) and a new phenanthropolone, 3,6,9-trimethoxyphenanthropolone ( 88 ), which exhibited antimalarial activity against the multiresistant K1 strain of P. falciparum with IC 50 values of 8.7 and 9.9 μM, respectively ( Figure 16 ).…”

Section: Plant-derived Antimalarial Compoundsmentioning

confidence: 99%

Antimalarial Activity of Plant Metabolites

Pan

Shi

et al. 2018

IJMS

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Malaria, as a major global health problem, continues to affect a large number of people each year, especially those in developing countries. Effective drug discovery is still one of the main efforts to control malaria. As natural products are still considered as a key source for discovery and development of therapeutic agents, we have evaluated more than 2000 plant extracts against Plasmodium falciparum. As a result, we discovered dozens of plant leads that displayed antimalarial activity. Our phytochemical study of some of these plant extracts led to the identification of several potent antimalarial compounds. The prior comprehensive review article entitled “Antimalarial activity of plant metabolites” by Schwikkard and Van Heerden (2002) reported structures of plant-derived compounds with antiplasmodial activity and covered literature up to the year 2000. As a continuation of this effort, the present review covers the antimalarial compounds isolated from plants, including marine plants, reported in the literature from 2001 to the end of 2017. During the span of the last 17 years, 175 antiplasmodial compounds were discovered from plants. These active compounds are organized in our review article according to their plant families. In addition, we also include ethnobotanical information of the antimalarial plants discussed.

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Section: Plant-derived Antimalarial Compoundsmentioning

confidence: 99%

Antimalarial Activity of Plant Metabolites

Pan

Shi

et al. 2018

IJMS

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“…A new phenanthrenone, 9-O-demethyltrigonostemone (37), and a new phenanthropolone (38) were isolated from the roots of Strophioblachia fimbricalyx Boerl. (Euphorbiaceae) and displayed antiplasmodial activity (IC 50 values of 8.7 and 9.9 µM, respectively) against K1 [25]. Fractionation of the ethyl acetate extract of Carpesium cernuum L. (Asteraceae) yielded four characterised sesquiterpenoid lactones among which 11(13)-dehydroivaxillin (57) and 11-epi-ivaxillin (58) exhibited antiplasmodial activity against D10 with IC 50 values of 2.0 and 9.3 µM [34].…”

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confidence: 99%

Natural Products Published in 2009 from Plants Traditionally Used to Treat Malaria

Béro

Quetin-Leclercq

2010

Planta Med

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Malaria is a major parasitic disease and is responsible for almost one million deaths each year in Africa. There is an urgent need to discover new active compounds. Nature and particularly plants are a potential source of new antimalarial drugs since they contain a quantity of metabolites with a great variety of structures and pharmacological activities. This review covers the compounds with antiplasmodial activity isolated from plants which have been published during 2009 organized according to their phytochemical classes. Details are given for substances with IC₅₀ values ≤ 11 µM. Sixty-seven references are identified.

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“…As shown in Fig. 3a , compound 2 , 9-O-demethyltrigonostemone, was isolated from the roots of Trigonostemon chinensis and has been reported to show cytotoxicity in multiple types of cancer cells [ 24 ]. Compound 7 is shikonin from Radix Arnebiae and was reported to possess anti-inflammatory activity [ 25 ].…”

Section: Resultsmentioning

confidence: 99%

Discovery and characterization of natural products as novel indoleamine 2,3-dioxygenase 1 inhibitors through high-throughput screening

et al. 2019

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Indoleamine 2,3-dioxygenase 1 (IDO1) is emerging as a promising therapeutic target for the treatment of malignant tumors characterized by dysregulated tryptophan metabolism. However, the antitumor efficacy of existing small-molecule IDO1 inhibitors is still unsatisfactory, and the underlying mechanism remains largely undefined. To identify novel IDO1 inhibitors, an in-house natural product library of 2000 natural products was screened for inhibitory activity against recombinant human IDO1. High-throughput fluorescence-based screening identified 79 compounds with inhibitory activity > 30% at 20 μM. Nine natural products were further confirmed to inhibit IDO1 activity by > 30% using Ehrlich’s reagent reaction. Compounds 2 , 7 , and 8 were demonstrated to inhibit IDO1 activity in a cellular context. Compounds 2 and 7 were more potent against IDO1 than TDO2 in the enzymatic assay. The kinetic studies showed that compound 2 exhibited noncompetitive inhibition, whereas compounds 7 and 8 were graphically well matched with uncompetitive inhibition. Compounds 7 and 8 were found to bind to the ferric-IDO1 enzyme. Docking stimulations showed that the naphthalene ring of compound 8 formed “T-shaped” π–π interactions with Phe-163 and that the 6-methyl-naphthalene group formed additional hydrophobic interactions with IDO1. Compound 8 was identified as a derivative of tanshinone, and preliminary SAR analysis indicated that tanshinone derivatives may be promising hits for the development of IDO1 inhibitors. This study provides new clues for the discovery of IDO1/TDO2 inhibitors with novel scaffolds.

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Cytotoxic and Antiplasmodial Compounds from the Roots of Strophioblachia fimbricalyx

Cited by 19 publications

References 8 publications

Antimalarial Activity of Plant Metabolites

Antimalarial Activity of Plant Metabolites

Natural Products Published in 2009 from Plants Traditionally Used to Treat Malaria

Discovery and characterization of natural products as novel indoleamine 2,3-dioxygenase 1 inhibitors through high-throughput screening

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