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Antiplasmodial Activity (antiplasmodial + activity)
Selected AbstractsSynthesis and Evaluation of the Antitrypanosomal and Antiplasmodial Activities of New 4-Aminobicyclo[2.2.2]octane Derivatives.CHEMINFORM, Issue 5 2006Werner Seebacher Abstract For Abstract see ChemInform Abstract in Full Text. [source] ChemInform Abstract: A New Series of Amodiaquine Analogues (I) Modified in the Basic Side Chain with in vitro Antileishmanial and Antiplasmodial Activity.CHEMINFORM, Issue 15 2010Stefano Guglielmo Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] Synthesis and Antiplasmodial Activity of Highly Active Reverse Analogues of the Antimalarial Drug Candidate FosmidomycinCHEMMEDCHEM, Issue 10 2010Christoph T. Behrendt Inhibition of enzymes involved in the nonmevalonate pathway of isoprenoid biosynthesis represents a promising strategy for the development of novel antimalarial agents. A small series of reverse hydroxamate-based fosmidomycin analogues was synthesized and evaluated for their inhibitory activity against the recombinant 1-deoxy- D -xylulose 5-phosphate reductoisomerases (DXRs) of Escherichia coli and Plasmodium falciparum, as well as for their in vitro antiplasmodial activity and cytotoxicity. [source] Antiplasmodial agents from the Bhutanese medicinal plant Corydalis callianthaPHYTOTHERAPY RESEARCH, Issue 4 2010Phurpa Wangchuk Abstract The alkaloidal components of the Bhutanese medicinal plant Corydalis calliantha Long, which is used for the treatment of malaria, have been assessed. Four known alkaloids, protopine (1), scoulerine (2), cheilanthifoline (3) and stylopine (4) are reported from this plant for the first time. The protopine alkaloid, protopine, and the tetrahydroprotoberine alkaloid, cheilanthifoline, showed promising in vitro antiplasmodial activities against Plasmodium falciparum, both wild type (TM4) and multidrug resistant (K1) strains with IC50 values in the range of 2.78,4.29,µm. Such activity had not been demonstrated previously for cheilanthifoline. The results thus support, at a molecular level, the clinical use of this plant in the Bhutanese traditional medicine and identified cheilanthifoline as a potential new antimalarial drug lead. Copyright © 2009 John Wiley & Sons, Ltd. [source] Antiplasmodial and cytotoxic activity of khellactone derivatives from Angelica purpuraefolia chungPHYTOTHERAPY RESEARCH, Issue 3 2010Ill-Min Chung Abstract The methanolic extract of the rhizomes parts of Agelica purpuraefolia was investigated for its activity against chloroquine-sensitive strains of Plasmodium falciparum using the parasite lactate dehydrogenase assay method. Two natural khellactone, (+)-4,-Decanoyl- cis -khellactone (1) and (+)-3,-Decanoyl- cis -khellactone (2) were isolated from the rhizomes parts of A. purpuraefolia. Two compounds were evaluated for in vitro antiplasmodial activities as well as their cytotoxic potential on SK-OV-3 cancer cell line cells. Compounds 1, 2 showed notable growth inhibitory activity against chloroquine-sensitive strains of Plasmodium falciparum with IC50 values from 1.5 and 2.4,,M. This compound showed no significant cytotoxicity (IC50 > 100,,M) evaluated using SK-OV-3 cancer cell line cells. This is the first report on the antiplasmodial activity of the compounds from A. purpuraefolia. Copyright © 2009 John Wiley & Sons, Ltd. [source] Evaluation of antiprotozoal and plasmodial enoyl-ACP reductase inhibition potential of turkish medicinal plantsPHYTOTHERAPY RESEARCH, Issue 2 2005D. Tasdemir Abstract A total of 58 extracts of different polarity were prepared from various organs of 16 species of Turkish plants and screened for their antitrypanosomal, antileishmanial and antiplasmodial activities. No significant activity was observed against Trypanosoma cruzi, whereas many extracts showed appreciable trypanocidal potential against T. brucei rhodesiense, with the CHCl3 -soluble portion of Phlomis kurdica being the most active (IC50 2.7 µg[sol ]mL). Almost all extracts, particularly the CHCl3 phases, exhibited growth inhibition activity against Leishmania donovani amastigotes. The CHCl3 -solubles of Putoria calabrica roots (IC50 1.9 µg[sol ]mL), Wendlandia ligustroides leaves (IC50 2.1 µg[sol ]mL) and Rhododendronluteum leaves (IC50 2.3 µg[sol ]mL) displayed the highest leishmanicidal potential. The majority of the extracts also possessed antiplasmodial activity against the multi-drug resistant K1 Plasmodium falciparum strain. The most potent antiplasmodial activity was observed with the CHCl3 extracts of Phlomis kurdica (IC50 1.5 µg[sol ]mL), P. leucophracta (IC50 1.6 µg[sol ]mL), Scrophularia cryptophila (IC50 1.8 µg[sol ]mL), Morina persica (IC50 1.9 µg[sol ]mL) and the aqueous root extract of Asperula nitida subsp. subcapitellata (IC50 1.6 µg[sol ]mL). Twenty-one extracts with significant antimalarial activity (IC50 < 5 µg[sol ]mL) were also tested for their ability to inhibit the purified enoyl-ACP reductase (FabI), a crucial enzyme in the fatty acid biosynthesis of P. falciparum. The CHCl3 extract of Rhododendronungernii leaves (IC50 10 µg[sol ]mL) and the H2O-soluble portion of Rhododendronsmirnovii leaves (IC50 0.4 µg[sol ]mL) strongly inhibited the FabI enzyme. The preliminary data indicate that some (poly)phenolic compounds are responsible for the FabI inhibition potential of these extracts. The presented work reports for the first time the antiprotozoal activity of nine different genera as well as a target specific antimalarial screening for the identification of P. falciparum FabI inhibitors from medicinal plant extracts. Copyright © 2005 John Wiley & Sons, Ltd. [source] Shuangancistrotectorines,A,E, Dimeric Naphthylisoquinoline Alkaloids with Three Chiral Biaryl Axes from the Chinese Plant Ancistrocladus tectoriusCHEMISTRY - A EUROPEAN JOURNAL, Issue 14 2010Minjuan Xu Abstract Five novel dimeric naphthylisoquinoline alkaloids, shuangancistrotectorines,A (3,a), B (3,b), C (4), D (5,a), and E (5,b), have been isolated from the twigs of the Chinese plant Ancistrocladus tectorius. Their absolute stereostructures were determined by spectroscopic and chiroptical methods in combination with quantum chemical CD calculations. In contrast to all other known dimeric naphthylisoquinoline alkaloids, in which the central binaphthalene axis is 6,,6,,-coupled and thus not rotationally hindered, the dimers described here are linked via the sterically more hindered 3,,3,,- or 1,,1,,-positions of the naphthalene units. They are thus the first such dimers,and even the very first natural products at all,that have three consecutive stereogenic axes. Hence, including the stereogenic centers, they have up to seven stereogenic units in total. Some of the compounds, in particular shuangancistrotectorines,A, B, and D (3,a, 3,b, and 5,a) exhibit very good, and specific, antiplasmodial activities. [source] Novel Alkaloids from Myrioneuron nutansEUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Issue 9 2009Van Cuong Pham Abstract Two new alkaloids, dehydronitraramine (1) and N -formylmyrionine (2) were isolated from the leaves of Myrioneuron nutans, and their structures were determined from spectroscopic analysis, including mass spectrometry and 2D-NMR spectroscopy. The absolute configuration 8S, 9R, 10S of N -formylmyrionine (2) was established by N -formylation of the known (8S,9R,10S)-myrionine and then comparison of the optical rotation of the natural N -formylmyrionine (2) with that of the semi-synthetic (8S,9R,10S)- N -formylmyrionine. Dehydronitraramine (1) displayed a moderate antiplasmodial activity against Plasmodiumfalciparum with an IC50 value of 16 ,M, whereas both 1 and 2 showed a weak cytotoxicity against KB cells.(© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2009) [source] Antiplasmodial and cytotoxic activity of khellactone derivatives from Angelica purpuraefolia chungPHYTOTHERAPY RESEARCH, Issue 3 2010Ill-Min Chung Abstract The methanolic extract of the rhizomes parts of Agelica purpuraefolia was investigated for its activity against chloroquine-sensitive strains of Plasmodium falciparum using the parasite lactate dehydrogenase assay method. Two natural khellactone, (+)-4,-Decanoyl- cis -khellactone (1) and (+)-3,-Decanoyl- cis -khellactone (2) were isolated from the rhizomes parts of A. purpuraefolia. Two compounds were evaluated for in vitro antiplasmodial activities as well as their cytotoxic potential on SK-OV-3 cancer cell line cells. Compounds 1, 2 showed notable growth inhibitory activity against chloroquine-sensitive strains of Plasmodium falciparum with IC50 values from 1.5 and 2.4,,M. This compound showed no significant cytotoxicity (IC50 > 100,,M) evaluated using SK-OV-3 cancer cell line cells. This is the first report on the antiplasmodial activity of the compounds from A. purpuraefolia. Copyright © 2009 John Wiley & Sons, Ltd. [source] Evaluation of antioxidant and antimicrobial properties of Soymida febrifuga leaf extractsPHYTOTHERAPY RESEARCH, Issue 7 2008Boreddy Srinivas Reddy Abstract The present study was designed to evaluate the antioxidant and antimicrobial properties of hexane (LH), methanol (LM) and aqueous (LA) extracts of Soymida febrifuga (Maliaceae) leaves, which is a traditional folk medicine in India. No pharmacological evaluation of this plant (except antiplasmodial activity) has been reported to date. Antioxidant activity of different extracts was evaluated by DPPH free radical scavenging activity, taking total phenolic content (TPC) as an index. Antimicrobial activity was tested against six bacterial and five fungal strains using the agar hole diffusion method and the minimum inhibitory concentrations (MIC) and minimum microbicidal concentration (MMC) were determined for all the test organisms against the extracts. The results showed that the methanol and aqueous extracts of leaf had a higher antioxidant activity and total phenolic content than the hexane extract. The antioxidant activity and TPC of the extracts were highly correlated. Extracts also showed several degrees of antimicrobial activity against different microbes. The methanol extract was more potent against Aspergillus fumigatus and Candida tropicana. The lowest MIC values obtained for LM, LA and LH were 78, 156, 625 µg/mL against A. fumigatus, C. tropicana and C. albicans, respectively. Hence, this study confirms that Soymida febrifuga leaves possess potent antioxidant and antimicrobial activity. Copyright © 2008 John Wiley & Sons, Ltd. [source] Antimalarial compounds from Kniphofia foliosa rootsPHYTOTHERAPY RESEARCH, Issue 6 2005Abraham Abebe Wube Abstract During the course of screening Ethiopian medicinal plants for their antimalarial properties, it was found that the dichloromethane extract of the roots of Kniphofia foliosa Hochst. (Asphodelaceae), which have long been used in the traditional medicine of Ethiopia for the treatment of abdominal cramps and wound healing, displayed strong in vitro antiplasmodial activity against the chloroquine-sensitive 3D7 strain of Plasmodium falciparum with an ED50 value of 3.8 µg/mL and weak cytotoxic activity against KB cells with an ED50 value of 35.2 µg/mL. Five compounds were isolated from the roots and evaluated for their invitro antimalarial activity. Among the compounds tested, 10-(chrysophanol-7,-yl)-10-(,)-hydroxychrysopanol-9-anthrone and chryslandicin, showed a high inhibition of the growth of the malaria parasite, P. falciparum with ED50 values of 0.260 and 0.537 µg/mL, respectively, while the naphthalene derivative, 2-acetyl-1-hydroxy-8-methoxy-3-methylnaphthalene, exhibited a less significant antimalarial activity with an ED50 value of 15.4 µg/mL. To compare the effect on the parasite with toxicity to mammalian cells, the cytotoxic activities of the isolated compounds against the KB cell line were evaluated and 10-(chrysophanol-7,-yl)-10-(,)-hydroxychrysopanol-9-anthrone and chryslandicin displayed very low toxicity with ED50 values of 104 and 90 µg/mL, respectively. This is the first report of the inhibition of the growth of P. falciparum by anthraquinone-anthrone dimers and establishes them as a new class of potential antimalarial compounds with very little host cell toxicity. Copyright © 2005 John Wiley & Sons, Ltd. [source] Evaluation of antiprotozoal and plasmodial enoyl-ACP reductase inhibition potential of turkish medicinal plantsPHYTOTHERAPY RESEARCH, Issue 2 2005D. Tasdemir Abstract A total of 58 extracts of different polarity were prepared from various organs of 16 species of Turkish plants and screened for their antitrypanosomal, antileishmanial and antiplasmodial activities. No significant activity was observed against Trypanosoma cruzi, whereas many extracts showed appreciable trypanocidal potential against T. brucei rhodesiense, with the CHCl3 -soluble portion of Phlomis kurdica being the most active (IC50 2.7 µg[sol ]mL). Almost all extracts, particularly the CHCl3 phases, exhibited growth inhibition activity against Leishmania donovani amastigotes. The CHCl3 -solubles of Putoria calabrica roots (IC50 1.9 µg[sol ]mL), Wendlandia ligustroides leaves (IC50 2.1 µg[sol ]mL) and Rhododendronluteum leaves (IC50 2.3 µg[sol ]mL) displayed the highest leishmanicidal potential. The majority of the extracts also possessed antiplasmodial activity against the multi-drug resistant K1 Plasmodium falciparum strain. The most potent antiplasmodial activity was observed with the CHCl3 extracts of Phlomis kurdica (IC50 1.5 µg[sol ]mL), P. leucophracta (IC50 1.6 µg[sol ]mL), Scrophularia cryptophila (IC50 1.8 µg[sol ]mL), Morina persica (IC50 1.9 µg[sol ]mL) and the aqueous root extract of Asperula nitida subsp. subcapitellata (IC50 1.6 µg[sol ]mL). Twenty-one extracts with significant antimalarial activity (IC50 < 5 µg[sol ]mL) were also tested for their ability to inhibit the purified enoyl-ACP reductase (FabI), a crucial enzyme in the fatty acid biosynthesis of P. falciparum. The CHCl3 extract of Rhododendronungernii leaves (IC50 10 µg[sol ]mL) and the H2O-soluble portion of Rhododendronsmirnovii leaves (IC50 0.4 µg[sol ]mL) strongly inhibited the FabI enzyme. The preliminary data indicate that some (poly)phenolic compounds are responsible for the FabI inhibition potential of these extracts. The presented work reports for the first time the antiprotozoal activity of nine different genera as well as a target specific antimalarial screening for the identification of P. falciparum FabI inhibitors from medicinal plant extracts. Copyright © 2005 John Wiley & Sons, Ltd. [source] Synthesis and Antiplasmodial Activity of Highly Active Reverse Analogues of the Antimalarial Drug Candidate FosmidomycinCHEMMEDCHEM, Issue 10 2010Christoph T. Behrendt Inhibition of enzymes involved in the nonmevalonate pathway of isoprenoid biosynthesis represents a promising strategy for the development of novel antimalarial agents. A small series of reverse hydroxamate-based fosmidomycin analogues was synthesized and evaluated for their inhibitory activity against the recombinant 1-deoxy- D -xylulose 5-phosphate reductoisomerases (DXRs) of Escherichia coli and Plasmodium falciparum, as well as for their in vitro antiplasmodial activity and cytotoxicity. [source] | ||||||||||