Trypanocidal Constituents in Plants. 1. Evaluation of Some Mexican Plants for Their Trypanocidal Activity and Active Constituents in Guaco, Roots of Aristolochia taliscana.

Abe, Fumiko; Nagafuji, Shinya; Yamauchi, Tatsuo; Okabe, Hikaru; Maki, Jun; Higo, Hiroo; Akahane, H.; Aguilar, Abigaı́l; Manuel, José; Reyes-Chilpa, Ricardo

doi:10.1248/bpb.25.1188

Cited by 62 publications

(49 citation statements)

References 18 publications

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“…The methanol extract from P. sapota stems presented trypanocidal activity in vitro (2 mg/mL) against epimastigote form of Trypanossoma cruzi (Abe et al, 2002). The ethanol extract from P. venosa leaves (250 mg/mL), as well as the hydroethanol fraction (500 mg/mL), presented antimalarial (against Plasmodium berghei) activity in vivo reducing the induced infection in rats (Montenegro et al, 2006).…”

Section: Trypanocidal and Antimalarial Activitiesmentioning

confidence: 99%

Genus Pouteria: chemistry and biological activity

Silva¹,

Simeoni²,

Silveira³

2009

Rev. bras. farmacogn.

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RESUMO: "Gênero Pouteria: Química e atividade biológica". O gênero Pouteria pertence à família Sapotaceae e pode ser encontrado em muitos continentes. As plantas desse gênero têm sido utilizadas na construção civil, na alimentação e também na medicina popular. Algumas atividades biológicas são reportadas às espécies desse gênero, tais como, antioxidante, anti-inflamatória, antibacteriana e antifúngica, mas seu real potencial como fonte de novos fármacos ainda é pouco conhecido. Assim, uma revisão sobre a composição química e as atividades biológicas de Pouteria é apresentada, com o intuito de estimular a continuação dos estudos das espécies aqui citadas, e a investigação de outras espécies para as quais não foram encontrados relatos.Unitermos: Pouteria, Sapotaceae, triterpenos, flavonoides, plantas medicinais. ABSTRACT:The genus Pouteria belongs to the family Sapotaceae and can be widely found around the World. These plants have been used as building material, as food, because the eatable fruits, as well as remedies in folk medicine. Some biological activities have been reported to species of this genus such as antioxidant, anti-inflammatory, antibacterial and antifungal. However, the real potential of this genus as source of new drugs or phytomedicines remains unknown. Therefore, a review of the so far known chemical composition and biological activities of this genus is presented to stimulate new studies about the species already reported moreover that species have no reference about chemistry or biological activities could be found until now.

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Section: Trypanocidal and Antimalarial Activitiesmentioning

confidence: 99%

Genus Pouteria: chemistry and biological activity

Silva¹,

Simeoni²,

Silveira³

2009

Rev. bras. farmacogn.

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“…10) MC 100 values of compounds 1-10 against epimastigotes and trypomastigotes were estimated by the same method as mentioned in the previous papers, 2,9) and are summarized in Table 3. Gentian violet 11) and ketoconazole 12) were also tested for comparison.…”

Section: 9)mentioning

confidence: 99%

Trypanocidal Constituents in Plants: 4. Withanolides from the Aerial Parts of Physalis angulata

Nagafuji

Okabe

Akahane

et al. 2004

Biological & Pharmaceutical Bulletin

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In the previous paper in this series, 2) we described the identification of trypanocidal xanthones in Garcinia subelliptica against epimastigotes and trypomastigotes of the protozoan Trypanosoma cruzi, which is the etiologic agent of Chagas' disease (American trypanosomiasis). In the course of our search for trypanocidal constituents in plants, we have found that the MeOH extract of the aerial parts of Physalis angulata L. (Solanaceae) showed considerable activity.P. angulata is indigenous to tropical America and was naturalized in Japan in the Edo era. It is an annual small herb and has been traditionally utilized for antipyretic purposes in Japan.3) The isolation of ergostane-type steroidal compounds, physagulins A-G, 4-6) withangulatin A 7) and physalins, 8) has been reported from this plant.T. cruzi is transformed into three stages in its life cycle: epimastigote in the insect gut; trypomastigote, an infectious form in the mammalian blood stream; and amastigote, a proliferative form in mammalian cells. During the isolation procedure, trypanocidal activity was monitored against epimastigotes, because it is easy to cultivate them and they are not infectious. Ten withanolides (1-10) were isolated from the active fraction. To check the therapeutic possibility of these withanolides, trypanocidal activity against trypomastigotes, an infectious form, was examined. Furthermore, evaluation of the IC 50 value against epimastigotes was performed using Cell Counting Kit-8 in order to compare with cytotoxicity at the IC 50 value. In this paper we describe the structural elucidation of the four new withanolides (2, 5, 9, 10) and the trypanocidal activity of the isolates. The possibility of chemotherapeutic utility is also discussed. MATERIALS AND METHODSPlant Materials P. angulata was cultivated in the medicinal plant garden of Fukuoka University and harvested in September 2002. The aerial parts were air-dried and powdered.Instruments and Reagents The instruments used in this study were a JEOL JNM-A500 for NMR spectra (500 MHz for 1 H-NMR, 125 MHz for 13 C-NMR), a JEOL JMS-HX 110 for MS spectra, a JASCO DIP 360 polarimeter for optical rotations, and a Labsystems Multiskan JX Microplate Reader for measuring the absorbance of a formazan product. The following materials were used for chromatography: Diaion HP-20 (a styrene polymer, Mitsubishi Chemical Industries, Ltd.), Silica gel 60N (Cica), Sephadex LH-20 (Pharmacia Fine Chemicals), and YMC gel (ODS, YMC Co. Ltd.). Newborn calf serum (NCS) was purchased from Nacalai Tesque. Dulbecco's modified Eagle's medium (DMEM) and RPMI 1640 medium were purchased from Sigma. Gentian violet, ketoconazole, and 3-(4,5-dimethyl-thiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) were purchased from Wako. A Cell Counting Kit-8 was purchased from Dojindo. Other reagents are the same as in the previous papers. 2,9)Cultivation of T. cruzi The strain of T. cruzi used in this study and the cultivation methods of epimastigotes and trypomastigotes were the same as those described in the previous p...

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“…The search of new drugs against leishmaniasis, potentially compounds and their derivatives have been described in the literature. [14][15][16] Neolignans are groups of compounds that show a wide range of biological effects including antifungal, [17][18][19] anti-schistosomal, [20][21][22][23] antiplasmodial, 24 trypanocidal, [25][26][27] antibacterial, 28 anti-PAF, 29,30 antipsychotic, 31 antioxidant, 32,33 activities, and biological activity against Escherichia coli,…”

Section: Introductionmentioning

confidence: 99%

Synthesis, X-ray crystal structure and theoretical calculations of antileishmanial neolignan analogues

Nascimento¹,

Santos²,

Santos³

et al. 2010

J. Braz. Chem. Soc.

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A síntese e a estrutura cristalina por difração de raios-X de dois análogos de neolignanas, 2-(4-clorofenil)-1-feniletanona (20) e 2-[tio(4-clorofenil)]-1-(3,4-dimetoxifenil)propan-1-ona (12) são descritas. O composto 12 apresenta atividade intracelular contra Leishmania donovani e Leishmania amazonensis de amastigotas que causam a leishmaniose tegumentar e visceral. Além disso, a teoria do funcional de densidade (DFT) com o funcional híbrido B3LYP foi empregado para calcular um conjunto de descritores moleculares para dezenove análogos sintéticos de neolignanas com atividades antileishmaniose. Posteriormente, a análise discriminante stepwise foi realizada para investigar possíveis relações entre a estrutura molecular e atividades biológicas. Por meio dessa análise os compostos foram classificados em dois grupos ativos e inativos de acordo com seu grau de atividade biológica, e as propriedades mais importantes foram as cargas de alguns átomos, a afinidade eletrônica e o ClogP.The synthesis and X-ray crystal diffraction structure of two analogues of neolignans, 2-(4-chlorophenyl)-1-phenylethanone (20) and 2-[(4-chlorophenyl)thio]-1-(3,4-dimethoxyphenyl) propan-1-one (12) is described. The compound 12 presents activity against intracellular Leishmania donovani and Leishmania amazonensis amastigotes that cause cutaneous and visceral leishmaniasis. In addition, the density functional theory (DFT) with the B3LYP hybrid functional was employed to calculate a set of molecular descriptors for nineteen synthetic analogues of neolignans with antileishmanial activities. Afterwards, the stepwise discriminant analysis was performed to investigate possible relationship between the molecular descriptors and biological activities. Through this analysis the compounds were classified into two groups active and inactive according to their degree of biological activities, and the more important properties were charges on some key atoms, electronic affinity and ClogP.

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Trypanocidal Constituents in Plants. 1. Evaluation of Some Mexican Plants for Their Trypanocidal Activity and Active Constituents in Guaco, Roots of Aristolochia taliscana.

Cited by 62 publications

References 18 publications

Genus Pouteria: chemistry and biological activity

Genus Pouteria: chemistry and biological activity

Trypanocidal Constituents in Plants: 4. Withanolides from the Aerial Parts of Physalis angulata

Synthesis, X-ray crystal structure and theoretical calculations of antileishmanial neolignan analogues

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