Pentacyclic triterpenoids from Mitracarpus frigidus (Willd. ex Roem. &amp; Schult.) K. Shum: in vitro cytotoxic and leishmanicidal and in vivo anti-inflammatory and antioxidative activities

Fabri, Rodrigo Luiz; Garcia, Roberta Alvim; Florêncio, Jônatas Rodrigues; Carvalho, Lidiane O. de; Pinto, Nícolas de Castro Campos; Coimbra, Elaine Soares; Souza-Fagundes, Elaine M.; Ribeiro, Antônia; Scio, Elita

doi:10.1007/s00044-014-1093-y

Cited by 14 publications

(3 citation statements)

References 55 publications

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“…For example, lupeol was found to have anti-cancer and anti-inflammatory properties [Saleem, 2009]. Methyl ursolate displayed in vitro cytotoxic and leishmanicidal activities, while in vivo anti-inflammatory and antioxidative abilities [Fabri et al, 2014]. Lupeol acetate showed to slow down the progression of rheumatoid arthritis by inhibiting the activation of macrophages and osteoclastogenesis [Wang et al, 2016].…”

Section: Resultsmentioning

confidence: 99%

Chemical Content of L. Serriola: Fatty Acid Esters and Triterpene Compounds From the Roots

Shukurlu¹

2020

plantfungalres

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This work aimed to study the chemical composition of the crystalline mass obtained from the acetone extract of the roots of Lactuca serriola L. Its characterization by gas chromatography-mass spectrometry (GC-MS) analyses led to the identification of 21 substances including palmitic acid, methyl ester, n-hexadecanoic acid, methyl-trans-oleate, 11-octadecenoic acid methyl ester, methyl stearate, oleic acid, 11-eicosenoic acid methyl ester, common in the most plant species. Furthermore, some triterpenoid compounds [olean-12-en-3-one, 13,27-cycloursan-3-one, ursa-9(11),12-dien-3-yl acetate, lupeol, germanicol, lup-20( 29)-en-3-ol, acetate, (3β)] characteristic of the L. serriola were identified. Despite the richness of chemical composition and the wide availability in Azerbaijani flora, L. serriola is still uninvestigated. Therefore, the study of the qualitative and quantitative composition of this plant represent interest.

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Section: Resultsmentioning

confidence: 99%

Chemical Content of L. Serriola: Fatty Acid Esters and Triterpene Compounds From the Roots

Shukurlu¹

2020

plantfungalres

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“…195 On testing their in vitro antileishmanial activity against amastigote form of L. major, the pentacyclic triterpenoids ursolic acid (103) and Me ursolate (104) obtained from the aerial parts of the plant Mitracarpus frigidus, were found to possess IC 50 values of 0.28 mM and 0.45 mM, respectively. 196 Compound (105), a nor-triterpene isolated from Lophanthera lactescens, showed antileishmanial activity against amastigote form of L. amazonensis with IC 50 value of 0.50 mM. 197 6.1.5.…”

Section: Brief Summary Of Promising Scaffoldsmentioning

confidence: 99%

Antileishmanial drug discovery: comprehensive review of the last 10 years

Sangshetti¹,

Khan²,

Kulkarni³

et al. 2015

RSC Adv.

133

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“…The seriousness of the disease prompted several research groups to work on the development of new antileishmanial agents and the class of scaffolds explored includes various quinolines, [10–13] chalcones, [14,15] nitroimidazole, [16] triazolopyrimidine, [17] pyrazolopyrimidine, [18,19] aminopyrazole, [20] triazine, [21,22] quinazoline, [23] thymidine, [24] triterpenoids, [25] and quinazolinone [26] . The isolation and synthesis of a new class of biaryl naphthylisoquinoline alkaloid ancistroealaine A ( 1a ) from Ancistrocladus ealaensis and other alkaloids ( 1b , 1c ), and their antileishmanial activity has generated interest in the development of new antileishmanial agents [27–29] .…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis of Biaryl Piperidine Derivatives and Their Evaluation as Potential Antileishmanial Agents against Leishmania donovani Strain Ag83

Rathnakar

Sinha

Prasad

et al. 2021

Chemistry & Biodiversity

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We have developed a new series of simple biaryl piperidine derivatives (11-19) based on biaryl naphthylisoquinoline alkaloid Ealamine-A. The target compounds were synthesized, analyzed by spectral data, and evaluated for antileishmanial activity against Leishmania donovani strain Ag83 by MTT assay. The compounds have shown the best to moderate antileishmanial activity. The 5'-fluoro-2'-methoxyphenyl derivative 14 and 3',5'-difluorophenyl derivative 16 have inhibited the promastigotes by 86 % and 85 % after 24 h and 92 % and 91 % after 48 h incubation, respectively, at 400 μM concentration. The % inhibition was lower with the lowering of the concentration and increased with the incubation time. Compounds 12, 15, and 18 have solubility issues and proved to be less active than the rest of the compounds. Molecular docking studies were performed on selective active compounds and the results indicate that these compounds may act by binding to the Leishmanolysin and the docking scores are in good correlation with the antileishmanial activity. These results provide an initial insight into the design of new therapeutics for neglected tropical diseases.

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Pentacyclic triterpenoids from Mitracarpus frigidus (Willd. ex Roem. & Schult.) K. Shum: in vitro cytotoxic and leishmanicidal and in vivo anti-inflammatory and antioxidative activities

Cited by 14 publications

References 55 publications

Chemical Content of L. Serriola: Fatty Acid Esters and Triterpene Compounds From the Roots

Chemical Content of L. Serriola: Fatty Acid Esters and Triterpene Compounds From the Roots

Antileishmanial drug discovery: comprehensive review of the last 10 years

Design, Synthesis of Biaryl Piperidine Derivatives and Their Evaluation as Potential Antileishmanial Agents against Leishmania donovani Strain Ag83

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