Moïse Sirlam, Peron Bosco Leutcha, Guy Raphael Sado Nouemsi, Humaira Zafar, Hycienth Fung Tegha, Denis Kehdinga Sema, Virginie Flaure Tsague Tankeu, Yves Oscar Nganso Ditchou, Madan Poka, Patrick Demana, Atia-Tul-Wahab, Muhammad Iqbal Choudhry, Xavier Siwe Noundou, Alain Meli Lannang
{"title":"Two new flavonoids from the leaves of Garcinia smeathmannii, in vitro and in silico anti-inflammatory potentials.","authors":"Moïse Sirlam, Peron Bosco Leutcha, Guy Raphael Sado Nouemsi, Humaira Zafar, Hycienth Fung Tegha, Denis Kehdinga Sema, Virginie Flaure Tsague Tankeu, Yves Oscar Nganso Ditchou, Madan Poka, Patrick Demana, Atia-Tul-Wahab, Muhammad Iqbal Choudhry, Xavier Siwe Noundou, Alain Meli Lannang","doi":"10.1016/j.fitote.2024.106273","DOIUrl":null,"url":null,"abstract":"<p><p>Garcinia smeathmannii is a well-known plant for its uses in the effective treatment of intestinal parasites, skin eruptions and skin burns. The dichloromethane-methanol (2:3) crude extract of the leaves of G. smeathmannii led to the isolation and characterization of twenty compounds (1-20) using chromatographic and spectroscopic techniques. Extracts and compounds were screened in vitro for their anti-inflammatory (ROS), antiglycation and antileishmanial (L. tropica) activities. Compounds were also screened for their in silico anti-inflammatory activities using Maestro 4.2.1 software with the co-crystal complex structures of the ovine oCOX-1: meloxicam (PDB Id: 4O1Z) and murine mCOX-2: meloxicam (PDB Id: 4M11) proteins. An unprecedented flavonol (1) and a flavone dimer (2) together with eighteen known compounds (3-20) were characterized. All the tested samples in vitro revealed no antiglycation and antileishmanial activities. Beside, extracts revealed moderate anti-inflammatory activities (IC<sub>50</sub> ranging from 24.1 ± 2.0 to 34.7 ± 0.8 μg/mL). Only compound (13) revealed an anti-inflammatory activity which was 9.33 times more active than the reference (Ibuprofen, IC<sub>50</sub> = 11.2 ± 1.9 μg/mL) with IC<sub>50</sub> of 1.2 ± 0.0 μg/mL. Compounds (2-9, 11-13 and 19-20) were docked and the docking scores were ranging from -10.178 to -6.119 (kcal/mol) which were in agreement with the experimental anti-inflammatory activity. These results are in agreement with the traditional uses of the leave of G. smeathmannii as cataplasm for skin eruption and as analgesic agent.</p>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":null,"pages":null},"PeriodicalIF":2.5000,"publicationDate":"2024-10-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Fitoterapia","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1016/j.fitote.2024.106273","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0
Abstract
Garcinia smeathmannii is a well-known plant for its uses in the effective treatment of intestinal parasites, skin eruptions and skin burns. The dichloromethane-methanol (2:3) crude extract of the leaves of G. smeathmannii led to the isolation and characterization of twenty compounds (1-20) using chromatographic and spectroscopic techniques. Extracts and compounds were screened in vitro for their anti-inflammatory (ROS), antiglycation and antileishmanial (L. tropica) activities. Compounds were also screened for their in silico anti-inflammatory activities using Maestro 4.2.1 software with the co-crystal complex structures of the ovine oCOX-1: meloxicam (PDB Id: 4O1Z) and murine mCOX-2: meloxicam (PDB Id: 4M11) proteins. An unprecedented flavonol (1) and a flavone dimer (2) together with eighteen known compounds (3-20) were characterized. All the tested samples in vitro revealed no antiglycation and antileishmanial activities. Beside, extracts revealed moderate anti-inflammatory activities (IC50 ranging from 24.1 ± 2.0 to 34.7 ± 0.8 μg/mL). Only compound (13) revealed an anti-inflammatory activity which was 9.33 times more active than the reference (Ibuprofen, IC50 = 11.2 ± 1.9 μg/mL) with IC50 of 1.2 ± 0.0 μg/mL. Compounds (2-9, 11-13 and 19-20) were docked and the docking scores were ranging from -10.178 to -6.119 (kcal/mol) which were in agreement with the experimental anti-inflammatory activity. These results are in agreement with the traditional uses of the leave of G. smeathmannii as cataplasm for skin eruption and as analgesic agent.
期刊介绍:
Fitoterapia is a Journal dedicated to medicinal plants and to bioactive natural products of plant origin. It publishes original contributions in seven major areas:
1. Characterization of active ingredients of medicinal plants
2. Development of standardization method for bioactive plant extracts and natural products
3. Identification of bioactivity in plant extracts
4. Identification of targets and mechanism of activity of plant extracts
5. Production and genomic characterization of medicinal plants biomass
6. Chemistry and biochemistry of bioactive natural products of plant origin
7. Critical reviews of the historical, clinical and legal status of medicinal plants, and accounts on topical issues.