a Department of Organic Chemistry, Faculty of Science , University of Yaoundé I , Yaoundé , Cameroon.
b Department Chemie , Universität Fribourg , Fribourg , Switzerland.
Pharm Biol. 2018 Dec;56(1):318-324. doi: 10.1080/13880209.2018.1476559.
The roots of Lophira lanceolata Van Tiegh. Ex Keay (Ochnaceae) have numerous medicinal values in the Central African region. Even though the MeOH extract of the roots has shown antimycobacterial activities, the constituents responsible for this inhibitory activity remain unknown.
Phytochemical investigation of the MeOH root extract of L. lanceolata and determination of the antimycobacterial activities of that extract and constituents against the growth of Mycobacterium tuberculosis.
Column chromatography was used to provide bioactive phytoconstituents. Those compounds were elucidated using MS and NMR spectroscopic data. Antimycobacterial screening of the extract (4.882-5000 µg/mL in DMSO during 24 h at 37 °C) and isolated compounds (0.244-250 µg/mL in DMSO during 24 h at 37 °C) was performed by microplate alamar blue assay (MABA) against two mycobacterial strains.
The investigation of L. lanceolata MeOH roots extract provided of mixture of unseparated biflavonoids with a newly described one, dihydrolophirone A (1a) associated to lophirone A (1b). The bioactive compounds that effectively inhibited the growth of M. tuberculosis AC45 were found to be compounds 1 and 2. They exhibited MIC values of 31.25 and 15.75 µg/mL, respectively, and their MIC was found to be 62.5 µg/mL against resistant strain AC83.
It is clearly evident from the results obtained that the mycobacterial activity of L. lanceolata could be related mainly to its steroid and flavonoid contents. Therefore, this study suggests the potential of the above-mentioned classes of compounds as promising candidate agents for developing new anti-tuberculosis drugs.
中央非洲地区，露兜树（Ochnaceae）的根具有许多药用价值。尽管甲醇提取物已显示出抗分枝杆菌活性，但负责这种抑制活性的成分仍不清楚。
对露兜树甲醇根提取物进行植物化学研究，并测定该提取物和成分对结核分枝杆菌生长的抗分枝杆菌活性。
使用柱层析法提供生物活性植物成分。使用 MS 和 NMR 光谱数据阐明这些化合物。通过微孔板阿尔玛蓝测定法（MABA）在 DMSO 中（37°C 下 24 小时 4.882-5000µg/mL）对提取物（在 DMSO 中 37°C 下 24 小时 0.244-250µg/mL）和分离化合物进行抗分枝杆菌筛选。
对露兜树甲醇根提取物的研究提供了混合物的未分离二氢黄酮与新描述的二氢洛菲酮 A（1a）相关联到洛菲酮 A（1b）。有效地抑制结核分枝杆菌 AC45 生长的生物活性化合物被发现是化合物 1 和 2。它们的 MIC 值分别为 31.25 和 15.75µg/mL，对耐药株 AC83 的 MIC 值为 62.5µg/mL。
从获得的结果可以清楚地看出，露兜树的分枝杆菌活性可能主要与其甾体和类黄酮含量有关。因此，本研究表明上述类化合物具有作为开发新抗结核药物的有前途的候选药物的潜力。
