Agbo Elizabeth O, Anyam John V, Agber Cyprian T, Adah Christie A, Agbo Christopher, Ijeomah Augustina O, Tor-Anyiin Terrumun A, Alkhalaf Hamed E, Sarode Aditya, Asseri Jamal I, Gray Alexander I, Igoli John O, De Koning Harry P
Phytochemistry Research Group, Department of Chemistry, Joseph Sarwuan Tarka University, Makurdi PMB 2373, Benue State, Nigeria.
Department of Chemistry, Benue State University, Makurdi PMB 102119, Benue State, Nigeria.
Molecules. 2025 Jun 5;30(11):2468. doi: 10.3390/molecules30112468.
The phytochemical screening of extracts of tubers has afforded the isolation of two novel chalcones, tarkalynins A and B, along with taccalonolide A and its 12-propanoate. The screening of stem bark yielded taraxerol acetate, dihydrochelerythrin and fagaramide. These compounds were obtained through column and thin-layer chromatography and identified using NMR and LC-HRMS. The compounds were tested against s427 and its multi-drug-resistant clone B48, against , and , and against . Cytotoxicity was tested against the human HEK293 cell line. The highest activities were observed with dihydrochelerythrin and fagaramide against s427 and B48, , and , with EC values of 1.37, 2.559, 1.09, and 5.44 µM and 17.8, 10.9, 10.9, and 13.3 µM, respectively. In addition, tarkalynin A and taraxerol acetate displayed promising activity against (EC = 21.4 and 21.3 µM, respectively). None of these compounds showed significant cross-resistance with existing trypanocides (RF ≈ 1; > 0.05). The compounds displayed low toxicity to human cells, with most exhibiting no growth inhibition at concentrations of 100, or even 300 µM. This report provides further evidence of the potential use of natural products for combating parasitic diseases.
对块茎提取物进行植物化学筛选，分离出了两种新型查耳酮，即塔卡林宁A和B，以及塔卡洛内酯A及其12 - 丙酸酯。对茎皮进行筛选得到了乙酸蒲公英赛醇、二氢白屈菜红碱和法加酰胺。这些化合物通过柱色谱和薄层色谱获得，并使用核磁共振和液相色谱 - 高分辨质谱进行鉴定。对这些化合物针对s427及其多药耐药克隆B48、针对……、针对……以及针对……进行了测试。对人HEK293细胞系进行了细胞毒性测试。观察到二氢白屈菜红碱和法加酰胺对s427和B48、……以及……的活性最高，其EC值分别为1.37、2.559、1.09和5.44 μM以及17.8、10.9、10.9和13.3 μM。此外，塔卡林宁A和乙酸蒲公英赛醇对……显示出有前景的活性（EC分别为21.4和21.3 μM）。这些化合物均未显示出与现有锥虫杀灭剂有显著的交叉耐药性（RF≈1；P>0.05）。这些化合物对人细胞毒性较低，大多数在100 μM甚至300 μM浓度下均未表现出生长抑制。本报告为天然产物用于对抗寄生虫病的潜在用途提供了进一步的证据。
