Anti-inflammatory, pro-proliferative and antimicrobial potential of the compounds isolated from Daemonorops draco (Willd.) Blume
Anti-inflammatory, pro-proliferative and antimicrobial potential of the compounds isolated from Daemonorops draco (Willd.) Blume
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DOI：
10.1016/j.jep.2020.113668
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发表时间：
2021-03-25
影响因子：
5.4
通讯作者：
Ortega Domenech, M.
中科院分区：
文献类型：
--
作者：
Apaza Ticona, L.;Rumbero Sanchez, A.;Ortega Domenech, M.
民族药理学相关性：Daemonorops draco（D. Draco）通常被称为“龙的血”，是印度尼西亚Momok、Anak Dalam和Talang Mamak部落最常用的植物之一，作为伤口愈合的药物。龙树脂此外，对两种细菌和一种酵母菌的抗菌活性进行了分析。材料和方法：生物导向分离的化合物具有抗炎，促增殖和抗菌活性的D。测定了血竭树脂对THP-1、HaCaT、NIH-3 T3细胞NF-κ B的抑制和Nrf 2的激活作用，对NIH-3 T3和HaCaT细胞的增殖作用，以及对大肠杆菌的抗菌作用。coli、S. aureus和C. albicans.Results:通过生物测定的引导分离产生了三种化合物的分离和通过核磁共振和质谱的表征：1（贝沙罗汀）、2（塔斯品碱）和3（2-羟基-1-萘甲醛异烟酰腙）。所有化合物均显示NF-κ B抑制活性，IC 50值分别为0.10-0.13、0.22-0.24和3.75-4.78 μ M，而阳性对照雷公藤红素的IC 50值为7.96 μ M。同样，所有化合物均显示出Nrf 2的活化作用，EC 50值分别为5.34-5.43、163.20-169.20和300.82-315.56 nM，而阳性对照CDDO-Me的EC 50为0.11 nM。此外，关于促增殖活性，化合物1（IC 50 = 8.62-8.71 nM）显示能力为100%，化合物2（IC 50 = 166-171 nM）显示出75%的能力，并且化合物3（IC 50 = 469-486 nM）显示出65%的能力，而FSB 10%（阳性对照）在NIH 3 T3细胞系（成纤维细胞）和HaCaT（角质形成细胞）中具有100%的促增殖活性。最后，所有化合物显示出抗微生物活性，其MIC值分别为0.12-0.16、0.31-0.39和3.96-3.99 μ M。金黄色葡萄球菌E. coli和C.结论：本研究首次从D. albicans树脂中分离得到3个化合物：贝沙罗汀、塔斯品碱和2-羟基-1-萘甲醛异烟酰腙。血竭，具有抗炎、促增殖和抗微生物活性。
Ethno-pharmacological relevance: Daemonorops draco (D. draco) commonly known as "Dragon's blood" is one of the most used plants by Momok, Anak Dalam and Talang Mamak tribes from Indonesia as a remedy for wound healing.Aim of the study: This study aimed to identify the extract, fractions and compounds responsible for the anti-inflammatory and pro-proliferative activities of the D. draco resin. Additionally, the antimicrobial activity against two bacteria and one yeast species was analysed.Materials and methods: Bio-guided isolation of compounds with anti-inflammatory, pro-proliferative and antimicrobial activities from the D. draco resin was carried out by measuring: the inhibition of NF-kappa B and activation of Nrf2 in THP-1, HaCaT, NIH-3T3 cells; cell proliferation in NIH-3T3 and HaCaT cells; and the antimicrobial effect on E. coli, S. aureus and C. albicans.Results: Guided isolation by bioassay gave rise to the isolation and characterisation by nuclear magnetic resonance and mass spectrometry of three compounds: 1 (Bexarotene), 2 (Taspine) and 3 (2-hydroxy-1-naphthaldehyde isonicotinoyl hydrazone). All compounds showed NF-kappa B inhibitory activity with IC50 values of 0.10-0.13, 0.22-0.24 and 3.75-4.78 mu M, respectively, while the positive control, Celastrol, had an IC50 of 7.96 mu M. Likewise, all compounds showed an activating effect of Nrf2 with EC50 values of 5.34-5.43, 163.20-169.20 and 300.82-315.56 nM, respectively, while the positive control, CDDO-Me, had an EC50 of 0.11 nM. In addition, concerning the pro-proliferative activity, compound 1 (IC50 = 8.62-8.71 nM) showed a capacity of 100%, compound 2 (IC50 = 166-171 nM) showed a capacity of 75%, and compound 3 (IC50 = 469-486 nM) showed a capacity of 65%, while FSB 10% (positive control) had a pro-proliferative activity of 100% in the NIH3T3 cell lines (fibroblasts) and HaCaT (keratinocytes). Finally, all the compounds showed antimicrobial activity with MIC values of 0.12-0.16, 0.31-0.39 and 3.96-3.99 mu M, respectively, in S. aureus, E. coli and C. albicans strains, while the positive control, Ofloxacin, had a MIC of 27.65 mu M.Conclusion: This study managed to isolate, for the first time, three compounds (Bexarotene, Taspine and 2-hydroxy-1-naphthaldehyde isonicotinoyl hydrazone) from the resin of D. draco, with anti-inflammatory, and pro proliferative as well as antimicrobial activities.