Key Laboratory of Marine Drugs, The Ministry of Education of China, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China.
Laboratory for Marine Drugs and Bioproducts, Qingdao National Laboratory for Marine Science and Technology, Qingdao 266071, China.
Molecules. 2018 Jun 5;23(6):1361. doi: 10.3390/molecules23061361.
has been traditionally used as a medicinal herb because of its health-promoting effects, such as its hepatoprotective and antioxidant activities. In the present study, the petroleum ether fraction, ethyl acetate fraction, -butanol fraction, and aqueous fraction were successively obtained from the ethanol extract of . Two fractions, ethyl acetate fraction and -butanol fraction, were found to display hepatoprotective and antioxidant activities. Further chemical investigation of the active fractions led to the isolation of its main constituents, including 11 flavonoids (⁻) and 8 indole alkaloids (⁻). There were 9 flavonoids (⁻) that were obtained from the ethyl acetate fraction, and 2 flavonoids ( and ) and 8 alkaloids (⁻) from the -butanol fraction. Compounds ⁻ and ⁻ were isolated for the first time from , and , , , , and were obtained from the genus initially. Subsequently, the isolated compounds were evaluated for their in vitro hepatoprotective effects on the human normal hepatocyte cell line L-O2 injured by d-galactosamine and radical scavenging activities against 1,1-diphenyl-2-picrylhydrazyl (DPPH). The flavonoids (-)-epigallocatechin () and (-)-epicatechin () exhibited prominent hepatoprotective activities with higher cell viability values (65.53% and 62.40% at 10 μM·mL, respectively) than the positive control, silymarin (61.85% at 10 μM·mL). In addition, compared with the positive control of vitamin C (IC: 5.14 μg·mL), (-)-gallocatechin () and (-)-epigallocatechin () exhibited stronger antioxidant activities with IC values of 3.80 and 3.97 μg·mL, respectively. Furthermore, the total flavonoids from were characterized using a high-performance liquid chromatography-linear ion trap quadrupole-Orbitrap-mass spectrometry (HPLC-LTQ-Orbitrap-MS). In total, 34 flavonoids were tentatively identified, which had not been previously reported from . In addition, we performed a semi-quantitative analysis of the isolated flavonoids. The contents of compounds ⁻ were 3.88, 17.73, 140.35, 41.93, 27.80, 4.34, 0.01, 0.20, 9.67, 795.85, and 5.23 μg·g, respectively. In conclusion, this study revealed that the flavonoids that were isolated from showed hepatoprotective and antioxidant activities, indicating that, besides alkaloids, the flavonoids should be the potential pharmacodynamic ingredients that are responsible for the hepatoprotective and antioxidant activities of .
它因具有促进健康的作用,如保肝和抗氧化活性,一直被用作药用植物。在本研究中,从 的乙醇提取物中依次得到石油醚部分、乙酸乙酯部分、正丁醇部分和水部分。发现乙酸乙酯部分和正丁醇部分具有保肝和抗氧化活性。对活性部分进行进一步的化学研究,分离得到其主要成分,包括 11 种黄酮类化合物(⁻)和 8 种吲哚生物碱(⁻)。从乙酸乙酯部分得到 9 种黄酮类化合物(⁻),从正丁醇部分得到 2 种黄酮类化合物(和)和 8 种生物碱(⁻)。化合物 ⁻ 和 ⁻ 首次从 中分离得到, 和 首次从 属中分离得到。随后,对分离得到的化合物进行了体外对 D-半乳糖胺损伤的人正常肝细胞系 L-O2 的保肝作用评价和对 1,1-二苯基-2-苦基肼(DPPH)自由基清除活性评价。黄酮类化合物 (-)-表没食子儿茶素()和 (-)-表儿茶素()表现出显著的保肝活性,细胞活力值高于阳性对照水飞蓟素(分别在 10 μM·mL 时为 65.53%和 62.40%)。此外,与阳性对照维生素 C(IC:5.14 μg·mL)相比,(-)-没食子儿茶素()和 (-)-表没食子儿茶素()表现出更强的抗氧化活性,IC 值分别为 3.80 和 3.97 μg·mL。此外,利用高效液相色谱-线性离子阱四极杆-Orbitrap 质谱(HPLC-LTQ-Orbitrap-MS)对 的总黄酮进行了表征。总共鉴定出 34 种黄酮类化合物,这些化合物以前从未从 中报道过。此外,我们对分离得到的黄酮类化合物进行了半定量分析。化合物 ⁻ 的含量分别为 3.88、17.73、140.35、41.93、27.80、4.34、0.01、0.20、9.67、795.85 和 5.23 μg·g。综上所述,本研究表明,从 中分离得到的黄酮类化合物具有保肝和抗氧化活性,表明除生物碱外,黄酮类化合物可能是具有保肝和抗氧化活性的潜在药效成分。