Zhao Min, Xu Wan-Feng, Shen Han-Yuan, Shen Pei-Qiang, Zhang Jun, Wang Dan-Dan, Xu Han, Wang Hong, Yan Ting-Ting, Wang Lin, Hao Hai-Ping, Wang Guang-Ji, Cao Li-Juan
State Key Laboratory of Natural Medicines, Key Lab of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing, Tongjiaxiang 24, Nanjing, 21009, China.
ChiaTai Qingchunbao Pharmaceutical Co. Ltd., Xixi Road 551, Xihu District, Hangzhou, China.
J Pharm Biomed Anal. 2017 May 10;138:134-141. doi: 10.1016/j.jpba.2017.02.013. Epub 2017 Feb 7.
Ophiopogon japonicus (Linn. f.) Ker-Gawl (O. japonicas), mainly cultivated in Sichuan and Zhejiang province in China, has different bioactive components and therefore their pharmacological activities. To explain the different clinical efficacy of O. japonicas derived preparations, herein we report differences of pharmacological activities between Sichuan and Zhejiang O. japonicas and behind them the exact differences of bioactive components. Based on a LC/MS-IT-TOF method, the differences of bioactive components between Sichuan and Zhejiang O. japonicas extracts were analyzed and respective characteristic components were picked out. We determined 39 ophiopogonones and 71 ophiopogonins compounds in Sichuan and Zhejiang O. japonicas extracts and found the contents of these compositions have several times difference. Evidenced by experimental data of pharmacological activities in inhibiting cardiomyocyte damage induced by HO, mouse macrophage cell inflammation induced by lipopolysaccharide and cytotoxicity in vitro, Zhejiang O. japonicas extract had a stronger antioxidant and anti-inflammatory capacity than Sichuan O. japonicas extract, and the two O. japonicas extracts exhibited selective cytotoxicity on different cancer cell lines in vitro. These data shed light on the links between bioactive components and pharmacological activities of O. japonicas derived preparations. Thus, geographical origin of O. japonicas should be considered to be a key factor in efficacy studies and further clinical application.
麦冬（Ophiopogon japonicus (Linn. f.) Ker-Gawl，即O. japonicas）主要在中国四川省和浙江省种植，具有不同的生物活性成分，因而具有不同的药理活性。为了解释麦冬衍生制剂不同的临床疗效，在此我们报告四川麦冬和浙江麦冬药理活性的差异以及其背后生物活性成分的确切差异。基于液相色谱/质谱-离子阱-飞行时间质谱（LC/MS-IT-TOF）方法，分析了四川麦冬和浙江麦冬提取物中生物活性成分的差异，并挑选出各自的特征成分。我们在四川麦冬和浙江麦冬提取物中测定了39种麦冬酮类化合物和71种麦冬皂苷类化合物，发现这些成分的含量存在数倍差异。通过抑制过氧化氢（HO）诱导的心肌细胞损伤、脂多糖诱导的小鼠巨噬细胞炎症以及体外细胞毒性的药理活性实验数据证明，浙江麦冬提取物比四川麦冬提取物具有更强的抗氧化和抗炎能力，并且两种麦冬提取物在体外对不同癌细胞系表现出选择性细胞毒性。这些数据揭示了麦冬衍生制剂生物活性成分与药理活性之间的联系。因此，在疗效研究和进一步的临床应用中，应考虑麦冬的地理来源是一个关键因素。
