Fujii Airi, Onishi Saki, Watanabe Nodoka, Kajimura Mizuki, Ito Kentaro, Minamisaka Keita, Nishidono Yuto, Shirako Saki, Ikeya Yukinobu, Nishizawa Mikio
Department of Medical Biosciences, Faculty of Life Sciences, Ritsumeikan University, Kusatsu 525-8577, Shiga, Japan.
Research Organization of Science and Technology, Ritsumeikan University, Kusatsu 525-8577, Shiga, Japan.
Molecules. 2025 Jan 19;30(2):416. doi: 10.3390/molecules30020416.
Traditional Japanese medicines, i.e., Kampo medicines, consist of crude drugs (mostly plants) that have empirical pharmacological functions ('' in Japanese), such as clearing heat. Crude drugs with cold properties, such as bark, have the empirical function of clearing heat as they cool the body. Because we found that anti-inflammatory compounds were present in several crude drugs for clearing heat, it is speculated that the empirical function of clearing heat may be linked to anti-inflammatory activities. When 10 typical crude drugs were selected from 22 herbal crude drugs for clearing heat, we identified anti-inflammatory compounds in five crude drugs, including bark. In this study, the other crude drugs were extracted and partitioned with ethyl acetate (EtOAc) and -butanol to obtain three crude fractions. All the EtOAc-soluble fractions, except that from fruits, inhibited interleukin (IL)-1β-induced nitric oxide (NO) production in primary-cultured rat hepatocytes. Anti-inflammatory compounds were identified from these EtOAc-soluble fractions: baicalein from roots, (-)-nyasol from rhizomes, and loniflavone from leaves and stems. (+)-Phillygenin was purified from fruits by removing cytotoxic oleanolic and betulinic acids. These compounds suppressed the production of NO and cytokines in hepatocytes. Anti-inflammatory compounds were not purified from the EtOAc-soluble fraction of roots because of their low abundance. Collectively, these findings indicate that anti-inflammatory compounds are present in all 10 crude drugs for clearing heat, confirming that these anti-inflammatory compounds in crude drugs provide the empirical functions for clearing heat. Other empirical functions of Kampo medicine can also be explained by modern pharmacological activities.
传统日本药物，即汉方药物，由具有实证药理功能（日语为“ ”）的生药（大多为植物）组成，比如清热。具有寒性的生药，如 树皮，因其能使身体凉爽而具有清热的实证功能。因为我们发现几种清热生药中存在抗炎化合物，所以推测清热的实证功能可能与抗炎活性有关。当从22种清热草药生药中挑选出10种典型生药时，我们在包括 树皮在内的5种生药中鉴定出了抗炎化合物。在本研究中，对其他生药用乙酸乙酯（EtOAc）和正丁醇进行提取和分配，以获得三种粗提物。除了 果实的EtOAc可溶部分外，所有其他EtOAc可溶部分均抑制原代培养大鼠肝细胞中白细胞介素（IL）-1β诱导的一氧化氮（NO）生成。从这些EtOAc可溶部分中鉴定出了抗炎化合物： 根中的黄芩素、 根茎中的（-）-尼亚索、 叶和茎中的独活黄酮。通过去除具有细胞毒性的齐墩果酸和桦木酸，从 果实中纯化出了（+）-费城尼亭。这些化合物抑制了肝细胞中NO和细胞因子的生成。由于 根的EtOAc可溶部分中抗炎化合物含量低，未从中纯化出抗炎化合物。总的来说，这些发现表明所有10种清热生药中都存在抗炎化合物，证实了生药中的这些抗炎化合物提供了清热的实证功能。汉方药物的其他实证功能也可以用现代药理活性来解释。
