Herbal Medicine, Hachimi-jio-gan, and Its Component Cinnamomi Cortex Activate the Peroxisome Proliferator-activated Receptor Alpha in Renal Cells

• Published in: Endocrine Journal Vol. 55; no. 3; pp. 529 - 533
• Main Authors: MONDEN, Tsuyoshi, HOSOYA, Takeshi, NAKAJIMA, Yasuyo, KISHI, Mikiko, SATOH, Teturou, HASHIMOTO, Koshi, KASAI, Kikuo, YAMADA, Masanobu, MORI, Masatomo
• Format: Journal Article
• Language: English
• Published: Japan The Japan Endocrine Society 2008
• Subjects: Animals; Cells, Cultured; Cercopithecus aethiops; cinnamomi cortex; COS Cells; Drugs, Chinese Herbal - chemistry; Drugs, Chinese Herbal - pharmacology; Hachimi-jio-gan; Humans; Kidney - drug effects; Kidney - metabolism; Ligands; Organ Specificity - drug effects; Plant Extracts - pharmacology; PPAR alpha - agonists; PPAR alpha - genetics; PPAR alpha - metabolism; PPARα; Transcriptional Activation - drug effects; Transfection
• ISSN: 0918-8959; 1348-4540
• DOI: 10.1507/endocrj.K07E-101

Hachimi-jio-gan is widely used to improve several disorders associated with diabetes, but its mechanism remains poorly understood. In an attempt to clarify the mechanism of Hachimi-jio-gan, we investigated the effects of this herbal medicine and its components in transfection studies of CV1 cells, especially nuclear receptor-mediated actions. One half (0.5) mg/ml of Hachimi-jio-gan activated peroxisome proliferator-activated receptor (PPARα), mediating the activation by 3.1-fold on DR1 response elements; however, it did not affect PPARγ, thyroid hormone receptor, androgen receptor, estrogen receptor or RXR. In addition, this activation was observed in a dose-dependent manner. Next, to determine which components of Hachimi-jio-gan activate PPARα-mediated transcription, 8 of its components (rehmanniae radix, orni fructus, dioscoreae rhizoma, alismatis rhizoma, hoelen, moutan cortex, cinnamomi cortex, aconiti) were tested. Only cinnamomi cortex (1.0 mg/ml) increased PPARα-mediated transcription by 4.1-fold, and this activation was specific for PPAR α, and not for other nuclear receptors. Moreover, this PPARα-related activation by cinnamomi cortex is specifically observed in renal cells. Taken together, these findings indicate that Hachimi-jio-gan and cinnamomi cortex may have a pharmacological effect through the target site for PPARα.