A strategy for discovering biologically active compounds with high probability in traditional Chinese herb remedies: An application of Saiboku-To in bronchial asthma

Homma, Masato; Oka, Kitaro; Yamada, Tadashi; Niitsuma, Tomoyuki; Ihto, Hisao; Takahashi, Noriyuki

doi:10.1016/0003-2697(92)90225-v

Cited by 83 publications

(51 citation statements)

References 17 publications

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“…However, the biologically active substances and the therapeutic mechanisms of most TCMs are still unclear due to the complexity of the chemical compositions of TCMs. Serum pharmacochemistry is an efficient tool for screening of the potentially active constituents in TCMs (Homma et al, 1992;Huang et al, 2004;Pan & Chen, 2006). Calycosin-7-glucoside, sennoside A, aloeemodin and rhein were detected as the predominant components in rat serum and were investigated in our current study.…”

Section: Discussionmentioning

confidence: 99%

Bioactivities and serum pharmacochemistry ofQi-Wei-Xiao-Yan-Tang

Liu

Peng

et al. 2013

Pharmaceutical Biology

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Context: Qi-Wei-Xiao-Yan-Tang (XYT), composed of Radix et Rhizoma Rhei, Radix Astragali, Radix Wikstroemiae Indicae, Fructus Ligustri Lucidi, Poria and Radix Glycyrrhizae, has been widely used as an anti-inflammatory drug.Objective: The present study investigated the anti-inflammatory, antibacterial effects and serum pharmacochemistry of XYT. Methods: The dimethylbenzene-induced inflammation test, the acetic acid-induced vascular permeability test and the carrageenan-induced paw edema test were used to evaluate the antiinflammatory activity of XYT (200, 100 and 50 mg/kg); minimal inhibitory concentration (MIC). Minimal bactericidal concentration (MBC) tests were used to evaluate the antibacterial activity of XYT. Additionally, serum pharmacochemistry was performed to study the biologically active substances. Results: All the tests for anti-inflammatory effects were shown active with these test systems; the anti-inflammatory effects at doses of 100 and 200 mg/kg were significant (p50.05); MIC and MBC tests indicated that XYT showed a broader antimicrobial spectrum and stronger toxicity to the tested microbes. Additionally, calycosin-7-glucoside, sennoside A, aloeemodin and rhein were detected as the predominant components in rat serum which may play the key role in the anti-inflammatory activities of XYT. Conclusions: This is the first report of the pharmacological activities and serum pharmacochemistry of XYT, and the first evidence of anti-inflammatory and antimicrobial properties of the extracts of XYT. The results of our work demonstrated that XYT has significant antiinflammatory and antibacterial properties, and calycosin-7-glucoside, sennoside A aloeemodin and rhein may be the biologically active substances of XYT. XYT can be utilized as an effective and safe disease preventive or therapeutic agent.

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Section: Discussionmentioning

confidence: 99%

Bioactivities and serum pharmacochemistry ofQi-Wei-Xiao-Yan-Tang

Liu

Peng

et al. 2013

Pharmaceutical Biology

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“…Liquiritigenin was isolated from Glycyrrhiza glabra. 7) Davidigenin was synthesized by hydrogenation of isoliquiritigenin. 8 Peripheral Blood Mononuclear Cell Culture PBMCs were separated from heparinized venous blood collected from healthy volunteers, as described previously.…”

Section: Methodsmentioning

confidence: 99%

“…6) They include medicarpin and liquiritigenin derived from Glycyrrhiza glabra; baicalin, baicalein, oroxylin A and wogonin from Scutellaria baicalensis; and davidigenin, a hydrogenated metabolite of liquiritigenin. Since these compounds are actually absorbed into the body and excreted in the urine as free and glucuronide conjugate forms, 7) we hypothesized that they would play an important role for the clinical effects of TJ-9. Therefore, in the current study, we investigated the effects of these 7 compounds and IFN-a on inducing apoptosis in human lung fibroblasts and peripheral Shosaiko-to is a Kampo medicine used for the treatment of chronic hepatitis in Japan.…”

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confidence: 99%

Induction of Apoptosis in Human Lung Fibroblasts and Peripheral Lymphocytes in Vitro by Shosaiko-to Derived Phenolic Metabolites.

Liu

Tanaka

Horigome

et al. 2002

Biological & Pharmaceutical Bulletin

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Shosaiko-to (TJ-9), a drug-extract preparation comprised of 7 kinds of herbal components, is one of the most commonly used Kampo medicines being mainly indicated for chronic liver injury in Japan. Recently, over 200 cases of interstitial pneumonia have been reported resulting from TJ-9 therapy.2,3) The cases of interstitial pneumonia have been noted to increase when treated with interferon (IFN)-a and TJ-9 at the same time.4) Accordingly, the combination has been contraindicated in Japan since 1994; however, the mechanisms of interstitial pneumonia induced by TJ-9 and IFN-a are not fully understood. It was observed that TJ-9 and IFN-a inhibited the proliferation of lung fibroblasts and increased the production of interleukin-6 (IL-6) by fibroblasts from healthy subjects and patients with idiopathic pulmonary fibrosis (IPF) in vitro.5) Although interstitial pneumonia induced by TJ-9 and/or IFN-a has been suggested to be caused by an allergic-immunological mechanism rather than toxicity, 4) other possible explanations remain to be investigated.Identification of the biologically active compounds might be a solution in clarifying the serious side effect of this crude drug. As possible candidates, 7 phenolic compounds have been found in human urine after administration of TJ-9 (Fig. 1). 6) They include medicarpin and liquiritigenin derived from Glycyrrhiza glabra; baicalin, baicalein, oroxylin A and wogonin from Scutellaria baicalensis; and davidigenin, a hydrogenated metabolite of liquiritigenin. Since these compounds are actually absorbed into the body and excreted in the urine as free and glucuronide conjugate forms, 7) we hypothesized that they would play an important role for the clinical effects of TJ-9. Therefore, in the current study, we investigated the effects of these 7 compounds and IFN-a on inducing apoptosis in human lung fibroblasts and peripheral Shosaiko-to is a Kampo medicine used for the treatment of chronic hepatitis in Japan. Lately, over 200 cases of interstitial pneumonia have been reported resulting from Shosaiko-to therapy, and the number of cases increased when patients were administrated interferon (IFN)-a a at the same time. However, the mechanisms of this Shosaiko-to implicated interstitial pneumonia are not fully understood. In this study, we examined by flow cytometry analysis the in vitro effects of 7 phenolic compounds (lignans and flavonoids), which were detected from human urine after administration of Shosaiko-to, and IFN-a a on inducing apoptosis in human lung fibroblasts and peripheral blood mononuclear cells (PBMCs). Among the 7 compounds, baicalein and medicarpin (10 m mg/ml) showed significant apoptosis-inducing effects on human PBMCs. In human lung fibroblasts, medicarpin exhibited a significantly higher activity to induce apoptosis compared to the control, and the percentage of cells undergoing apoptosis showed time-and dose-dependent increases. Baicalein (0.1 and 1 m mg/ml), liquiritigenin (10 m mg/ml) and davidigenin (10 m mg/ml) also showed significant effects after 96 h...

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“…(2) The components of Chinese medicines is very complicated, many inactive compounds interfere the in vivo experiment results so that the authentic evaluation for efficacy is very difficult. In 1988 and 1992, Homma et al [6] proposed serum pharmacological screening strategy based on hypothesis that the active compounds should appear in blood and urine with appropriate concentrations and urinary excretion rates after the administration of medicines which can be subdivided into serum pharmacology and serum pharmacochemistry. The schematic of method is illustrated in Fig.…”

Section: Pharmacological Screening In Biofluidsmentioning

confidence: 99%