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Chi X.-Y.,Guangdong Pharmaceutical University | Fu Y.-M.,Sinopharm Group Guangdong Medi world Pharmaceutical Co. | Cui Y.-X.,Guangdong Pharmaceutical University | Zhang S.,Guangdong Pharmaceutical University | Deng H.,Guangdong Pharmaceutical University
Chinese Traditional and Herbal Drugs | Year: 2016

Objective: To explore the relationship between chemical constituents of Isatidis Radix (IR)and the inhibition of bioactivity of neuraminidase (NA)on influenza virus in vitro. Methods: To establish the chemical fingerprints of IR extraction from different producing areas and determine the contents of common peaks by UPLC. To determine the activity of NA on influenza virus tested with IR by Kit. To analyze the correlation of the chemical information and biological effect by mathematical statistics methods such as grey correlation analysis and one-factor analysis. Results: The chemical contents and biological effect detection varied markedly in the products from different regions and by extracting methods. The result of comprehensive analysis showed that uridine and (R, S)-goitrin of common components in UPLC-fingerprints related with the inhibition of bioactivity of NA on influenza virus, and the content of (R, S)-goitrin was correlated significantly to the activity of NA. Conclusion: Based on the biological assay of NA on influenza virus, the correlation of the content of chemical components and biological effect is verified preliminarily, with a view to provide a more reliable data and reference for the selection and extraction of antiviral active ingredients fromIR. © 2016, Editorial Office of Chinese Traditional and Herbal Drugs. All right reserved.

Ning X.,Guangdong Pharmaceutical University | Yang Y.,Jinan University | Deng H.,Guangdong Pharmaceutical University | Zhang Q.,Jinan University | And 5 more authors.
Steroids | Year: 2017

17β-Hydroxysteroid dehydrogenase type 3 (17β-HSD3) is expressed almost exclusively in the testes and specifically converts the weak androgenic androstenedione to active testosterone (T) in the presence of NADPH. Additionally, studies have demonstrated that 17β-HSD3 is over-expressed in hormone-dependent prostate cancer. T, which interacts with the androgen receptor (AR), eventually stimulates the growth of prostate cancer cells. Defects in T synthesis or action impair the development of the male phenotype during embryogenesis and cause the autosomal recessive disorder male pseudohermaphroditism. Affected individuals are often born with female-appearing external genitalia and are reared as females. Since 17β-HSD3 plays a central role in T production, it has been recognized as a promising therapeutic target to reduce the circulating level of androgens and to suppress androgen-sensitive tumor proliferation. In recent decades, improvements have been made in the development of 17β-HSD3 inhibitors. Herein, we give an overview of the main structure and function of human 17β-HSD3 and summarize steroidal and non-steroidal inhibitors of 17β-HSD3, which can be a potential target for prostate cancer. © 2017 Elsevier Inc.

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