Screening, Characterization and Evaluation of Mangiferin Polymorphs

doi:10.1007/s13659-020-00247-z

应用天然产物 ›› 2020, Vol. 10 ›› Issue (4): 187-200.DOI: 10.1007/s13659-020-00247-z

• ORIGINAL ARTICLES • 上一篇下一篇

Screening, Characterization and Evaluation of Mangiferin Polymorphs

Shiying Yang¹, Qi Zhou¹, Baoxi Zhang¹, Li Zhang¹, Dezhi Yang¹, Haiguang Yang², Guanhua Du², Yang Lu¹

1 Beijing Key Laboratory of Polymorphic Drugs, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China;
2 Beijing Key Laboratory of Drug Targets and Screening Research, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China

收稿日期:2020-04-14 修回日期:2020-05-21 出版日期:2020-08-24 发布日期:2020-08-19
通讯作者: Guanhua Du, Yang Lu
基金资助:
The authors thank the financial support from Key National Research and Development Programmes (Grant No.2016YFC1000905), the Drug Innovation Major Project (Grant No. 2018ZX09711001-001-013), the National Natural Science Foundation of China (Grant No. 81703473), the Drug Innovation Major Project (Grant No. 2018ZX09711001-010, 2017ZX09101001003), and CAMS Innovation Found for Medical Sciences (Grant No. 2016-I2M-1-007).

Screening, Characterization and Evaluation of Mangiferin Polymorphs

Shiying Yang¹, Qi Zhou¹, Baoxi Zhang¹, Li Zhang¹, Dezhi Yang¹, Haiguang Yang², Guanhua Du², Yang Lu¹

1 Beijing Key Laboratory of Polymorphic Drugs, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China;
2 Beijing Key Laboratory of Drug Targets and Screening Research, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China

Received:2020-04-14 Revised:2020-05-21 Online:2020-08-24 Published:2020-08-19
Contact: Guanhua Du, Yang Lu
Supported by:
The authors thank the financial support from Key National Research and Development Programmes (Grant No.2016YFC1000905), the Drug Innovation Major Project (Grant No. 2018ZX09711001-001-013), the National Natural Science Foundation of China (Grant No. 81703473), the Drug Innovation Major Project (Grant No. 2018ZX09711001-010, 2017ZX09101001003), and CAMS Innovation Found for Medical Sciences (Grant No. 2016-I2M-1-007).

摘要/Abstract

摘要： Mangiferin is a compound with many pharmacological activities and exists in many natural products. Anhydrous and hydrate of mangiferin have been reported separately in two literatures, but the polymorphism of this compound has not been realized until this paper. In this study, polymorph screening of mangiferin has been carried out and five forms have been obtained including three new forms never reported. Several solid state characterization methods, such as powder X-ray diffraction, differential scanning calorimetry and thermogravimetry, are used to identify and characterize all of mangiferin forms. The comparison of the crystallographic data and hirshfeld surface analysis were first reported for mangiferin anhydrous and hydrate. Furthermore, the studies on stability, transformation and solubility have been undertaken, the results prompt that form V can be used as the dominant polymorph for the development of innovative pharmaceuticals.

关键词: Mangiferin, Polymorph screening, Characterize, Stability, Solubility

Abstract: Mangiferin is a compound with many pharmacological activities and exists in many natural products. Anhydrous and hydrate of mangiferin have been reported separately in two literatures, but the polymorphism of this compound has not been realized until this paper. In this study, polymorph screening of mangiferin has been carried out and five forms have been obtained including three new forms never reported. Several solid state characterization methods, such as powder X-ray diffraction, differential scanning calorimetry and thermogravimetry, are used to identify and characterize all of mangiferin forms. The comparison of the crystallographic data and hirshfeld surface analysis were first reported for mangiferin anhydrous and hydrate. Furthermore, the studies on stability, transformation and solubility have been undertaken, the results prompt that form V can be used as the dominant polymorph for the development of innovative pharmaceuticals.

Key words: Mangiferin, Polymorph screening, Characterize, Stability, Solubility

Shiying Yang, Qi Zhou, Baoxi Zhang, Li Zhang, Dezhi Yang, Haiguang Yang, Guanhua Du, Yang Lu. Screening, Characterization and Evaluation of Mangiferin Polymorphs[J]. 应用天然产物, 2020, 10(4): 187-200.

Shiying Yang, Qi Zhou, Baoxi Zhang, Li Zhang, Dezhi Yang, Haiguang Yang, Guanhua Du, Yang Lu. Screening, Characterization and Evaluation of Mangiferin Polymorphs[J]. Natural Products and Bioprospecting, 2020, 10(4): 187-200.

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Screening, Characterization and Evaluation of Mangiferin Polymorphs

Screening, Characterization and Evaluation of Mangiferin Polymorphs

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