A patent review of berberine and its derivatives with various pharmacological activities (2016–2020)
Abstract
INTRODUCTION: Berberine (BBR), as one of the outstanding representatives of isoquinoline alkaloids, has been used as an antibacterial drug for a long time in China since ancient times. Currently, a large number of studies have been reported that berberine has a wide spectrum of pharmacological activities, such as anti-tumor, anti-inflammatory, hypoglycemic, hypolipidemic, anti-obesity, and the like. AREAS COVERED: This review systematically discussed important patents on berberine and berberine derivatives in terms of pharmacological activity between 2016 and 2020. These patents were mainly searched through the European Patent Office database and Web of Science. These berberine patents (~41) cover a wide range of applications, mainly including antitumor, anti-inflammatory, antibacterial, anti-metabolic disorder, and other newly reported pharmacological activities. EXPERT OPINION: Berberine is an important lead compound with great potential for optimization in drug development. However, there is a lack of research related to the biomolecular targets of BBR, which directly restricts the development of berberine in the pharmaceutical field. The problems involved with poor bioavailability and cytotoxicity are also worth considering in the development of berberine-based drugs. Accordingly, the increasing number of patents involving biomolecular targets in BBR's patent applications will be published as its related pharmacological mechanisms are further deciphered.
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Berberine has been demonstrated to have the potential effect of hypoglycemia.
“Berberine, the main active component of Rhizoma Coptidis, has been demonstrated to have the potential effect of hypoglycemia.”
From The Effect of Berberine on Metabolic Profiles in Type 2 Diabetic Patients: A Systematic Review and Meta‐Analysis of Randomized Controlled Trials (2021) · cites this paper as [13]
Berberine is an important lead compound with a wide spectrum of pharmacological activities, including antitumor, anti-inflammatory, hypoglycemic, hypolipidemic, and antiobesity effects.
“Among the different alkaloids, berberine is an important lead compound with a wide spectrum of pharmacological activities, including antitumor, anti-inflammatory, hypoglycemic, hypolipidemic, and antiobesity effects [13].”
From The Effect of Berberine on Metabolic Profiles in Type 2 Diabetic Patients: A Systematic Review and Meta‐Analysis of Randomized Controlled Trials (2021) · cites this paper as [13]
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- Authors
- Kong, Y., Li, L., Zhao, L.-G., Yu, P., & Li, D.-D.
- Affiliations
- Nanjing Forestry University (CN)
- Anhui University of Science and Technology (CN)
- Corresponding author
- Zhao, Lin-Guo
- Yu, Pan
- Li, Dong-Dong
- Venue
- Expert Opinion on Therapeutic Patents
- Publisher
- Informa UK Limited
- Published
- 2021-09-17
- Volume
- 32
- Issue
- 2
- Pages
- 211-223
- ISSN
- 1354-3776 (ISSN-L)
- 1744-7674
- OpenAlex
- W3196603633
- Cited by
- 52
- References
- 80
- Citations by year
- 2026: 6 · 2025: 20 · 2024: 11 · 2023: 10 · 2022: 4 · 2021: 1
- FWCI
- 0.82
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Expert Opinion on Therapeutic Patents (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Project for Young Teachers of Nanjing Forestry University
- Topics
- Health Sciences › Medicine › Pharmacology › Berberine and alkaloids research
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Synthesis and Biological Activity
- Health Sciences › Medicine › Complementary and alternative medicine › Traditional Chinese Medicine Analysis
- Keywords
- berberine, berberine derivatives, isoquinoline alkaloids, patent analysis, anticancer activity, anti-inflammatory activity, antibacterial activity, anti-obesity, hypoglycemic activity, hypolipidemic activity, bioavailability, cytotoxicity, drug development
- MeSH terms
- Anti-Inflammatory Agents, Berberine, Biological Availability, Humans, Hypoglycemic Agents, Patents as Topic
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