108275-17-8Relevant articles and documents
Synthesis, biological evaluation and molecular modeling of novel triazole-containing berberine derivatives as acetylcholinesterase and β-amyloid aggregation inhibitors
Shi, Anding,Huang, Ling,Lu, Chuanjun,He, Feng,Li, Xingshu
, p. 2298 - 2305 (2011)
A series of novel triazole-containing berberine derivatives were synthesized via the azide-alkyne cycloaddition reaction. Their biological activity as inhibitors of both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) were evaluated. Among t
A novel berberine-based colorimetric and fluorimetric probe for hydrazine detection
Ruan, Shutang,Gao, Yu,Wang, Yunyun,Li, Mingxin,Yang, Haiyan,Song, Jie,Wang, Zhonglong,Wang, Shifa
, p. 15752 - 15757 (2020)
Hydrazine in water and soil has caused serious diseases that threaten human health. It is critical to develop a simple and effective method for hydrazine detection. In this work, a simple fluorescent probe (BP) for hydrazine detection was synthesized from the isoquinoline alkaloid berberine. The probe has a short synthesis route (2 steps), low detection limit (1.37 μM), excellent fluorescence properties, and convenient naked-eye detection. In addition, BP displayed excellent selectivity and specificity over other metal ions, anions, and amines. Moreover, BP was also successfully used to detect hydrazine gas at different concentrations. This journal is
Triple stimuli-responsive supramolecular nanoassembly with mitochondrial targetability for chemophotothermal therapy
Cheng, Yu,Ji, Yuanhui,Tong, Jiwei
, p. 35 - 49 (2020)
Mitochondria play crucial roles in a variety of cellular physiological processes, mitochondria-accumulating drug delivery has drawn pronounced attention in the field of cancer theranostics. Camptothecin (CPT) is a DNA Topoisomerase I inhibitor and exerts a broad-spectrum anticancer profile. Berberine (BBR) is able to perferably enter into cancer cell mitochondria and trigger the cell apoptosis. In this work, CPT and BBR were combined together (CPT-ss-BBR) through GSH-responsible disulfide bond, and then co-assembled with photosensitizer indocyanine green (ICG) into nanodrugs (CPT-ss-BBR/ICG NPs), which was driven through hydrophobic, π-π stacking and especially, electrostatic interactions of anions and cations as found by molecular dynamics simulations and quantum chemistry calculations. Our developed nanodrugs displayed an average size of ~168 nm and showed exceptional instability by irradiation presence, acid condition and high concentration of GSH, thereby eliciting the rapid disassembly and accelerating drug release. The better therapy effect of CPT-ss-BBR/ICG NPs on A549 cells might be attributed to triply stimuli-responsive rapid disassembly, preferable accumulation into mitochondria and combined chemotherapy and photothermal therapy, all of which directly rendered the notable loss of mitochondria membrane potential, high level of reactive oxygen species in cancer cells, accelerated the apoptosis of cancer cells and repressed the growth of tumors.
Synthesis of 9-O-glycosyl-berberine derivatives and bioavailability evaluation
Chen, Zhu,Ye, Xiaoli,Yi, Jun,Chen, Xin,Li, Xuegang
, p. 1641 - 1646 (2012)
To increase the bioavailability of berberine, three new 9-O-glycosyl-berberine derivatives, 9-O-glucosyl-(4a), 9-O-arabinosyl-(4b), and 9-O-erythrol-(4c) were obtained and confirmed by UV, 1HNMR, 13CNMR, and MS. The pharmacokinetic profiles of these synthetic compounds have been evaluated compared with berberine (1) and 9-O-alkyl-berberine (5) derivatives, which showed that maximum concentration (Cmax) and area under concentration-time curve (AUC) of 9-O-glycosyl-berberine increased dramatically. The results indicated that hydrophilic modification could significantly improve the bioavailability of berberine; 9-O-glycosyl-berberine might be a promising prodrug. Springer Science+Business Media, LLC 2011.
Hypolipidemic Berberine Derivatives with a Reduced Aromatic Ring C
Nechepurenko,Boyarskikh,Khvostov,Baev,Komarova,Filipenko,Tolstikova,Salakhutdinov
, p. 916 - 922 (2015)
A series of aromatic and reduced berberine derivatives were synthesized. Their hypocholesterolemic activity was studied in vitro and in vivo. As a rule, berberine derivatives containing a reduced ring C were more capable of increasing the LDL receptor gene expression than the corresponding aromatic derivatives. Tests using a Triton WR1339-induced hypercholesterolemia model showed that 9-O-tosyltetrahydroberberine and 12-bromotetrahydroberberine possessed pronounced hypocholesterolemic activity and reduced the total cholesterol level by 33 and 27%; the triglyceride level, by 25 and 26%, respectively.
Syntheses and absorption spectra of some compounds with the berbine structure
Pavelka,Kovar
, p. 3654 - 3669 (1976)
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Antimicrobial activity of 9-O-acyl- and 9-O-benzoyl-substituted berberrubines
Hong, Sa Weon,Kim, Sung Han,Jeun, Jung Ae,Lee, Sang Jun,Kim, Sung Uk,Kim, Jung Han
, p. 361 - 363 (2000)
In the course of a structure-activity relationship study on berberrubine derivatives, a series of compounds bearing 9-O-acyl- (4-6) and 9-O-benzoyl- (7) substituents was synthesized with the expectation of increasing the antimicrobial activity. One of the
Antimicrobial Activity of 9-O-Acyl- and 9-O-Alkylberberrubine Derivatives
Kim, Sung Han,Lee, Sang Jun,Lee, Joo Hyoung,Sun, Won Suck,Kim, Jung Han
, p. 277 - 281 (2002)
For the structure-activity relationship study on berberrubine derivatives, a series of compounds bearing 9-O-acyl- and 9-O-alkyl-substituents were synthesized and tested for antimicrobial activity against Gram-positive, Gram-negative bacteria and fungi. O
A class of intestinal lysis type co-drugs and their preparation and use
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Paragraph 0150-0151; 0181-0184, (2022/01/20)
The present invention relates to a class of intestinal cleavage type co-drugs (Codrug) and preparation and use thereof, in particular, the present invention provides a co-drug compound as shown in formula I. The present invention further provides a method