Delving into the Latest Updates on Bergeninum with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target-

Action-

Mechanism-

Therapeutic Areas

Nervous System DiseasesEndocrinology and Metabolic Disease

Active Indication

Diabetic Neuropathies

Inactive Indication-

Originator Organization-

Active Organization

Prince Sattam Bin Abdulaziz University

Inactive Organization-

License Organization-

Drug Highest PhaseApproved

First Approval Date

China (01 Jan 1995)

Regulation-

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Structure/Sequence

Molecular FormulaC14H16O9

InChIKeyYWJXCIXBAKGUKZ-HJJNZUOJSA-N

CAS Registry477-90-7

Photothermo-chemotherapy has shown a synergistic anti-cancer efficiency and can enhance the therapeutic effect of simple chemotherapy. The photothermal conversion characteristics of carriers are vital in photothermal chemotherapy. In this study, we developed functional carbon dots (CDs) as a photothermal agent and carrier to load bergenin (Ber) for simultaneous biological imaging and photo-chemothermal synergistic therapy. CDs were successfully synthesized using a one-step solvothermal method with citric acid and polyethyleneimine in formamide. Surface morphology, chemical composition and structure, luminescent properties, and photothermal properties of synthesized CDs and CDs/Ber were investigated. The CDs (<10 nm) displayed a mono-dispersed state and uniform spherical morphology with a graphite-like structure. Ber was loaded onto CDs by π-π stacking and intermolecular hydrogen bonds, with a high drug loading efficiency of 95.8 %. In vitro release studies verified pH-dependent sustained drug release, with release rates of 37.84 ± 1.67 % (pH 6.5) and 29.19 ± 0.28 % (pH 7.4), which conformed to the Weibull model. The CDs/Ber had excellent photothermal performance, stability, and high conversion efficiency (54.9 %) by non-radiative transitions. The CDs acted as an ideal theranostic and photothermal agent for fluorescence imaging, photothermal imaging, ablation, and necrosis of cancer cells. CDs/Ber exhibited excellent water-solubility, biocompatibility, and passive tumor-targeting capability. Cytotoxicity experiments proved that combined therapy of CDs/Ber induced the highest cell-killing level. The biodistribution and pharmacodynamics experiments of CDs/Ber in the lung tumor model within 14 days post-exposure to one-time near-infrared radiation (NIR) irradiation indicated that CDs prolonged the residence time of Ber in tumor tissues and actualized effective synergistic photothermal chemotherapy, yielding a true "1 + 1 > 2" effect. The results of this study indicated that CDs/Ber had great potential in dual-triggered drug delivery and photothermal-chemotherapy, and acted as an excellent candidate for efficient cancer therapy.

01 Aug 2025·JOURNAL OF MOLECULAR HISTOLOGY

Bergenin exerts anti-cancer activity in hepatocellular carcinoma via the PI3K/Akt/mTOR and MAPK/ERK pathways

Article

Author: Lu, Guangrui ; Wang, Chunrong ; Hu, Jianghong ; Wu, Mengjie ; Zhuang, Xun ; Chen, Zhen ; Chen, Mengjiao ; Ge, Zhenghui ; Zhai, Haoqing

OBJECTIVE:

Hepatocellular carcinoma (HCC) remains a therapeutic challenge with limited treatment options. This study investigated the anti-tumor potential of bergenin, a bioactive acylated iridoid glycoside, against HCC and elucidated its underlying molecular mechanisms.

METHODS:

We systematically evaluated bergenin's effects using: (1) in vitro functional assays including CCK-8 viability, colony formation, TUNEL, flow cytometry, wound healing, and transwell assays; (2) molecular analyses of apoptosis markers (cleaved caspase-3/-9), metastasis-related proteins (MMP-2/-9), and key signaling pathways; and (3) in vivo xenograft models assessing tumor growth inhibition.

RESULTS:

Bergenin demonstrated potent anti-HCC activity through multiple mechanisms: (1) dose-dependently inhibiting cell proliferation and colony formation; (2) inducing apoptosis via caspase-3/-9 activation; (3) suppressing migration and invasion through MMP-2/-9 downregulation; and (4) significantly inhibiting tumor growth in vivo. Mechanistically, bergenin concurrently inhibited both PI3K/Akt/mTOR and MAPK/ERK signaling pathways in vitro and in vivo.

CONCLUSION:

Our findings demonstrate that bergenin exerts anti-HCC effects by simultaneously targeting proliferation, apoptosis, and metastasis through dual inhibition of oncogenic PI3K/Akt/mTOR and MAPK/ERK pathways.

01 Aug 2025·MICROBIAL PATHOGENESIS

Antibacterial activity of a plant natural poly-phenol against zoonotic Streptococcus suis

Article

Author: Yuan, Fangyan ; Zhou, Danna ; Liu, Wei ; Liu, Zewen ; Zhu, JiaJia ; Tian, Haibin ; Li, Chang ; Gao, Ting ; Wu, Qiong ; Li, Lu ; Chen, Mo ; Yang, Keli ; Wang, Yanjun ; Tian, Yongxiang ; Guo, Rui

The increasing emergence and dissemination of multi-drugs resistant bacterial pathogens accelerate the desires for novel antimicrobials. Natural products are great resources for the discovery of antimicrobial compound. In this study, pyrogallol was screened from 25 poly-phenols for its antibacterial activity against multi-drugs resistant Streptococcus suis (S. suis), particularly, pyrogallol had synergistic antimicrobial effect with doxycycline, sulfafurazole and clindamycin, respectively. Pyrogallol showed significant inhibitory effects on bacterial biofilm formation, and caused cell wall and cell membrane injury to S. suis. Furthermore, mechanistic studies demonstrated that pyrogallol might interact with peptidoglycan and decreased the expression of virulence and growth-related genes, such as ftsZ, stK, sly, fbps and luxS. In cell model, pyrogallol protected Nptr cells from S. suis-mediated cell damage. Finally, in mouse model, the pyrogallol and antibiotics combination groups with dosage given in the half could be as effective as antibiotics groups. In summary, these results demonstrated the capacity of pyrogallol serving as a candidate for novel antibiotic alternative and antibiotic adjuvant to circumvent the antibiotics resistance and reduced antibiotic consumption.

100 Deals associated with Bergeninum

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