MOLECULES
·
2024
·Vol. 29
·期 1
·273
·
IF 4.2
Jinsheng Li,Xueli Hou,Jinlong Xiao,Li Zhu,Yujie Deng,Ziyi Li,Zijian Zhao,Zhenghong Luo,Hao Wei
The isoquinoline alkaloid berberine, derived from Coptidis rhizoma, exhibits antibacterial, hypoglycemic, and anti-inflammatory properties. Canagliflozin is a sodium–glucose cotransporter 2 (SGLT2) inhibitor. We synthesized compounds B9OC and B9OBU by conjugating canagliflozin and n-butane at the C9 position of berberine, aiming to develop antimicrobial agents for combating bacterial infections worldwide. We utilized clinically prevalent pathogenic bacteria, namelyStaphylococcus aureus,Escherichia coli, andPseudomonas aeruginosa, to investigate the antibacterial efficacy of B9OC. This was accomplished through the determination of the MIC80values, analysis of bacterial growth curves, evaluation of biofilm formation using crystal violet staining, assessment of impact on bacterial proteins via SDS-PAGE analysis, and observation of alterations in bacterial morphology utilizing field emission scanning electron microscopy. Meanwhile, the ADMET of compound B9OC was predicted using a computer-aided method. The findings revealed that B9OC exhibited lower minimal inhibitory concentrations against all three bacteria compared to berberine alone or in combination with canagliflozin. The minimal inhibitory concentrations (MICs) of B9OC against the three experimental strains were determined to be 0.035, 0.258, and 0.331 mM. However, B9OBu exhibited a lower level of antimicrobial activity compared to berberine. The compound B9OC exhibits a broad spectrum of antibacterial activity by disrupting the integrity of bacterial cell walls, leading to cellular rupture and the subsequent degradation of intracellular proteins.
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JOURNAL OF COLLOID AND INTERFACE SCIENCE
·
2025
·
IF 9.7
He Feng,Yang-Jian Hong,Qi-Qi Zheng,Jia-Ming Ge,Hong-Wei Cheng,Yu-Peng Liu,Jie Deng,Qing-Lin Li,Song-Nan Qu
Precise delivery of antitumor drugs has become a research focus in cancer treatment. Herein, we developed a bovine serum albumin (BSA) modified carbon dots (CDs) and berberine (BBR) composite for improved intravenous BBR delivery. The surface-negatively charged CDs can associate with positively charged BBR through electrostatic interactions, resulting in CDs and BBR composite (BBR@CDs). BBR@CDs can be further stabilized by modification with BSA, resulting in enlarged composite (BSA@BBR@CDs) with much better water solubility. In vitro, with BSA modification, BSA@BBR@CDs was more readily taken up by tumor cells than BBR@CDs. After entering cells, BSA@BBR@CDs could more efficiently target mitochondria, resulting in mitochondrial dysfunction and eventually showing a stronger pro-apoptotic effect on tumor cells than BBR. In vivo, BSA@BBR@CDs can well accumulate in tumors via intravenous injection and significantly inhibit the tumor growth without significant toxicity to other organs. Therefore, BSA@BBR@CDs holds potential as a promising nanomedicine for cancer therapy.
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ChemistrySelect
·
2025
·Vol. 10
·期 35
·e03533
·
IF 2
Xiaodan Zheng,Ruolong Ma,Ziyan Song,Limeng Zhang,Chuanda Ruan,Wenzhi Yang,Yi Zhang,Xiaohui Yan,Fei Tian
With the widespread overuse of antibiotics, Staphylococcus aureus has developed multiple resistances to a variety of first-line antibiotics; therefore, it is imperative to explore novel antimicrobial strategies to solve the problem of resistance. Traditional Chinese medicines (TCM) are considered sources of chemicals with potential healing properties. In this study, berberine (BBR) and ferulic acid (FA) were used as raw materials to prepare nanoparticles with enhanced antibacterial activity by self-assembly technology. The study revealed that the self-assembly process involves non-covalent interactions. Minimum inhibitory concentration (MIC) of the FA-BBR NPs was 0.1 µmol/mL, and the antibacterial rate of FA-BBR NPs with a concentration of 0.2 µmol/mL against S. aureus was 94.56 ± 0.57%, which was significantly higher than monomers. The Bradford protein concentration assay was used to analyze the leakage of cellular contents. Scanning electron microscopy (SEM) and the fluorescent probe DiSC 3 (5) revealed that the nanoparticles can affect the integrity and permeability of bacterial biofilm, which is a key factor contributing to their superior antibacterial activity. Graphical A self-assembled carrier-free nano drug delivery system composed of ferulic acid and berberine was developed using a one-step self-assembly approach. FA-BBR NPs were found to significantly improve the solubility and antibacterial activity of the individual traditional Chinese medicine compounds. The two components primarily interact through noncovalent forces, including hydrogen bonding, ᴨ-ᴨ stacking, and electrostatic interactions. Further investigation revealed that FA-BBR NPs exerted enhanced antibacterial effects by compromising the integrity and permeability of bacterial cell membranes.
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Frontiers in Chemistry
·
2024
·
IF 3.8
Baodong Feng,Linqi Su,Yang Yang,Renyan Liu,Yu Zhang,Lingyi Xin,Li Wang,Zhiming Yang,Xuemei Wei,Qinhua Chen
Background: Ulcerative colitis (UC) is a chronic inflammatory bowel disease (IBD) influenced by multiple factors. Berberine, an isoquinoline alkaloid derived from the root and bark of Coptis chinensis Franch., has shown promise in managing UC, but its underlying mechanisms remain unclear.Methods: To elucidate the relationship between berberine, ulcerative colitis (UC), and the organism’s metabolome, we established a dextran sulfate sodium (DSS)-induced UC model in rats. Colonic tissue was collected for histopathological examination, while plasma samples were analyzed using liquid chromatography-tandem mass spectrometry (LC-MS/MS) with dynamic Multiple Reaction Monitoring (dMRM). This approach, characterized by its short analysis time of 20 min per sample, excellent reproducibility, and straightforward data processing, allowed for the comprehensive detection of a wide array of metabolites, including amino acids, lipids, and organic acids, many of which are implicated in the pathophysiology of UC.Results: Our results showed that berberine modulated the metabolic disturbances of 33 compounds in the plasma of UC rats, primarily including amino acids, pyrimidines, organic phosphoric acids, fatty acyls, and organonitrogen compounds. These altered metabolites were associated with various pathways, such as amino acid metabolism, glutathione metabolism, nicotinate and nicotinamide metabolism, taurine and hypotaurine metabolism, pyrimidine metabolism, glyoxylate and dicarboxylate metabolism, and the citrate cycle (TCA cycle). Notably, 3-hydroxyproline, homocysteic acid, L-threonine, L-lysine, carbamoyl phosphate, O-phosphoethanolamine, taurine, leucine, and phosphorylcholine exhibited significant differences between the Treatment and Model groups, with levels reverting to those of the Control group (p < 0.001). These findings suggested that these compounds may serve as potential plasma biomarkers for UC.Conclusion: This study provided valuable insights into the mechanism by which berberine exerted its therapeutic effects on UC through metabolomics. Our results highlighted berberine’s potential to modulate key metabolic pathways and restore the levels of several metabolites, suggesting its utility as a therapeutic agent for UC. These findings underscored the importance of metabolomics in understanding the pathophysiology and treatment of UC.
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MEDICINAL CHEMISTRY RESEARCH
·
2017
·Vol. 26
·期 3
·672-679
·
IF 1.277
Liu Zhenbao,Wang Xiaohong,Zhang Hang,Zhang Shanshan,Li Yiqian,Liu Yanfei,Peng Dongming
Berberine owns multiple pharmacological activities, especially anti-inflammatory activity. To enhance the anti-inflammatory therapeutic efficiency of berberine, a series of novel 9- O -substituted berberine derivatives ( 5a – 5d ) were synthesized and their anti-inflammatory activities were evaluated. 13 C-NMR, 1 H-NMR, IR and high resolution mass spectrum (HRMS) results indicated that these derivatives were successfully synthesized. The xylene-induced inflammatory mice model demonstrated that these derivatives showed dose-dependent inhibition of ear inflammatory swelling. Comparing to berberine, ibuprofen and naproxen-modified berberine derivatives enhanced anti-inflammatory activities, while aspirin and nicotinic acid-modified berberine derivatives showed lower anti-inflammatory effects at the same dosages. This could be attributed to the enhanced inhibition of secretion of cytokines, including interleukin-6 and tumor necrosis factor-α, by ibuprofen and naproxen berberine derivatives, while aspirin and nicotinic acid berberine derivatives showed lower inhibition of tumor necrosis factor-α than berberine. These results suggest that ibuprofen and naproxen-modified berberine derivatives are promising new anti-inflammatory drug candidates.
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NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS
·
2023
·
IF 1.3
Zizhen Huang,Jie Wang,Hui Chen,Ruofei Feng,Chunxia Tan
Four organic-polyoxometalate hybrids BR4[SiW12O40] (BR–SiW), BR3[PMo12O40] (BR–PMo), BR4K[EuSiW11O40]·2H2O (BR–EuSiW) and BR6Na3[EuW10O36] (BR–EuW) were fabricated by the polyoxometalates (POMs) anions and berberine cations (BR) noted for the alkaloids in traditional Chinese herbal medicine. These hybrids have been characterized and confirmed. The interaction between hybrids and human serum albumin (HSA) was investigated in a buffer solution (pH 7.4) using ultraviolet–visible light absorption and fluorescence techniques. The classical Stern–Volmer equation was used to analyze the fluorescence quenching at three temperatures (296, 303 and 310 K), and the static quenching mechanism for interaction was proposed. The Thermodynamic parameters, enthalpy, entropy change, and Gibbs free energy of hybrids interacting on HSA were calculated by Scatchard equation. The results indicated that therewas one binding site on the protein and BR–POMs all showed stronger binding force than that of raw materials. Synchronous fluorescence results showed that the binding sites of BR–POMs and HSA were not effectively affected the surrounding microenvironment. The following antibacterial experiments implied that inhibitory effect of hybrids were synergistic effect from organic active ingredient and POMs but the simple combination. All these data were prepared for further research on biology.
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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2026
·
IF 5.2
Xiaoxi Gao,Dehai Hou,Tianyu Ma,Sizhuo Liu,Ruiping Wang,Yang Ping,Jin Su
A synergistic nano-strategy co-delivering sorafenib and berberine to overcome resistance and reduce toxicity. • Optimized nanostructured lipid carriers with high drug loading, sustained release, and good stability were successfully prepared. • Pharmacokinetics showed significantly enhanced oral bioavailability (4.59-fold and 2.28-fold for SORB and BBR). • Superior antitumor efficacy and biosafety were systematically verified both in vitro and in vivo. Sorafenib (SORB) is a first-line drug for advanced hepatocellular carcinoma, but its clinical use is limited by poor water solubility, low oral bioavailability, and drug resistance. Berberine (BBR) has been shown to reverse multidrug resistance and enhance drug sensitivity. Here, we designed a nanostructured lipid carrier co-loaded with SORB and BBR (SBER NLC). The optimized formulation had a particle size of 123.17 ± 3.28 nm, PDI of 0.211 ± 0.012, and zeta potential of −18.30 ± 0.95 mV. Encapsulation efficiencies were 78.77 ± 0.93% (SORB) and 79.58 ± 1.04% (BBR), with drug loadings of 1.75 ± 0.06% and 1.28 ± 0.13%, respectively. SBER NLC showed stable storage properties and sustained release in simulated gastrointestinal fluids. Pharmacokinetic studies demonstrated significantly enhanced oral bioavailability of both drugs compared with free drug suspension. In vitro, SBER NLC exhibited stronger cytotoxicity and migration inhibition against HepG2 cells, while the blank carrier was nontoxic. In a HepG2 xenograft mouse model, SBER NLC achieved the strongest tumor suppression without causing body weight loss or major organ damage, and induced extensive nuclear pyknosis and necrosis in tumor tissue. This study provides an efficient nano-delivery strategy for combined SORB and BBR in hepatocellular carcinoma treatment. Download: Download high-res image (226KB) Download: Download full-size image
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BIOORGANIC CHEMISTRY
·
2026
·
IF 5.1
Zhi-chuan Chen,Jia-yi Li,Jian-rong Teng,Hong-zu Wei,Chang-chun Wen,Rui-xue Liu,Yan-cheng Liu,Hong Liang
Pharmaceutical co-crystals could modulate the physio-chemical properties of active pharmaceutical ingredients (APIs) and co-crystal formations (CCFs) via non-covalent interactions, including hydrogen bonds, π–π stacking and hydrophobic effects, which may generate synergistic pharmacological effects. Aiming to the antibiotic resistance and drug residues in aquaculture resulting from antibiotic overuse, in this study, we chose the key bioactive ingredients from traditional Chinese medicine (TCM), namely berberine (BBR), gallic acid (GA), and resveratrol (RSV), sourced from Coptis chinensis , Galla chinensis , and Polygonum cuspidatum , respectively. Through mixed-solution crystallization, two novel co -crystals of berberine and polyphenols (BBR-GA and BBR-RSV) were synthesized. Structural characterization using single crystal X-ray diffraction, Fourier infrared spectroscopy (FT-IR), nuclear magnetic resonance (NMR), and Hirshfeld surface analysis verified that both BBR-GA and BBR-RSV are predominantly stabilized by hydrogen bonds and hydrophobic interactions. Thermogravimetric analysis indicated that both BBR-GA and BBR-RSV display thermal stability, with decomposition temperatures higher than 200 °C. In vitro antibacterial tests against three typical aquatic pathogens revealed that both BBR-GA and BBR-RSV retained the broad-spectrum antibacterial activity of their respective API monomers. Specifically, BBR-RSV exhibited significant inhibitory effects against Aeromonas veronii and Citrobacter freundii , with minimum inhibitory concentration (MIC) of 0.125 mg/mL and 0.25 mg/mL, respectively. This study gives the first investigation on the potential application of the co-crystals from the active ingredients of TCM in the antibacterial field of aquaculture. It suggests that the co -crystals of berberine with natural polyphenols hold promise for development as new green veterinary drugs to substitute veterinary antibiotics.
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Materials Today Bio
·
2025
·
IF 10.2
Weibei Sheng,Lin Li,Zimeng Zhou,Jin Zhao,Shaohua Ma,Yaohang Yue,Jian Weng,Ao Xiong,Deli Wang,Jianjing Lin,Hui Zeng,Peng Liu
The inflammatory microenvironment mediated by synovial macrophages, particularly the pro-inflammatory M1 subtype, plays a central role in OA progression and represents a critical therapeutic target. However, delivery strategies that enable efficient and selective targeting of M1 macrophages for modulating the inflammatory microenvironment are still limited. To address this challenge, we developed a glucose-functionalized nanoparticle system (Ber-MNPs) to deliver berberine directly to pro-inflammatory M1 subtype macrophages—via GLUT1-mediated targeting, thereby modulating the inflammatory microenvironment to alleviate OA progression. The Ber-MNPs exhibited excellent targeting specificity toward M1 macrophages in vitro . In addition, Ber-MNPs can suppress macrophage polarization toward the pro-inflammatory M1 phenotype, promote their transition to the anti-inflammatory M2 phenotype, and downregulate inflammatory cytokines, thereby protecting chondrocytes from catabolic damage. In a surgically induced OA mouse model, intra-articularly administered Ber-MNPs exhibited prolonged joint retention and mitigated OA progression by attenuating synovial inflammation and preserving cartilage integrity. Together, this study establishes a M1 macrophage-targeted nanotherapeutic platform that achieves precise inflammatory modulation, offering a new strategy for reshaping the synovial inflammatory microenvironment and achieving effective delay of OA progression
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Nanoscale
·
2025
·
IF 5.1
Anqi Xia,Wenhui Yuan,Shanshan Xu,Ting Wu,Wenlu Yan,Ying Cao,Yaping Li,Qi Yin
Berberine hydrochloride (BH), a classic drug for treating acute enteritis, has been found to possess multiple immunoregulatory functions. However, its impact on the chemotherapy of colorectal cancer (CRC) has not been revealed. In addition, a suitable oral delivery system for BH is required to reduce and slow its clearance in the intestines and to improve its bioavailability. In the present work, a BH-loaded hybrid liposome containing a prebiotic inulin derivative, named BLPN, was designed and constructed. BLPN was stable in media simulating the gastrointestinal environment. It showed a bidirectional modulatory effect on immune cells, depending on the BH concentration. After oral administration, BLPN prolonged the retention time of BH in the intestines and blood circulation. In an MC38 orthotopic CRC mouse model, BLPN substantially increased the BH accumulation inside tumors. A chemotherapeutic agent, irinotecan hydrochloride-loaded liposome (ILPS), was also prepared. The combination of BLPN with ILPS activated both innate and adaptive anti-tumor immune cells and promoted the secretion of proinflammatory cytokines, which enhanced the extravasation of ILPS from the blood vessels within the tumor. The combination with BLPN significantly improved the CRC tumor-suppressive effect of ILPS and extended the survival time of tumor-bearing mice. This study provides a potential strategy for improving CRC chemotherapy by combining it with a prebiotic oral delivery system for BH.
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EXPERIMENTAL CELL RESEARCH
·
2023
·
IF 3.7
Yuehao Tan,Can Li,Jiali Zhou,Fengmei Deng,Yilun Liu
Berberine (BBR) is an effective drug against liver fibrosis (LF). Autophagy is involved in the pathogenesis of LF; however, the mechanism linking BBR to autophagy in LF remains unresolved. To explore the underlying mechanism, we assessed the effects of BBR on autophagy and apoptosis of activated hepatic stellate cells (HSCs) in vitro and in a murine model of fibrosis. The decreased expression of the autophagy activation marker ATG5 , autophagosome formation, and autophagy flux in the HSC model confirmed that BBR inhibited autophagy in activated HSCs and in mice with liver fibrosis. Moreover, ATG5 was necessary for inducing autophagy and HSC activation. BBR suppressed ATG5 expression by upregulating miR-30a-5p expression, which affected the stability of ATG5 mRNA by binding to its 3′-untranslated region, an effect that was attenuated by treatment with a miR-30a-5p inhibitor. BBR also markedly induced HSC apoptosis, as indicated by the upregulated expression of the pro-apoptosis markers p53, BAX, and cleaved PARP and the downregulated expression of the anti-apoptosis marker BCL-2, effects that were reversed by ATG5 overexpression. In vivo, BBR improved mouse LF by decreasing collagen deposition, inflammatory cell infiltration , and expression of fibrosis markers hydroxyproline, α-smooth muscle actin, and collagen type 1-A1 and the autophagy marker LC3. BBR had a protective effect on mouse fibrotic livers and reduced serum aspartate aminotransferase and alanine aminotransferase levels . Collectively, these results reveal a novel mechanism of BBR-induced autophagy inhibition triggering apoptosis in HSCs, providing a reliable experimental and theoretical basis for developing BBR-based candidate drugs for LF.
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Nanoscale
·
2022
·Vol. 14
·期 27
·9818-9831
·
IF 8.307
Rong-Tian Li,Ming Chen,Zi-Chuan Yang,Yong-Jian Chen,Nai-Han Huang,Wen-Hua Chen,Jun Chen,Jin-Xiang Chen
We designed and synthesized three new berberine-based compounds, namely, pyridine-2,6-dimethyl-/2,2′-bipyridine-3,3′-dimethyl-tethered berberine dimers BD1 and BD2, and a tetrakis(4-benzyl)ethylene linked berberine tetramer BD4. We identified that the dimer BD2 and tetramer BD4, as well as 1,10-phenanthroline-2,9-dimethyl-linked berberine dimer BD3 previously reported by us, showed remarkable aggregation-induced emission (AIE) properties which endowed them with higher singlet oxygen (1O2) production ability than berberine. Of the four compounds, BD3 exhibits the lowest ΔEST energy with the highest 1O2 generation ability and thus was selected for further construction of AuNSs–BD3@HA (denoted as ABH, AuNSs = gold nanostars; HA = hyaluronic acid). The nanosystem of ABH shows a remarkable therapeutic effect toward breast cancer by combining photodynamic therapy (PDT) from BD3, photothermal therapy (PTT) from AuNSs, and the CD44-targeting capability of HA. The synergistically enhanced PDT and PTT induce superior cancer cell apoptosis/necrosis in vitro and anti-breast cancer activity in vivo. This study provides a new concept for PDT using natural product derivatives and their combination with PTT for efficient treatment of tumors.
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