Insights on exploring the therapeutic potential and structural modification of Tetrandrine DOI
Liang Gong, He Liu, Bo Xu

et al.

Future Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 16(24), P. 2687 - 2700

Published: Nov. 28, 2024

Tetrandrine (Tet), a bisbenzylisoquinoline alkaloid from Stephania tetrandra, is noted for its diverse pharmacological effects but faces limitations in clinical use due to toxicity, poor solubility, and low bioavailability. Researchers are working address these issues by developing Tet derivatives with greater therapeutic potential through structural modification. Generally, key modifications include: 1) introducing an aromatic heterocycle or hydrophobic alkyne unit at the C-5 position can enhance antitumor activity; 2) adding amide, sulfonamide, electron-withdrawing group C-14 3) changing structure quaternary ammonium salt alter solubility greatly boost antibacterial 4) modification of C-12-methoxybenzyl motif metabolic stability thus change activity analogs; 5) simplification may result identification anticancer lead compounds novel mechanisms action. This review systematically summarizes strategies evaluates biological activities derivatives, aiming guide further optimization facilitate discovery analogs improved efficacy. The future direction possibility also considered.

Language: Английский

Integrated network pharmacological analysis and multi-omics techniques to reveal the mechanism of polydatin in the treatment of silicosis via gut-lung axis DOI Creative Commons
Bingbing Wu,

Yiwen Tang,

Liyuan Zhao

et al.

European Journal of Pharmaceutical Sciences, Journal Year: 2025, Volume and Issue: unknown, P. 107030 - 107030

Published: Feb. 1, 2025

Silicosis is a pulmonary disease characterized by inflammation and progressive fibrosis. Previous studies have shown that polydatin (PD) has potential biological activity in key signaling pathways regulating apoptosis. To investigate the effect of PD on rats with silicosis, this study used network pharmacology molecular docking methods to determine target treatment for silicosis. The therapeutic silicosis was confirmed measuring lung injury score, hydroxyproline content, mRNA expression levels targets. In addition, metagenomic sequencing gas chromatography-mass spectrometry were gut microbiota composition targeted metabolomics analysis, respectively. results showed could inhibit inflammation-related indexes apoptosis-related at protein levels. also regulates diversity intestinal flora content short-chain fatty acids. conclusion, current data suggest protective against silica-induced plays role acid through gut-lung axis.

Language: Английский

Citations

0
Tetrandrine induces cell cycle arrest in cutaneous melanoma cells by inhibiting IL-6/CDC42 signaling DOI
Liang Niu, Jin Chang, Shuo Liu

et al.

Archives of Dermatological Research, Journal Year: 2025, Volume and Issue: 317(1)

Published: Feb. 20, 2025

Language: Английский

Citations

0
Tetrandrine augments melanoma cell immunogenicity via dual inhibition of autophagic flux and proteasomal activity enhancing MHC-I presentation DOI Creative Commons
Lina He,

Yu-jiao Liu,

Junbo Jiang

et al.

Acta Pharmacologica Sinica, Journal Year: 2025, Volume and Issue: unknown

Published: Feb. 27, 2025

Abstract MHC-I-mediated antigen presentation is pivotal in antitumor immunity, enabling the recognition and destruction of tumor cells by CD8 + T cells. Both proteasome autophagy serve as essential cellular degradation mechanisms that regulate stability functionality MHC-I molecules. In melanoma, modulating pathways affect can profoundly influence therapeutic outcomes immunotherapy. Our initial effort this study was a screening process to identify natural compounds capable amplifying surface expression on B16 melanoma Utilizing flow cytometry with fluorescently tagged antibodies, we identified tetrandrine (Tet), bisbenzylisoquinoline alkaloid derived from root Stephania tetrandra , potent enhancer We demonstrate (2.5, 5, 7.5 μM) dose-dependently upregulates both total protein levels or A375 simultaneously inhibiting proteasomal activity, two key involved degradation. This dual inhibition stabilizes molecules, leading enhanced improved co-culture systems, treatment increased cell activation cytotoxicity against cells, evidenced elevated IFN-γ secretion apoptosis. Administration (50 mg·kg -1 ·d i.g., for 15 days) significantly suppressed growth mouse models accompanied infiltration within microenvironment. Notably, synergized anti-PD-1 immune checkpoint therapy, compared either alone. revealed (7.5 blocked lysosomal calcium efflux channel TPC2, disrupting homeostasis, thus impairing acidification thereby stabilizing molecules promoting presentation. These results highlight tetrandrine’s unique mechanism action enhancing through autophagic flux underscores potential novel immunomodulatory agent boost cell-mediated eradication enhance efficacy therapies.

Language: Английский

Citations

0
Neuroinflammation and energy metabolism: a dual perspective on ischemic stroke DOI Creative Commons
Lei Wen, Hao Zhuang, Weiyi Huang

et al.

Journal of Translational Medicine, Journal Year: 2025, Volume and Issue: 23(1)

Published: April 10, 2025

Ischemic stroke is a prevalent form of cerebrovascular accident, with its pathogenesis involving the intricate interplay between neuroinflammation and energy metabolism. Cerebral ischemia disrupts oxygen supply, triggering metabolic dysregulation activating neuroinflammatory responses, ultimately resulting in cellular damage. This review provides an exhaustive analysis complex mechanisms ischemic stroke, particular focus on interaction The interruption supply due to cerebral initiates activates including release inflammatory cytokines activation immune cells, contributing damage further disturbances. Studies indicate that metabolism significantly impairs neural cell function interacts neuroinflammation, exacerbating brain injury. Therapeutic strategies primarily concentrate modulating suppressing emphasizing importance in-depth research into their provide theoretical foundation for new treatment stroke. Future should how balance anti-inflammatory regulation minimize promote recovery.

Language: Английский

Citations

0
Tetrandrine and adriamycin reverse multidrug resistance by regulating NLRP3/Caspase-1/GSDMD signaling in human breast cancer cells DOI
Guosong Xin,

Yingping Hou,

Yuhan Liu

et al.

European Journal of Pharmacology, Journal Year: 2025, Volume and Issue: 998, P. 177635 - 177635

Published: April 17, 2025

Language: Английский

Citations

0
Tetrandrine ameliorated atherosclerosis in vitamin D3/high cholesterol diet-challenged rats via modulation of miR-34a and Wnt5a/Ror2/ABCA1/NF-kB trajectory DOI Creative Commons

Yasmin El Zouka,

Eman Sheta,

Mona Abdelrazek Salama

et al.

Scientific Reports, Journal Year: 2024, Volume and Issue: 14(1)

Published: Sept. 12, 2024

Language: Английский

Citations

2
Microgel-Encapsulated Tetrandrine Nanoparticles Promote Spinal Cord Repair by Sustaining Neuroinflammation Inhibition DOI
Chongxi Xu, Xiue Jiang,

Wumeng Yin

et al.

Journal of Materials Chemistry B, Journal Year: 2024, Volume and Issue: 13(2), P. 683 - 694

Published: Nov. 22, 2024

By embedding Tet nanoparticles in microgels, we developed a dual-drug system for controlled drug delivery to restrain neuroinflammation SCI.

Language: Английский

Citations

2
Advances in nano‐preparations for improving tetrandrine solubility and bioavailability DOI
Jie Ling,

Jingping Wu,

Yuening Cao

et al.

Archiv der Pharmazie, Journal Year: 2024, Volume and Issue: 357(10)

Published: June 20, 2024

Abstract Tetrandrine (TET) is a natural bis‐benzylisoquinoline alkaloid isolated from Stephania species with wide range of biological and pharmacologic activities; it mainly serves as an anti‐inflammatory agent or antitumor adjuvant in clinical applications. However, limitations such prominent hydrophobicity, severe off‐target toxicity, low absorption result suboptimal therapeutic outcomes preventing its widespread adoption. Nanoparticles have proven to be efficient devices for targeted drug delivery since drug‐carrying nanoparticles can passively transported the tumor site by enhanced permeability retention (EPR) effects, thus securing niche cancer therapies. Great progress has been made nanocarrier construction TET due their outstanding advantages increased water‐solubility, improved biodistribution blood circulation, reduced irritation, combinational therapy. Herein, we systematically reviewed latest advancements TET‐loaded respective features expectation providing perspective guidelines future research potential applications TET.

Language: Английский

Citations

1
Acoustic resonance technology and quality by design approach facilitate the development of the robust tetrandrine nano-delivery system DOI
Xiaoyang Zhang, Xi Wang,

Jianlu Qu

et al.

European Journal of Pharmaceutics and Biopharmaceutics, Journal Year: 2024, Volume and Issue: unknown, P. 114522 - 114522

Published: Oct. 1, 2024

Language: Английский

Citations

0
Insights on exploring the therapeutic potential and structural modification of Tetrandrine DOI
Liang Gong, He Liu, Bo Xu

et al.

Future Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 16(24), P. 2687 - 2700

Published: Nov. 28, 2024

Tetrandrine (Tet), a bisbenzylisoquinoline alkaloid from Stephania tetrandra, is noted for its diverse pharmacological effects but faces limitations in clinical use due to toxicity, poor solubility, and low bioavailability. Researchers are working address these issues by developing Tet derivatives with greater therapeutic potential through structural modification. Generally, key modifications include: 1) introducing an aromatic heterocycle or hydrophobic alkyne unit at the C-5 position can enhance antitumor activity; 2) adding amide, sulfonamide, electron-withdrawing group C-14 3) changing structure quaternary ammonium salt alter solubility greatly boost antibacterial 4) modification of C-12-methoxybenzyl motif metabolic stability thus change activity analogs; 5) simplification may result identification anticancer lead compounds novel mechanisms action. This review systematically summarizes strategies evaluates biological activities derivatives, aiming guide further optimization facilitate discovery analogs improved efficacy. The future direction possibility also considered.

Language: Английский

Citations

0