The bioactive agent andrographolide was screened with pharmaceutically acceptable coformers to discover a novel solid form that will solve the chemical instability and poor solubility problems of this herbal medicine. Liquid-assisted grinding of andrographolide with GRAS (generally regarded as safe) coformers in a fixed stoichiometry resulted in cocrystals with vanillin (1:1), vanillic acid (1:1), salicylic acid (1:1), resorcinol (1:1), and guaiacol (1:1). All the crystalline products were characterized by thermal, spectroscopic, and diffraction methods. Interestingly, even though the cocrystals are isostructural, their physicochemical properties are quite different. The andrographolide-salicylic acid cocrystal completely inhibited the chemical transformation of andrographolide to its inactive sulfate metabolite, and moreover, the cocrystal exhibited a dissolution rate that was three times faster and a drug release that was two times higher than pure andrographolide.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1002/asia.201300859 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Coacervate-Derived Assembly of Poly(ethylene glycol) Nanoparticles for Combinational Tumor Therapy.
Adv Healthc Mater
January 2025
Key Laboratory of Colloid and Interface Chemistry of the Ministry of Education, School of Chemistry and Chemical Engineering, Shandong University, Jinan, Shandong, 250100, China.
Coacervates have garnered significant attention as potential drug carriers. However, the instability resulting from their intrinsic membrane-free nature restricts the application of coacervates in drug delivery. Herein, the engineering of poly(ethylene glycol) nanoparticles (PEG NPs) is reported using coacervates composed of PEG and polyphenols as the templates, where PEG is subsequently cross-linked based on different chemistries (e.
View Article and Find Full Text PDFTargeting chromosomally unstable tumors with a selective KIF18A inhibitor.
Nat Commun
January 2025
Volastra Therapeutics, New York, NY, USA.
Chromosome instability is a prevalent vulnerability of cancer cells that has yet to be fully exploited therapeutically. To identify genes uniquely essential to chromosomally unstable cells, we mined the Cancer Dependency Map for genes essential in tumor cells with high levels of copy number aberrations. We identify and validate KIF18A, a mitotic kinesin, as a vulnerability of chromosomally unstable cancer cells.
View Article and Find Full Text PDFInitiator-Free Thiol-Aldehyde Photo Polycondensation.
Angew Chem Int Ed Engl
January 2025
Anhui Agricultural University, Materials and Chemistry, CHINA.
Traditional photopolymerizations generally requires an initiator for initiating the polymerization while few cases have created degradable chemical bonds. Moreover, the migration instability and cytotoxicity of photo initiators are posing issues to human health and the environment. In this work, we discovered an initiator-free photo polycondensation system (IFPPC) between polymercaptans and aldehyde monomers, producing high strength plastic materials with exchangeable and degradable dithioacetal groups.
View Article and Find Full Text PDFRealizing C-C Coupling via Accumulation of C1 Intermediates within Dual-Vacancy-Induced Dipole-Limited Domain Field to Propel Photoreduction of CO-to-C2 Fuel.
Adv Mater
January 2025
Faculty of Chemistry and Chemical Engineering, Shantou University, Shantou, 515063, P. R. China.
Photocatalytic conversion of CO and HO into high-value-added C2 fuels remains a tough challenge, mainly due to the insufficient concentration of photogenerated electrons for the instability of C1 intermediates, which often tend to desorb easily and disable to form C─C bonds. In this work, photoreduction of CO-to-CH is successfully achieved by introducing adjacent C, N dual-vacancy sites within the heptazine rings of ultrathin g-CN, which results in the opening of two neighboring heptazine rings and forms a distinctive dipole-limited domain field (DLDF) structure. In situ X-ray photoelectron spectra and in situ fourier transform infrared spectra provide direct evidence of the rapid accumulation and transformation of C1 intermediates, especially CO and CHO, within the DLDF.
View Article and Find Full Text PDFAdaptation of E. coli to Ciprofloxacin and Enrofloxacin: Differential Proteomics of the SOS Response and RecA-Independent Mechanisms.
Int J Antimicrob Agents
December 2024
University of Amsterdam, Swammerdam Institute of Life Sciences, Molecular Biology and Microbial Food Safety, Amsterdam, The Netherlands. Electronic address:
Antibiotic resistance is a growing global healthcare challenge, treatment of bacterial infections with fluoroquinolones being no exception. These antibiotics can induce genetic instability through several mechanisms, one of the most significant being the activation of the SOS response. During exposure to sublethal concentration, this stress response increases mutation rates, accelerating resistance evolution.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!