Reverse Zagreb Indices and Their Application in the Evaluation of Physiochemical Properties of Anticancer/Antibacterial Drugs.

Recent advancements in chemical graph theory have facilitated a deeper understanding of the relationship between chemical structures and their underlying graphs based upon classical graph theory principles. Quantitative structure-property relationship (QSPR) analysis stands out as a powerful tool for probing chemical graphs. Topological indices, graph invariants assigning numerical values to graphs, play a pivotal role in statistically correlating physical properties, chemical reactivity, and biological activity across diverse chemical structures.

NRPS substrate promiscuity leads to more potent antitubercular sansanmycin analogues.

Sansanmycins, members of the uridyl peptide antibiotics, are assembled by nonribosomal peptide synthetases (NRPSs), the substrate promiscuity of which results in the diversity of products. Further exploration of the NRPSs' substrate promiscuity by reinvestigating sansanmycin producer strain led to the isolation and structural elucidation of eight new uridyl peptides, sansanmycins H-O (1-8). Among them, sansanmycin L, containing a 6-OH-bicyclic residue and Phe3 first found at the position AA3, exhibited activity against M.

Discovery, synthesis and biological evaluation of cycloprotoberberine derivatives as potential antitumor agents.

A series of new 1,13-cycloprotoberberine derivatives defined through variations at the 9-position were designed, synthesized and evaluated for their cytotoxicities in human HepG2 (hepatoma), HT1080 (fibrosarcoma) and HCT116 (colon cancer) cells. The preliminary structure-activity relationship (SAR) revealed that the replacement of 9-methoxyl with an ester moiety might significantly enhance the antiproliferative activity in vitro. Notably, compound 7f demonstrated equipotent cytotoxicity activity against breast cancer MCF-7 (parent) and doxorubicin (DOX)-resistant MCF-7 (MCF-7/ADrR) cells, indicating a mode of action different from that of DOX.

SsaA, a member of a novel class of transcriptional regulators, controls sansanmycin production in Streptomyces sp. strain SS through a feedback mechanism.

Sansanmycins, produced by Streptomyces sp. strain SS, are uridyl peptide antibiotics with activities against Pseudomonas aeruginosa and multidrug-resistant Mycobacterium tuberculosis. In this work, the biosynthetic gene cluster of sansanmycins, comprised of 25 open reading frames (ORFs) showing considerable amino acid sequence identity to those of the pacidamycin and napsamycin gene cluster, was identified.

Draft genome sequence of Streptomyces sp. strain SS, which produces a series of uridyl peptide antibiotic sansanmycins.

Streptomyces sp. SS produces a series of uridyl peptide antibiotic sansanmycins. Here, we present a draft genome sequence of Streptomyces sp.

[In vivo distribution of FITC-labeled boanmycin hydrochloride in situ gel].

This study is to evaluate the sustained-release effect of the thermosensitive in situ gel for injection of boanmycin hydrochloride (BAM) by bioluminescence imaging in nude mice. BAM was labeled with fluorescein isothiocyanate (FITC). The FITC-labeled BAM (FITC-BAM) was purified by dialysis and Sephadex G25 gel column, and then was identified by matrix-assisted laser desorption ionization/time of flight (MALDI-TOF).

A marine-derived Streptomyces sp. MS449 produces high yield of actinomycin X2 and actinomycin D with potent anti-tuberculosis activity.

In the course of our screening program for anti-Mycobacterium bovis bacillus Calmette-Guérin (BCG) and anti-Mycobacterium tuberculosis H37Rv (MTB H37Rv) agents from our marine natural product library, a newly isolated actinomycete strain, designated as MS449, was picked out for further investigation. The strain MS449, isolated from a sediment sample collected from South China Sea, produced actinomycin X(2) and actinomycin D in substantial quantities, which showed strong inhibition of BCG and MTB H37Rv. The structures of actinomycins were elucidated by nuclear magnetic resonance and mass spectrometric analysis.

Synthesis and in vitro antitubercular evaluation of novel sansanmycin derivatives.

Tuberculosis (TB) is a major health problem worldwide. A series of novel sansanmycin derivatives were designed, semi-synthesized and evaluated for their activity against drug-susceptible Mycobacterium tuberculosis strain H(37)Rv with sansanmycin A (SSA) as the lead. Among these analogs tested, compound 1d possessing an isopropyl group at the amino terminal afforded an increased antimycobacterial activity with a MIC value of 8 μg/mL in comparison with SSA.

[Thermosensitive in situ gel of boanmycin hydrochloride for injection].

Poloxamer F127, poloxamer F68 and hydroxypropyl methylcellulose K4M were used to prepare the thermosensitive in situ gel of boanmycin hydrochloride for injection. Its gelation temperature, rheological behavior, texture characteristics, scanning electron microscopy, in vitro and in vivo drug release were evaluated. These results showed that the formulation was a fluid solution at room temperature, which could become semisolid at the temperature of 37 degrees C, and the thermally induced sol-gel transition allowed to be injectable and in situ setting.

Potent antitumor actions of the new antibiotic boningmycin through induction of apoptosis and cellular senescence.

Boningmycin, a new antibiotic of the bleomycin family, is isolated from the fermentation broth of Streptomyces verticillus var. pingyangensis n.sp.

Mechanisms of the antitumor action of the new antibiotic NC0604, a member of the bleomycin family.

NC0604, the new antibiotic of the bleomycin family, was isolated from the fermentation broth of Streptomyces verticillus var. pingyangensis n.sp.

Effects of combined treatment with sansanmycin and macrolides on Pseudomonas aeruginosa and formation of biofilm.

Objective: To observe the effects of combined treatment with sansanmycin and macrolides on Pseudomonas aeruginosa and formation of biofilm.

Methods: Micro-dilution method was used to determine the minimal inhibitory concentrations (MICs) of sansanmycin, gentamycin, carbenicillin, polymyxin B, roxithromycin, piperacillin, and tazobactam. PA1 and PA27853 biofilms were observed under optical microscope after staining and under SEM after treatment with sansanmycin at different dosages and combined treatment with sansanmycin and roxithromycin.

Isolation and characterization of antibiotic NC0604, a new analogue of bleomycin.

NC0604, a new analogue of bleomycin, was isolated from fermentation broth of Streptomyces verticillus var. pingyangensis n.var.

Sansanmycins B and C, new components of sansanmycins.

Two new antibiotics, sansanmycins B and C, were isolated from Streptomyces sp. SS. Their structures were elucidated by extensive 1D and 2D NMR and MS spectral analyses.

A new nucleosidyl-peptide antibiotic, sansanmycin.

A new nucleosidyl-peptide antibiotic, sansanmycin, was isolated from an unidentified Streptomyces sp SS. The structure of sansanmycin was elucidated by analyses of its alkaline hydrolysate and spectroscopic analyses. Sansanmycin exhibits antibacterial activity against Mycobacterium tuberculosis H(37)Ra and Pseudomonas aeruginosa with MIC values of 10 and 12.