Discovery of 15-deoxynaphthomycins activating the antioxidant NRF2-ARE pathway from Streptomyces sp. N50 via genome mining, global regulator introduction, and molecular networking DOI Creative Commons
Min-Seon Kim,

Baskar Selvaraj,

Hee-Tae Yeo

и другие.

Microbial Cell Factories, Год журнала: 2025, Номер 24(1)

Опубликована: Янв. 10, 2025

Genome mining is a promising avenue for expanding the repertoire of microbial natural products, which are important drug development. This approach involves predicting genetically encoded small molecules by examining bacterial genomes via accumulated knowledge biosynthesis. However, it also that microbes produce predicted molecule in practice. Here, we introduce an endophytic Streptomyces sp. N50, was isolated from medicinal plant Selaginella tamariscina. Upon sequencing its entire genome, 33 biosynthetic gene clusters (BGCs) were identified chromosome and megaplasmid. Subsequent genome revealed new 15-deoxynaphthomycin could be produced due to presence enoyl reductase domain, absent known BGC naphthomycin, type ansamycin antibiotics. In addition, engineered strain with introduction global regulatory afsR2 into N50 successfully 15-deoxynaphthomycins. Furthermore, molecular network analysis MS/MS selectively confirmed additional sulfur-containing congeners. Eventually, six 15-deoxynaphthomycins elucidated N50. family compounds exhibit various biological activities. Also, quinone moieties these compounds, activate NRF2, they tested their ability NRF2. Among three (1, 5, 6) activated antioxidant NRF2-ARE signaling pathway. Treatment significantly elevated NRF2 levels HepG2 cells further induced expression target genes associated response. study suggests combination mining, engineering networking helpful generating as pharmaceutical candidates microorganisms.

Язык: Английский

A General Platform for Visible Light Sulfonylation Reactions Enabled by Catalytic Triarylamine EDA Complexes DOI
Juan D. Lasso, Durbis J. Castillo‐Pazos, Jan Michael Salgado

и другие.

Journal of the American Chemical Society, Год журнала: 2024, Номер 146(4), С. 2583 - 2592

Опубликована: Янв. 17, 2024

Catalytic electron donor–acceptor (EDA) complexes have recently emerged as a powerful and sustainable alternative to iridium- ruthenium-based photoredox synthetic methods. Yet, these remain underexplored reliant on the use of meticulously designed acceptors that require previous installation. Herein, we report novel EDA complex employing tris(4-methoxyphenyl) amine catalytic donor for sulfonylation alkenes using inexpensive readily available sulfonyl chlorides. Applying this operationally simple, visible-light-mediated general platform, both redox-neutral net-reductive functionalization more than 60 substrates, encompassing vinylic or allylic sulfonylation, hydrosulfonylation, sulfamoylation activated unactivated alkynes.

Язык: Английский

Процитировано

44
Emerging trends and future opportunities for coumarin-heterocycle conjugates as antibacterial agents DOI Creative Commons
Yasser Fakri Mustafa

Results in Chemistry, Год журнала: 2023, Номер 6, С. 101151 - 101151

Опубликована: Окт. 5, 2023

Infectious diseases resulting from various strains of pathogenic bacteria are among the leading causes death and morbidity worldwide. The currently-available antibacterial medications developed natural or synthetic sources cornerstone bacterial infection intervention, but somehow mounting spread expansion multidrug-resistant harmful has become a major concern for medical-providing communities pharmaceutical-releasing companies. pervasiveness coumarin-based products in nature simplicity their lab chemical synthesis, addition to ability coumarin backbone communicate, may interact with DNA gyrase at B subunit hinder secondary structure by abolishing ATPase activity; thus, conjugates have potential act as agents. It is conceivable that conjugation nucleus other heterocyclic-based scaffolds present opportunities creation novel drugs. This presentation be based on fact several coumarin-heterocycle conjugates, including clorobiocin, coumermycin A1, novobiocin, already been used medical methods treatment infectious diseases. study explores, during period last 5 years, relationships between activity action. investigation also explored developing these into medicines.

Язык: Английский

Процитировано

39
Targeted isolation of antitubercular cycloheptapeptides and an unusual pyrroloindoline-containing new analog, asperpyrroindotide A, using LC–MS/MS-based molecular networking DOI Creative Commons

Yi-Qian Han,

Qun Zhang, Weifeng Xu

и другие.

Marine Life Science & Technology, Год журнала: 2023, Номер 5(1), С. 85 - 93

Опубликована: Янв. 20, 2023

Further insights on the secondary metabolites of a soft coral-derived fungus Aspergillus versicolor under guidance MS/MS-based molecular networking led to isolation seven known cycloheptapeptides, namely, asperversiamides A-C (1-3) and asperheptatides A-D (4-7) an unusual pyrroloindoline-containing new cycloheptapeptide, asperpyrroindotide A (8). The structure 8 was elucidated by comprehensive spectroscopic data analysis, its absolute configuration determined advanced Marfey's method. semisynthetic transformation 1 into successfully achieved reaction conditions were optimized. Additionally, series derivatives (10-19) asperversiamide (1) semi-synthesized their anti-tubercular activities evaluated against Mycobacterium tuberculosis H37Ra. preliminary structure-activity relationships revealed that serine hydroxy groups tryptophan residue are important activity.The online version contains supplementary material available at 10.1007/s42995-022-00157-8.

Язык: Английский

Процитировано

24
Sulfur-containing marine natural products as leads for drug discovery and development DOI
Feng-Wei Guo, Qun Zhang, Yu‐Cheng Gu

и другие.

Current Opinion in Chemical Biology, Год журнала: 2023, Номер 75, С. 102330 - 102330

Опубликована: Май 29, 2023

Язык: Английский

Процитировано

24
Anticancer Potential of the S‐Heterocyclic Ring Containing Drugs and its Bioactivation to Reactive Metabolites DOI

Sumit Maji,

Biplab Debnath,

Shambo Panda

и другие.

Chemistry & Biodiversity, Год журнала: 2024, Номер 21(7)

Опубликована: Май 9, 2024

Sulfur-containing heterocyclic derivatives have been disclosed for binding with a wide range of cancer-specific protein targets. Various interesting sulfur-containing heterocyclics such as benzothiazole, thiazole, thiophene, thiazolidinedione, benzothiophene, and phenothiazine, etc shown to inhibit diverse signaling pathways implicated in cancer. Significant progress has also made molecular targeted therapy against specific enzymes kinase receptors due potential interactions inside the ATP pocket. ring metal complexes i. e., benzothiophene phenothiazines are among most promising active anticancer compounds. However, sulfur heteroaromatic rings, particularly high structural alert their metabolism reactive metabolites. The mere presence itself does not determine compound toxicity therefore, this review focuses on some findings that shed light factors influencing toxicity. In current review, synthetic strategies introducing core synthesized discussed structure-activity relationships enhance our understanding mechanisms develop safer therapeutic options. marketed drugs included direct synthesis novel compounds will help development potent, sulfur-based near future.

Язык: Английский

Процитировано

11
The anti-cancer effectiveness of some heterocyclic compounds containing sulfur atom DOI Creative Commons

Hasan Tuhmaz Hamad

Results in Chemistry, Год журнала: 2025, Номер unknown, С. 102182 - 102182

Опубликована: Март 1, 2025

Язык: Английский

Процитировано

2
Thiophenes—Naturally Occurring Plant Metabolites: Biological Activities and In Silico Evaluation of Their Potential as Cathepsin D Inhibitors DOI Creative Commons
Sabrin R. M. Ibrahim, Abdelsattar M. Omar, Alaa Bagalagel

и другие.

Plants, Год журнала: 2022, Номер 11(4), С. 539 - 539

Опубликована: Фев. 17, 2022

Naturally, thiophenes represent a small family of natural metabolites featured by one to five thiophene rings. Numerous plant species belonging the Asteraceae commonly produce thiophenes. These possessed remarkable bioactivities, including antimicrobial, antiviral, anti-inflammatory, larvicidal, antioxidant, insecticidal, cytotoxic, and nematicidal properties. The current review provides an update over past seven years for reported derivatives, their sources, biosynthesis, spectral data, bioactivities since last published in 2015. Additionally, with help SuperPred webserver, AI (artificial intelligence) tool, potential drug target compounds was predicted. In silico studies were conducted Cathepsin D ADMET (drug absorption/distribution/metabolism/excretion/and toxicity) properties prediction, molecular docking binding interaction, dynamics evaluate ligand-target interaction stability under simulated physiological conditions.

Язык: Английский

Процитировано

36
Identification of marine natural product Pretrichodermamide B as a STAT3 inhibitor for efficient anticancer therapy DOI Creative Commons
Rui Li, Yue Zhou, Xinxin Zhang

и другие.

Marine Life Science & Technology, Год журнала: 2023, Номер 5(1), С. 94 - 101

Опубликована: Фев. 6, 2023

The Janus kinase (JAK)/signal transducer and activator of transcription 3 (STAT3) regulates the expression various critical mediators cancer is considered as one central communication nodes in cell growth survival. Marine natural products (MNP) represent great resources for discovery bioactive lead compounds, especially anti-cancer agents. Through medium-throughput screening our in-house MNP library, Pretrichodermamide B, an epidithiodiketopiperazine, was identified a JAK/STAT3 signaling inhibitor. Further studies that B directly binds to STAT3, preventing phosphorylation thus inhibiting signaling. Moreover, it suppressed growth, vitro, at low micromolar concentrations demonstrated efficacy vivo by decreasing tumor xenograft mouse model. In addition, shown able induce cycle arrest promote apoptosis. This study novel STAT3 inhibitor, which should be further exploration promising therapy.

Язык: Английский

Процитировано

18
Dithiocarbamate based novel anti-histaminic agents: Synthesis, characterization, crystal structure and thermal study DOI
Anupam Singh, R. Kumar, Riya Patel

и другие.

Dalton Transactions, Год журнала: 2024, Номер 53(33), С. 14077 - 14088

Опубликована: Янв. 1, 2024

Complexes of Co( iii ) (1), Ni( ii (2), Cu( (3), and Zn( (4) derived from an N -(4-fluorobenzyl) -(pyridin-2-ylmethyl) dithiocarbamate ligand. Complex 3 showed maximum reduction in clonidine-induced catalepsy after 180 minutes treatment.

Язык: Английский

Процитировано

7
Natural Products from Marine-Derived Fungi with Anti-Inflammatory Activity DOI Creative Commons

Yikang Qiu,

Shiji Chen,

Miao Yu

и другие.

Marine Drugs, Год журнала: 2024, Номер 22(10), С. 433 - 433

Опубликована: Сен. 25, 2024

Inflammation is considered as one of the most primary protective innate immunity responses, closely related to body’s defense mechanism for responding chemical, biological infections, or physical injuries. Furthermore, prolonged inflammation undesirable, playing an important role in development various diseases, such heart disease, diabetes, Alzheimer’s atherosclerosis, rheumatoid arthritis, and even certain cancers. Marine-derived fungi represent promising sources structurally novel bioactive natural products, have been a focus research anti-inflammatory drugs. This review covers secondary metabolites with activities from marine-derived fungi, over period spanning August 2018 July 2024. A total 285 metabolites, including 156 compounds 11 skeleton structures, are described. Their structures categorized into five categories: terpenoids, polyketides, nitrogen-containing compounds, steroids, other classes. The targets, well vitro vivo screening models, were surveyed statistically summarized. paper aims offer valuable insights researchers exploration products discovery

Язык: Английский

Процитировано

7