Synthesis of Novel Drug Benvitimod

Gao, Jun; Yue, Zhang; Zheng, He Tang; Wang, Chun Fang; Liu, Hui Xian; Zhao, Sihai

doi:10.4028/www.scientific.net/amr.236-238.2378

Cited by 5 publications

(3 citation statements)

References 10 publications

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“…101,102 It was first developed under the name WBI-1001 by Welichem Biotech Inc. in China. 103 Benvitimod 1% (Beijing Wenfeng Tianji Pharma Ltd.) uses a petrolatum-based vehicle for delivery while tapinarof 1% uses a "novel" cream-based vehicle developed by Dermavant Sciences Inc. [103][104][105][106][107] The active ingredient remains the same (3,5-dihydroxy-4-isopropyl-trans-stilbene), isolated from the bacterium Photorhabdus luminescens. 108,109…”

Section: Tapinarofmentioning

confidence: 99%

Aryl hydrocarbon receptor/nuclear factor E2‐related factor 2 (AHR/NRF2) signalling: A novel therapeutic target for atopic dermatitis

Hwang

Newton

Hsiao

et al. 2022

Experimental Dermatology

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Aryl hydrocarbon receptor (AHR)/nuclear factor‐erythroid 2‐related factor 2 (NRF2) modulation is emerging as novel targets in the treatment of atopic dermatitis and other inflammatory skin disorders. Agonist activation of this pathway has downstream effects on epidermal barrier function, immunomodulation, oxidative stress reduction and cutaneous microbiome modulation. Tapinarof, a dual agonist of the AHR/NRF2 signalling pathway, has shown promise in phase 2 trials for atopic dermatitis. In this review, we summarize current knowledge of the AHR/NRF2 pathway and implications in skin disease process. We also review the therapeutic potential of current AHR agonists and propose future directions to address knowledge gaps.

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Section: Tapinarofmentioning

confidence: 99%

Aryl hydrocarbon receptor/nuclear factor E2‐related factor 2 (AHR/NRF2) signalling: A novel therapeutic target for atopic dermatitis

Hwang

Newton

Hsiao

et al. 2022

Experimental Dermatology

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“…The large-scale preparation of EDITS reported by Gao et al (47) was scaled to the research laboratory and provided sufficient EDITS for this study with the following modifications. The alkylation procedure used by Gao et al on methyl 3,5-dimethoxybenzoate gave the 4-isopropyl derivative (compound 1 in Fig.…”

Section: Liquid Chromatography-electrospray Ionization-tandem Mass Spmentioning

confidence: 99%

Death Becomes Them: Bacterial Community Dynamics and Stilbene Antibiotic Production in Cadavers of Galleria mellonella Killed by Heterorhabditis and Photorhabdus spp

Wollenberg

Jagdish

Slough

et al. 2016

Appl Environ Microbiol

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Insect larvae killed by entomopathogenic nematodes are thought to contain bacterial communities dominated by a single bacterial genus, that of the nematode's bacterial symbiont. In this study, we used next-generation sequencing to profile bacterial community dynamics in greater wax moth (Galleria mellonella) larvae cadavers killed by Heterorhabditis nematodes and their Photorhabdus symbionts. We found that, although Photorhabdus strains did initially displace an Enterococcus-dominated community present in uninfected G. mellonella insect larvae, the cadaver community was not static. Twelve days postinfection, Photorhabdus shared the cadaver with Stenotrophomonas species. Consistent with this result, Stenotrophomonas strains isolated from infected cadavers were resistant to Photorhabdus-mediated toxicity in solid coculture assays. We isolated and characterized a Photorhabdus-produced antibiotic from G. mellonella cadavers, produced it synthetically, and demonstrated that both the natural and synthetic compounds decreased G. mellonella-associated Enterococcus growth, but not Stenotrophomonas growth, in vitro. Finally, we showed that the Stenotrophomonas strains described here negatively affected Photorhabdus growth in vitro. Our results add an important dimension to a broader understanding of Heterorhabditis-Photorhabdus biology and also demonstrate that interspecific bacterial competition likely characterizes even a theoretically monoxenic environment, such as a Heterorhabditis-Photorhabdus-parasitized insect cadaver. IMPORTANCEUnderstanding, and eventually manipulating, both human and environmental health depends on a complete accounting of the forces that act on and shape microbial communities. One of these underlying forces is hypothesized to be resource competition. A resource that has received little attention in the general microbiological literature, but likely has ecological and evolutionary importance, is dead/decaying multicellular organisms. Metazoan cadavers, including those of insects, are ephemeral and nutrient-rich environments, where resource competition might shape interspecific macrobiotic and microbiotic interactions. This study is the first to use a next-generation sequencing approach to study the community dynamics of bacteria within a model insect cadaver system: insect larvae parasitized by entomopathogenic nematodes and their bacterial symbionts. By integrating bioinformatic, biochemical, and classic in vitro microbiological approaches, we have provided mechanistic insight into how antibiotic-mediated bacterial interactions may shape community dynamics within insect cadavers.

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“…We first assessed the cytotoxicity of the AmILs against HeLa cervical cancer cells and BEAS-2B lung epithelial cells using the MTS assay. In the MTS assays, and all other assays, the final concentration of DMSO in the assay media was ≤0.1 % as DMSO can affect the permeability of cell membranes at concentrations exceeding 2 %, [47][48][49] and 0.1 % DMSO has been used in previous studies 7,24 assessing the cytotoxicity of AmILs (see ESI † for full details of assay solutions). The AmILs produced dose-dependent reductions in cell viability and the dose-response curves (Fig.…”

Section: Amil Library Design and Effects On Cell Viabilitymentioning

confidence: 99%

Aromatic long chain cations of amphiphilic ionic liquids permeabilise the inner mitochondrial membrane and induce mitochondrial dysfunction at cytotoxic concentrations

et al. 2023

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Synthesis of Novel Drug Benvitimod

Cited by 5 publications

References 10 publications

Aryl hydrocarbon receptor/nuclear factor E2‐related factor 2 (AHR/NRF2) signalling: A novel therapeutic target for atopic dermatitis

Aryl hydrocarbon receptor/nuclear factor E2‐related factor 2 (AHR/NRF2) signalling: A novel therapeutic target for atopic dermatitis

Death Becomes Them: Bacterial Community Dynamics and Stilbene Antibiotic Production in Cadavers of Galleria mellonella Killed by Heterorhabditis and Photorhabdus spp

Aromatic long chain cations of amphiphilic ionic liquids permeabilise the inner mitochondrial membrane and induce mitochondrial dysfunction at cytotoxic concentrations

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