Re-discovery of MS-347a as a fungicide candidate through a new drug discovery platform with a multidrug-sensitive Saccharomyces cerevisiae screening system and the introduction of a global secondary metabolism regulator, laeA gene

Bioscience Biotechnology and Biochemistry, Journal Year: 2024, Volume and Issue: 88(7), P. 824 - 829

Published: April 25, 2024

ABSTRACT We found that the culture broth of fungi showed anti-fungal activity against multidrug-sensitive budding yeast. However, we could not identify compound due to small quantity. Therefore, attempted increase productivity target by introduction a global secondary metabolism regulator, laeA strain, which led successful isolation 10-folds greater amount MS-347a (1) than Aspergillus sp. FKI-5362. Compound 1 was effective Candida albicans and detailed remains unverified. After our screening, inhibit growth broad plant pathogenic fungal species belonging Ascomycota. It is noteworthy little insecticidal silkworms, suggesting its selective biological fungi. Our study implies combination strategy yeast useful for new drug discovery.

Language: Английский

---

Corey–Fuchs reaction enabled synthesis of natural products: a review

RSC Advances, Journal Year: 2025, Volume and Issue: 15(11), P. 8121 - 8155

Published: Jan. 1, 2025

Corey–Fuchs reaction is a two-step involving the synthesis of terminal alkyne from aldehyde. It pivotal organic reaction, plays significant role in various natural products and their derivatives.

Language: Английский

---

Synthesis and biological evaluation of MS-347a derivatives against plant pathogenic fungi based on a strategy of <i>laeA</i> gene introduction

Nippon Nōyaku Gakkaishi, Journal Year: 2024, Volume and Issue: 49(4), P. 224 - 231

Published: Nov. 20, 2024

Our group previously identified MS-347a (1) as a new fungicide candidate from the culture broth of mutant strain, Aspergillus sp. KTF-0058, which had laeA gene inserted. This strain was able to produce sufficient supply 1, allowing for its use investigate structure-activity relationship. To this end, we synthesized 11 derivatives and evaluated their antifungal activity. Among these derivatives, aldehyde derivative exhibited superior potency compared some acyl were maintain activity 1 despite significant structural changes. From results, it is found that one most promising fungicidal candidates, introduction groups could be utilized create chemical probes target-identification experiments.

Language: Английский

---

Synthesis, Structural Validation, and SAR of Antifungal Fusaramin

Synfacts, Journal Year: 2024, Volume and Issue: 20(03), P. 0311 - 0311

Published: Feb. 14, 2024

Key words structure–activity relationship (SAR) - antimicrobial antifungal

Language: Английский

---

Discovery of an anti-malarial compound, burnettiene A, with a multidrug-sensitive Saccharomyces cerevisiae screening system based on mitochondrial function inhibitory activity

Bioscience Biotechnology and Biochemistry, Journal Year: 2024, Volume and Issue: 88(10), P. 1212 - 1216

Published: July 9, 2024

In this paper, we describe our discovery of burnettiene A (1) as an antimalarial compound from the culture broth Lecanicillium primulinum (current name: Flavocillium primulinum) FKI-6715 strain utilizing original multidrug-sensitive yeast system. This polyene-decalin polyketide natural product was originally isolated antifungal active Aspergillus burnettii. However, activity 1 has been revealed in only one fungal species, and mechanism action remains unknown. After validation mitochondrial function inhibitory 1, envisioned a new drug platform based on activity. We evaluated showed against Plasmodium falciparum FCR3 (chloroquine sensitive) K1 resistant). Our study utility screening system for candidates.

Language: Английский

---

Synthesis and biological evaluation of burnettiene A derivatives enabling discovery of novel fungicide candidates

Nippon Nōyaku Gakkaishi, Journal Year: 2024, Volume and Issue: unknown

Published: Jan. 1, 2024

An antifungal polyene-decalin polyketide natural product, burnettiene A (

Language: Английский

---