Steroidal hydrazones as antimicrobial agents: biological evaluation and molecular docking studies.

Most of pharmaceutical agents display several or even many biological activities. It is obvious that testing even one compound for thousands of biological activities is a practically not reasonable task. Therefore, computer-aided prediction is the method of choice for the selection of the most promising bioassays for particular compounds.

Antimicrobial Activity of Catechol-Containing Biopolymer Poly[3-(3,4-dihydroxyphenyl)glyceric Acid] from Different Medicinal Plants of Boraginaceae Family.

This study reports the antimicrobial activities of the biopolymers poly[3-(3,4-dihydoxyphenyl)glyceric acid] (PDHPGA) and poly[2-methoxycarbonyl-3-(3,4-dihydroxyphenyl)oxirane] (PMDHPO), extracted from the six plants of Boraginaceae family: (), (), and (), (), (), and () collected in various parts of Georgia. The study revealed that the antibacterial activities were moderate, and biopolymers from only three plants showed activities against all tested bacteria. Biopolymers from stems as well as and did not show any activity except low activity against a resistant strain, which was the most resistant among all three resistant strains.

Antimicrobial Activity of Some Steroidal Hydrazones.

Twelve steroid based hydrazones were in silico evaluated using computer program PASS as antimicrobial agents. The experimental evaluation revealed that all compounds have low to moderate antibacterial activity against all bacteria tested, except for with MIC at a range of 0.37-3.

Caffeic and 3-(3,4-dihydroxyphenyl)glyceric acid derivatives as antimicrobial agent: biological evaluation and molecular docking studies.

Herein we report the evaluation of the antimicrobial activity of some previously synthesized 3-(3,4-dihydroxyphenyl)glyceric acid in benzylated and in free 3,4 hydroxy groups in catechol moiety along with some caffeic and 3-(3,4-dihydroxyphenyl)glyceric acid amides using the microdilution method. The evaluation revealed that compounds showed in general moderate to low activity with MIC in range of 0.36-4.

Enzymatic Synthesis and Antimicrobial Activity of Oligomer Analogues of Medicinal Biopolymers from Comfrey and Other Species of the Boraginaceae Family.

This study reports the first enzymatic synthesis leading to several oligomer analogues of poly[3-(3,4-dihydroxyphenyl)glyceric acid]. This biopolymer, extracted from plants of the Boraginaceae family has shown a wide spectrum of pharmacological properties, including antimicrobial activity. Enzymatic ring opening polymerization of 2-methoxycarbonyl-3-(3,4-dibenzyloxyphenyl)oxirane (MDBPO) using lipase from leads to formation of poly[2-methoxycarbonyl-3-(3,4-dibenzyloxyphenyl)oxirane] (PMDBPO), with a degree of polymerization up to 5.

Novel antimicrobial agents' discovery among the steroid derivatives.

Fourteen steroid compounds were in silico evaluated using computer program PASS as antimicrobial agents. The experimental studies evaluation revealed that all compounds have good antibacterial activity with MIC at range of 0.003-0.

New Caffeic Acid Derivatives as Antimicrobial Agents: Design, Synthesis, Evaluation and Docking.

Background: Phenolic acids (caffeic-, ferulic and p-coumaric acid) are widely distributed in the plant kingdom and exhibit broad spectrum of biological activities, including antimicrobial activity.

Objective: The goal of this paper is the synthesis of some caffeic acid derivatives selected based on computer-aided predictions and evaluate their in vitro antimicrobial properties against Gram positive and Gram negative bacteria and also a series of fungi.

Methods: In silico prediction of biological activity was used to identify the most promising structures for synthesis and biological testing, and the putative mechanisms of their antimicrobial action.

Microbial biogeography of the transnational fermented milk matsoni.

The fermented milk matsoni is a traditional, national food product of both Georgia and Armenia. Little is known about the effects of biogeography and milk type on the microbial biodiversity of matsoni or the fungal composition of matsoni fermentations. High-throughput marker-gene sequencing was used to survey the bacterial and fungal communities of matsoni from different milk types and regions throughout Armenia and Georgia.

[Development of technology for the substance of poly[3-(3,4-dihydroxyphenyl) glyceric acid] from Symphytum asperum].

Comfrey (Symphytum L.) is used to treat bone fractures, tendon injuries, ulcer lesions of gastrointestinal tract. It promotes wound healing, accelerates exudates resorption in lungs and reduces joints' inflammation.

Poly[3-(3, 4-dihydroxyphenyl) glyceric acid] from Comfrey exerts anti-cancer efficacy against human prostate cancer via targeting androgen receptor, cell cycle arrest and apoptosis.

The major obstacles in human prostate cancer (PCA) treatment are the development of resistance to androgen ablation therapy leading to hormone-refractory state and the toxicity associated with chemotherapeutic drugs. Thus, the identification of additional non-toxic agents that are effective against both androgen-dependent and androgen-independent PCA is needed. In the present study, we investigated the efficacy of a novel phytochemical poly[3-(3, 4-dihydroxyphenyl)glyceric acid] (p-DGA) from Caucasian species of comfrey (Symphytum caucasicum) and its synthetic derivative syn-2, 3-dihydroxy-3-(3, 4-dihydroxyphenyl) propionic acid (m-DGA) against PCA LNCaP and 22Rv1 cells.

Poly[3-(3,4-dihydroxyphenyl)glyceric acid] from Anchusa italica roots.

Elucidation of the main structural unit of a water-soluble, high-molecular weight preparation from the crude polysaccharides of Anchusa italica Retz. roots has been carried out. According to 13C NMR, 1H NMR and 2D heteronuclear 1H/13C HSQC spectral data, the main structural element of the high-molecular, water-soluble preparation was a regularly substituted polyoxyethylene chain, namely poly[oxy-1-carboxy-2-(3,4-dihydroxyphenyl)ethylene].

Enantioselective synthesis and antioxidant activity of 3-(3,4-dihydroxyphenyl)-glyceric acid--basic monomeric moiety of a biologically active polyether from Symphytum asperum and S. caucasicum.

The racemic and enantioselective synthesis of a novel glyceric acid derivative, namely, 2,3-dihydroxy-3-(3,4-dihydroxyphenyl)-propionic acid as well as the antioxidant activities is described. The virtually pure enantiomers, (+)-(2R,3S)-2,3-dihydroxy-3-(3,4-dihydroxyphenyl)-propionic acid and (-)-(2S,3R)-2,3-dihydroxy-3-(3,4-dihydroxyphenyl)-propionic acid were synthesized for the first time via Sharpless asymmetric dihydroxylation of trans-caffeic acid derivatives using the enantiocomplementary catalysts, (DHQD)(2)-PHAL and (DHQ)(2)-PHAL. The determination of enantiomeric purity of the novel chiral glyceric acid derivatives was performed by high-performance liquid chromatographic techniques on the stage of their alkylated precursors.

Composition of intracellular soluble proteins in Mycobacterium "rubrum" and its mutants.

The composition of intracellular soluble proteins in a parental strain of Mycobacterium "rubrum" and its mutants was studied by polyacrylamide gel gradient electrophoresis. The composition of the protein fractions of the parental and the mutant strains was similar, they differed in one protein only. The presence of a 60 kDa protein should be stressed since its increased amount may be connected with a different intensity of the production of pigments in the strains studied.

[Kinetics of growth and development of Mycobacterium rubrum under conditions of periodic culturing].

The kinetics of growth, development, carotenogenesis and changes in the composition of the reaction medium were studied in the course of Mycobacterium rubrum batch cultivation in synthetic and complex media. The culture growth was found to be composed of five phases in the synthetic medium and of four phases in the complex medium. When the culture was grown in the synthetic medium, the phenomenon of distinct diauxy was recorded by changes in the specific growth rate as well as the economic and metabolic coefficients.