Delving into the Latest Updates on Erythromycin Salnacedin with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Actagen, Erythromycin salnacedin (USAN), Erythromycin salnacedin dihydrate

+ [5]

Target

50S subunit

Mechanism

50S subunit inhibitors(50S ribosomal subunit inhibitors)

Therapeutic Areas

Skin and Musculoskeletal Diseases

Active Indication-

Inactive Indication

Acne Vulgaris

Originator Organization

Genta, Inc.

Active Organization-

Inactive Organization

Genta, Inc.

Drug Highest PhaseDiscontinuedPhase 3

First Approval Date-

Regulation-

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Structure

Molecular FormulaC49H82N2O19S

InChIKeyWBZMMSVPKOTDDO-LJNQDACXSA-N

CAS Registry149908-23-6

Capsules (300 mg) containing Lactobacillus brevis G101 (1×10(10) CFU/individual) or maltodextrin (placebo) was orally administered in 30 respondents with self-recognized monosodium glutamate (MSG) symptom complex for 5 days and the rice with black soybean sauce containing 6 g MSG (RBSM) was ingested 30 min after the final administration. Thereafter, the MSG symptom complex (rated on a 5-point scale: 1, none; 5, strong) was investigated in a double blind placebo controlled study. The intensity of the MSG symptom complex was significantly reduced in respondents of the G101 intake group (2.87 ± 0.73) compared to that in those treated with the placebo (3.63 ± 1.03) (P = 0.0016). Respondents in the placebo group exhibited more of the various major conditions of the MSG symptom complex than in the G101 intake group. Although there was no significant difference in the appearance time of the MSG symptom complex between subjects orally administered G101 and those administered the placebo, its disappearance in < 3 h was observed in 69.9% of subjects in the G101 treatment group and in 38.0% of subjects in the placebo group (P = 0.0841).

CONCLUSIONS:

Oral administration of Lactobacillus brevis G101 may be able to reduce the intensity of the MSG symptom complex.

28 Nov 2014·Journal of microbiology and biotechnologyQ4 · ENGINEERING & TECHNOLOGY

Lactobacillus brevis G101 Inhibits the Absorption of Monosodium Glutamate in Mice

Q4 · ENGINEERING & TECHNOLOGY

Article

Author: Han, Myung Joo ; Kim, Dong-Hyun ; Jang, Se-Eun ; Kim, Se-Young

To evaluate the effect of Lactobacillus brevis G-101 on absorption of monosodium glutamate (MSG), we orally administered MSG with or without G-101 in mice and measured the maximum concentration (Cmax) and blood concentration curve (AUC) of MSG and γ- aminobutyric acid (GABA). Oral administration of G-101 (1 × 10(9) CFU/mouse) potently inhibited Cmax and AUC of MSG by 97.8% and 94.3%, respectively (p < 0.05), but increased those of GABA by 32.1% and 67.7%, respectively (p < 0.05). G-101 inhibited the absorption of MSG. These results suggest that G-101 may reduce the side effect of MSG by inhibiting the absorption of MSG.

01 Sep 2013·Journal of applied microbiologyQ3 · BIOLOGY

Lactobacillus brevis G-101 ameliorates colitis in mice by inhibiting NF-κB, MAPK and AKT pathways and by polarizing M1 macrophages to M2-like macrophages

Q3 · BIOLOGY

Article

Author: Hyam, S.R. ; Han, M.J. ; Kim, D.-H. ; Jang, S.-E. ; Lee, B.-G. ; Kim, S.-Y.

AIM:

We isolated Lactobacillus brevis G-101 from kimchi lactic acid bacteria (LAB) strains, which induced IL-10 expression in lipopolysaccharide (LPS)-stimulated peritoneal macrophages. To evaluate the inflammatory effect of G-101, we examined its inhibitory effect in 2,4,6-trinitrobenzene sulfonic acid (TNBS)-induced colitic mice.

MATERIALS AND RESULTS:

The colitic mice were prepared by intrarectal injection of TNBS. We measured intestinal mucosal cytokines by enzyme-linked immunosorbent assay; activation of transcription factors, by immunoblotting; and macrophage polarization markers, by real-time polymerase chain reaction. Of 200 LAB strains tested, Lact. brevis G-101 showed most potent activity for induction of IL-10 expression in LPS-stimulated peritoneal macrophages. However, it significantly inhibited the expression of TNF-α, IL-1β and IL-6 and the phosphorylation of IRAK1 and AKT, and activated NF-κB and MAPKs. Treatment with TNBS caused colon shortening; increased myeloperoxidase activity; and increased IL-1β, IL-6 and TNF-α expression in mice. Oral administration of Lact. brevis G-101 significantly inhibited these activities. Lactobacillus brevis G-101 inhibited TNBS-induced IRAK-1 phosphorylation and NF-κB activation, as well as the expression of COX-2 and iNOS. Lactobacillus brevis G-101 inhibited the expression of M1 macrophage markers, but increased the expression of M2 macrophages in the colons of TNBS-treated mice.

CONCLUSIONS:

Lactobacillus brevis G-101 may improve colitis by inhibiting the IRAK1/NF-κB, MAPK and AKT pathways and by polarizing M1 macrophages to M2-like macrophages.

SIGNIFICANCE AND IMPACT OF THE STUDY:

These results suggest that IL-10 expression-inducing LAB can ameliorate colitis by inhibiting NF-κB activation and macrophage polarization.

100 Deals associated with Erythromycin Salnacedin

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