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Overview

Tags

Endocrinology and Metabolic Disease

Nervous System Diseases

Neoplasms

Synthetic peptide

Small molecule drug

Disease domain score

A glimpse into the focused therapeutic areas

Technology Platform

Most used technologies in drug development

Targets

Most frequently developed targets

Disease Domain	Count

Endocrinology and Metabolic Disease	2
Nervous System Diseases	1
Neoplasms	1

Top 5 Drug Type	Count

Synthetic peptide	1
Small molecule drug	1

Top 5 Target	Count

PPAR x RXRA	1
SSTR(Somatostatin receptor)	1

The present study was aimed to evaluate the anticonvulsant activity of acteoside and explore its mechanism of action. Initially, the acteoside was evaluated in maximal electroshock (MES) and pentylenetetrazole (PTZ)-induced convulsions, and later it was evaluated against N-methyl-D-aspartic acid (NMDA)-induced mortality in Swiss albino mice. Based on the response in these models, further evaluations were performed to explore the mechanism of action. In the results, the acteoside (10, 25, and 50 mg/kg) has shown significant anticonvulsant activity in the PTZ model (p < 0.01 for all doses); however, there was no protection observed in MES and NMDA models. Therefore, further mechanism-based studies were performed on the PTZ model, and the outcomes have revealed that there was a significant reduction in GABA (p < 0.01 for both regions) and elevation of glutamate (p < 0.01 for both regions) in the cortex and hippocampus regions of PTZ-treated animals. Further, the antioxidant levels (SOD, catalase, GPx, GR, GSH, LPO) were altered significantly (p < 0.01 for all parameters), with reduced GABA_A mRNA levels (p < 0.01) in the PTZ control compared with the normal control. Interestingly, co-administration of acteoside (25 mg/kg) (p < 0.01 for all parameters) has restored all the PTZ-induced alterations compared to PTZ-control. Moreover, the anti-PTZ action of acteoside was completely blocked in the presence of flumazenil, and thus confirmed the GABAergic mechanism behind the anticonvulsant activity of acteoside. Besides, actophotometer and rotarod tests have confirmed that the acteoside is free from central side effects like motor incoordination and locomotor deficits.

01 Nov 2020·Drug and Chemical ToxicologyQ4 · MEDICINE

Effect of endosulfan and bisphenol A on the expression of SUMO and UBC9

Q4 · MEDICINE

Article

Author: Yarahalli Jayaram, Vidhya ; Reddy, Divijendra ; Baggavalli, Somesh ; Sistla, Srinivas ; Malempati, Rajyalakshmi

This study was designed to investigate possible interference of Xenobiotics with SUMOylation in eukaryotic cells. To begin with, we docked 71 chemical structures from PubChem with human SUMO1 and UBC9 protein structures using Auto Dock 4.2 and Hex 6.3 and selected five compounds for binding studies in Surface Plasmon Resonance (SPR) with human SUMO1. In SPR studies, only endosulfan showed binding to SUMO1 (K_d1.313 × 10-4 M). Further, we treated HePG2 and differentiated 3T3-L1 cells with endosulfan/bisphenol A/perfluorooctanoic acid (PFOA) to test induction of oxidative stress and SUMO isoform/UBC9 expression. Treatment with these compounds resulted in higher levels of nitric oxide (NO), NOS2A mRNA, and reactive oxygen species (ROS) associated with decreased NADPH levels. Additionally, treatment with these chemicals resulted in elevated mRNA levels of IL-6 and IL-1β in 3T3-L1 cells. In HePG2 cells, endosulfan treatment resulted in elevated mRNA levels of SUMO1, 3 and UBC9, whereas, treatment with bisphenol A resulted in increased mRNA of SUMO2, 3 and UBC9. Treatment with PFOA resulted in elevated mRNA levels of SUMO2. Apart from influencing the gene expression, endosulfan caused decrease in SUMO1-Sumoylation of few proteins. We propose that one reason for the severe health consequences of exposure to endosulfan/bisphenol could be due to induction of oxidative stress and modulation in SUMO and UBC9 gene expression.

01 Aug 2020·Pharmacological ReportsQ4 · MEDICINE

Correction to: Efficacy and safety of inhalation budesonide in the treatment of pediatric asthma in the emergency department: a systematic review and meta-analysis

Q4 · MEDICINE

Article

Author: Viswanatha, Gollapalle Lakshminarayanashastry ; Shylaja, Hanumanthappa ; Prasad, Nunna Bheema Lingeswara ; Venkataranganna, Marikunte Venkatanarasappa ; Nandakumar, Krishnadas

The original version of this article, published on 29 March 2020 unfortunately contains a mistake.

100 Deals associated with Connexios Life Sciences Pvt Ltd.

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100 Translational Medicine associated with Connexios Life Sciences Pvt Ltd.

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Pipeline

Pipeline Snapshot as of 26 Nov 2024

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

Preclinical

1

Phase 1 Clinical

Other

12

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Current Projects

Drug(Targets)	Indications	Global Highest Phase

Octreotide oral film(Connexios Life Sciences Pvt Ltd.) ( SSTR )	Malignant Carcinoid Syndrome More	Phase 1
CNX-013 ( PPAR x RXRA )	Diabetes Mellitus More	Preclinical
CNX-018	Diabetes Mellitus, Type 2 More	Pending
CNX-015	Lipid Metabolism Disorders More	Pending
CDR-267F018	Lipid Metabolism Disorders More	Pending