AbstractBackground and AimsEndosidins are a group of low-molecular-weight compounds, first identified by ‘chemical biology’ screening assays, that have been used to target specific components of the endomembrane system. In this study, we employed multiple microscopy-based screening techniques to elucidate the effects of endosidin 5 (ES5) on the Golgi apparatus and the secretion of extracellular matrix (ECM) components in Penium margaritaceum. These effects were compared with those caused by treatments with brefeldin A and concanamycin A. Penium margaritaceum’s extensive Golgi apparatus and endomembrane system make it an outstanding model organism for screening changes to the endomembrane system. Here we detail changes to the Golgi apparatus and secretion of ECM material caused by ES5.MethodsChanges to extracellular polymeric substance (EPS) secretion and cell wall expansion were screened using fluorescence microscopy. Confocal laser scanning microscopy and transmission electron microscopy were used to assess changes to the Golgi apparatus, the cell wall and the vesicular network. Electron tomography was also performed to detail the changes to the Golgi apparatus.Key ResultsWhile other endosidins were able to impact EPS secretion and cell wall expansion, only ES5 completely inhibited EPS secretion and cell wall expansion over 24 h. Short treatments of ES5 resulted in displacement of the Golgi bodies from their typical linear alignment. The number of cisternae decreased per Golgi stack and trans face cisternae in-curled to form distinct elongate circular profiles. Longer treatment resulted in a transformation of the Golgi body to an irregular aggregate of cisternae. These alterations could be reversed by removal of ES5 and returning cells to culture.ConclusionsES5 alters secretion of ECM material in Penium by affecting the Golgi apparatus and does so in a markedly different way from other endomembrane inhibitors such as brefeldin A and concanamycin A.

01 Jan 2017·BioMed Research International

Hydroethanolic Extract of Strychnos pseudoquina Accelerates Skin Wound Healing by Modulating the Oxidative Status and Microstructural Reorganization of Scar Tissue in Experimental Type I Diabetes

Article

Author: Sarandy, Mariáurea M. ; Novaes, Rômulo D. ; Leite, João P. V. ; Gonçalves, Reggiani V. ; Xavier, Antônio A. ; Melo, Fabiana C. S. A. ; Vital, Camilo E.

The effect of topical application of ointment based on Strychnos pseudoquina hydroethanolic extract in the cutaneous wounds healing in diabetic rats was evaluated. Samples of S. pseudoquina were submitted to phytochemical prospection and in vitro antioxidant assay. Thirty Wistar rats were divided into 5 groups: Sal-wounds treated with 0.9% saline solution; VH-wounds treated with 0.6 g of lanolin cream (vehicle); SS-wounds treated with silver sulfadiazine cream (10 mg/g); ES5- and ES10-wounds treated with an ointment of S. pseudoquina extract, 5% and 10%, respectively. Fragments of wounds were removed for histological and biochemical analysis every 7 days during 21 days. ES showed equivalent levels per gram of extract of total phenols and flavonoids equal to 122.04 mg for TAE and 0.60 mg for RE. The chlorogenic acid was one of the major constituents. S. pseudoquina extract presented high antioxidant potential in vitro. ES5 and ES10 showed higher wound healing rate and higher amount of cells, blood vessels, and type III and I collagen. The oxidative stress markers were lower in the ES5 and ES10 groups, while the antioxidants enzymes levels were higher. Ointment based on S. pseudoquina extract promotes a fast and efficient cutaneous repair in diabetic rats.

01 Jun 2006·Experimental oncology

Antitumor activities of the four sesquiterpene lactones from Elephantopus scaber L.

Article

Author: Xu, G ; Liang, Q ; He, S ; Gong, Z ; Yu, W ; Xi, L

AIMTo evaluate antitumor activity of sesquiterpene lactones (scabertopin (ES-2), isoscabertopin (ES-3), deoxyelephantopin (ES-4), isodeoxyelephantopin (ES-5)) isolated from Elephantopus scaber L. in vitro and in vivo.METHODSSMMC-7721, Caco-2 and HeLa cell lines were treated with ES-2,3,4,5. Cell viability was determined by MTT assay. Agarose gel electrophoresis was used to detect DNA fragmentation. To evaluate in vivo antitumor activity of ES-4, experimental murine tumor model was used.RESULTSIt was shown that ES-2, ES-4, ES-5 exhibited significant antitumor effect in vitro in a concentration-dependent manner. However, the effect of ES-3 on the growth of tested cell lines was relatively weak. In HeLa cells exposed to ES-4 for 48 h, morphological changes and DNA ladder pattern evidencing on apoptosis were detected. ES-4 revealed in vivo antitumor activity.CONCLUSIONAntitumor activity of studied sesquiterpene lactones may be due, at least in part, to induction of apoptosis in vitro. ES-4 possesses also antitumor activity in vivo.

100 Deals associated with Equin

R&D Status

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Brain Cancer	Preclinical	GB	Incanthera Research & Development Ltd.	30 Jan 2022
Bladder Cancer	Preclinical	GB	Incanthera Research & Development Ltd.	-
Breast Cancer	Preclinical	GB	Incanthera Research & Development Ltd.	-
Colonic Cancer	Preclinical	GB	Incanthera Research & Development Ltd.	-
Liver Cancer	Preclinical	GB	Incanthera Research & Development Ltd.	-
Lung Cancer	Preclinical	GB	Incanthera Research & Development Ltd.	-
Melanoma	Preclinical	GB	Incanthera Research & Development Ltd.	-
Pancreatic Cancer	Preclinical	GB	Incanthera Research & Development Ltd.	-
Stomach Cancer	Preclinical	GB	Incanthera Research & Development Ltd.	-

Clinical Result

Indication

Phase

Evaluation

View All Results

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Deal

Boost your decision using our deal data.

view full example data

Core Patent

Boost your research with our Core Patent data.

view full example data

Clinical Trial

Identify the latest clinical trials across global registries.

view full example data

Approval

Accelerate your research with the latest regulatory approval information.

view full example data

Regulation

Understand key drug designations in just a few clicks with Synapse.

view full example data

Chat with Hiro

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis


No Data

Equin

Overview

Basic Info

Related

R&D Status

Clinical Result

Translational Medicine

Deal

Core Patent

Clinical Trial

Approval

Regulation