Delving into the Latest Updates on Ecraprost with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Circulase, Ecraprost (USAN/INN)

+ [1]

Target

SLCO3A1

Mechanism

SLCO3A1 agonists(PGE1 agonists)

Therapeutic Areas

Cardiovascular Diseases

Active Indication-

Inactive Indication

Chronic Limb-Threatening IschemiaPeripheral Arterial Disease

Originator Organization

Mitsubishi Tanabe Pharma Corp.

Active Organization-

Inactive Organization

Mitsubishi Tanabe Pharma Corp.

AGC, Inc. (Japan)

Drug Highest PhaseDiscontinuedPhase 3

First Approval Date-

Regulation-

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Structure

Molecular FormulaC28H48O6

InChIKeyHITYEEHTEOQBAC-OSIGYOHNSA-N

CAS Registry136892-64-3

AbstractThere is a need for new natural products with antimicrobial activity to treat multidrug resistant bacteria that can cause human illness. Some of them are foodborne pathogens. Two different Gram-negative psychrotrophic strains were isolated from healthy trout river samples (Salmotrutta). Based on phenotypic characterization, proteomics, genotyping and phylogenetic analyses of 16 rRNA gene, strains TCPS12 and TCPS13 were identified as Shewanellabaltica and Pseudomonasfragi, respectively. Both of them produced an exopolysaccharide that showed antimicrobial activity against four foodborne pathogens. P. fragi supernatant (AS13) showed higher antimicrobial activity than S. baltica supernatant (AS12) against all tested pathogens. The stability of the antimicrobial activity of AS13 was assessed against Enterococcus faecalis ATCC 29212 under different conditions. This solution was stable when exposed for 30 min to temperatures ranging from 40 to 100 °C. In addition, it retained its activity within a pH range of 2–8 during 2 h of incubation, showing higher activity at pH 6. Serine proteases and α-amylase inactivated significantly the antimicrobial activity of AS13, suggesting that the active molecule could most likely be a glycoprotein. These products are interesting for their possible application as biopreservatives in the food industry.

01 Feb 2022·Journal of Hazardous MaterialsQ1 · ENVIRONMENTAL SCIENCE & ECOLOGY

Selenate increased plant growth and arsenic uptake in As-hyperaccumulator Pteris vittata via glutathione-enhanced arsenic reduction and translocation

Q1 · ENVIRONMENTAL SCIENCE & ECOLOGY

Article

Author: Tu, Shuxin ; Liu, Xue ; Chen, Jia-Yi ; Han, Ran ; Guan, Dong-Xing ; Ma, Lena Q ; Cao, Yue ; Ding, Song ; Dai, Zhi-Hua

The beneficial effects of selenium on As uptake and plant growth in As-hyperaccumulator Pteris vittata are known, but the associated mechanisms remain unclear. Here, we investigated the effects of selenate on arsenic accumulation by P. vittata under two arsenate levels. P. vittata plants were exposed to 13 (As₁₃) or 133 µM (As₁₃₃) arsenate and 5 µM selenate in 0.2-strength Hoagland solution. After 14 d of growth, plant biomass, Se and As content, As speciation, and malondialdehyde (MDA), glutathione reductase (GR), glutathione peroxidase (GPX), and glutathione (GSH and GSSG) levels were determined. The results show that selenate promoted P. vittata growth and increased As concentrations in the roots and fronds by 256% from 97 to 346 mg kg^-1 and 142% from 213 to 514 mg kg^-1 under As₁₃ treatment, and by 166% from 500 to 1332 mg kg^-1 and 534% from 777 to 4928 mg kg^-1 under As₁₃₃ treatment. In addition, selenate increased the glutathione content in P. vittata roots and fronds by 75-86% under As₁₃ treatment and 44-45% under As₁₃₃ treatment. Selenate also increased the GPX activity by 161-173%, and GR activity by 72-79% in P. vittata under As₁₃ and As₁₃₃ treatments. The HPLC-ICP-MS analysis indicated that selenate increased both AsIII and AsV levels in P. vittata, with AsIII/AsV ratio being lower in the roots and higher in the fronds, i.e., more AsIII was being translocated to the fronds. Taken together, our results suggest that, via GPX-GR mediated enhancement of GSH-GSSG cycle, selenate effectively increases plant growth and As uptake in P. vittata by improving AsV reduction in the roots and AsIII translocation from the roots to the fronds.

01 Jun 2019·SLAS DiscoveryQ4 · BIOLOGY

Novel 2-Benzoyl-6-(2,3-Dimethoxybenzylidene)-Cyclohexenol Confers Selectivity toward Human MLH1 Defective Cancer Cells through Synthetic Lethality

Q4 · BIOLOGY

Article

Author: Tan, Pei Jean ; Ng, Kwok Wen ; Song, Dedrick Soon Seng ; Hii, Ling Wei ; Shaari, Khozirah ; Patel, Vyomesh ; Abas, Faridah ; Leong, Sze Wei ; Chung, Felicia Fei-Lei ; Mai, Chun Wai ; Leong, Chee Onn

DNA mismatch repair (MMR) deficiency has been associated with a higher risk of developing colorectal, endometrial, and ovarian cancer, and confers resistance in conventional chemotherapy. In addition to the lack of treatment options that work efficaciously on these MMR-deficient cancer patients, there is a great need to discover new drug leads for this purpose. In this study, we screened through a library of commercial and semisynthetic natural compounds to identify potential synthetic lethal drugs that may selectively target MLH1 mutants using MLH1 isogenic colorectal cancer cell lines and various cancer cell lines with known MLH1 status. We identified a novel diarylpentanoid analogue, 2-benzoyl-6-(2,3-dimethoxybenzylidene)-cyclohexenol, coded as AS13, that demonstrated selective toxicity toward MLH1-deficient cancer cells. Subsequent analysis suggested AS13 induced elevated levels of oxidative stress, resulting in DNA damage where only the proficient MLH1 cells were able to be repaired and hence escaping cellular death. While AS13 is modest in potency and selectivity, this discovery has the potential to lead to further drug development that may offer better treatment options for cancer patients with MLH1 deficiency.

100 Deals associated with Ecraprost

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External Link

KEGG	Wiki	ATC	Drug Bank
D02723	-	-	DB16148

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Chronic Limb-Threatening Ischemia	Phase 3	US	Mitsubishi Tanabe Pharma Corp.	01 Jul 2001
Chronic Limb-Threatening Ischemia	Phase 3	GB	Mitsubishi Tanabe Pharma Corp.	01 Jul 2001
Peripheral Arterial Disease	Phase 3	-	AGC, Inc. (Japan)	-