Delving into the Latest Updates on Crocin with Synapse

Overview

Basic Info

Drug Type

Chemical drugs

Synonyms

alpha- Crocin

Target

LIPE

Mechanism

Hormone sensitive lipase inhibitors, Lipid peroxidation inhibitors

Therapeutic Areas

Infectious DiseasesNervous System DiseasesCardiovascular Diseases+ [1]

Active Indication-

Inactive Indication

Lipid Metabolism DisordersMalariaStroke

Originator Organization

Kyushu University

Active Organization-

Inactive Organization

Kyushu UniversityKyung Hee UniversitySeoul National University Alumni

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC44H64O24

InChIKeySEBIKDIMAPSUBY-RTJKDTQDSA-N

CAS Registry42553-65-1

Background:Paraquat (PQ) is an effective herbicide which is widely used around the world to remove weeds in agriculture. As a water-soluble carotenoid, crocin is a pharmacologically active constituent of C. sativus L. (saffron).Objectives:In the present study, we investigated the effects of crocin-loaded niosomes (Cro-NIO) compared to free crocin on PQ-induced toxicity in the eukaryotic human embryonic kidney (HEK293) cell line.Methods:The Cro-NIO was synthesized and characterized. Cell viability was determined using the MTT assay in PQ-exposed HEK293 cell lines. The activities of biochemical markers were quantitatively determined to reveal the potential mechanism of PQ-induced oxidative stress in HEK293 cell line.Results:The particle size, zeta potential, polydispersity index (PDI), DL, and EE of Cro-NIO were 145.4 ± 19.5 nm, -22.3 ± 3.11 mV, 0.3 ± 0.03, 1.74 ± 0.01%, and 55.3 ± 7.1%, respectively. PQtreated HEK293 cell lines decreased cell viability. The results of oxidative status showed that PQ significantly could increase ROS accumulation, accompanied by a decreasing antioxidant defense system. However, treatment with Cro-NIO, compared to crocin, not only did dose-dependently improve the cell viability but also significantly attenuated the ROS accumulation and increased antioxidant markers.Conclusion:According to these results, Cro-NIO, compared to crocin, was superior to ameliorating PQ-induced cytotoxicity and oxidative damage in HEK293 cells.

01 Feb 2025·Food Chemistry

Augmenting antioxidative capacity of myosin and cytoprotective potential of myosin digestion products through the integration of crocin and crocetin: A comprehensive analysis via quantum chemical computing and molecular dynamics

Article

Author: Zhang, Chenxia ; Lou, Aihua ; Mo, Lan ; Wang, Shuai ; Luo, Jie ; Li, Maiquan ; Xue, Chaoyi ; Quan, Wei ; Shen, Qingwu ; Zhang, Jian ; Hu, Zhonghao ; Liu, Huixue

This study explores the binding properties of two important constituents from Crocus sativus L (crocin and crocetin) with myosin, examining their influence on antioxidant capacity in myosin and a grilled meat model. And their impact on cytoprotective potential of myosin digestion products was also assessed in Caco-2 cells. Crocin and crocetin exhibited discernible binding affinity to myosin via static quenching, which induced conformational alterations that bolstered the antioxidant capacity of myosin, preventing peroxidation, which also corroborated in a grilled meat model. Crocin resulted in greater enhancement of antioxidant capacity and binding affinity, as confirmed by quantum chemical calculations. Molecular dynamics simulations revealed the stable binding of crocin to GLU:272, GLU:606, GLN:628, and PHE:417 residues of myosin. In addition, crocin substantially enhanced the protective efficacy of myosin digestion products against H₂O₂-induced damage in Caco-2 cells by upregulating superoxide dismutase and GSH-Px and simultaneously downregulating reactive oxygen species and malondialdehyde levels.

01 Feb 2025·Journal of Chromatography B

Evaluation of the effect of Ela tablets in the treatment of diabetic nephropathy based on rat experiments and screening strategy for quality markers of Ela tablets targeting aldose reductase

Article

Author: Xin, Xuelei ; Keremu, Aizaiti ; Aisa, Haji Akber ; Guo, Shunan ; Maiwulanjiang, Maitinuer ; He, Fei ; Hu, Miao

Ela tablets (ALP) is a traditional Uyghur medicinal formulation comprising 9 herbs. Clinical applications have demonstrated its potential in treating diabetic nephropathy (DN). However, its specific medicinal effects and pharmacodynamic components have not been elucidated. This research aims to investigate the efficacy of ALP in treating DN and to explore the quality markers (Q-markers) for its exertion of efficacy. Using the UHPLC-Q-Orbitrap HRMS technique, a total of 60 compounds were identified within ALP. Animal experiments were conducted to investigate the effect of ALP intervention at doses of 80, 160, and 320 mg/kg in Sprague-Dawley rats. Then, fingerprints of ten batches of ALP extracts were established using UPLC-DAD. Spectrum-effect relationship analysis of these fingerprints and aldose reductase (AR) activity was conducted by chemometric analysis methods. The results were further validated by molecular docking and cellular experiments. The animal experiments indicated that ALP had a therapeutic effect on DN. Specifically, ALP reduced biochemical indexes such as serum creatinine (SCr), 24-hour urinary total protein (24 h UTP), uric acid (UA), blood urea nitrogen (BUN), triglycerides (TG), and total cholesterol (TC). ALP stabilized body weight and fasting blood glucose, enhanced the antioxidant capacity of kidneys, and improved renal pathology. Comprehensive analysis indicated that crocin-I and gallic acid may be used as Q-markers for ALP. In summary, ALP has been identified as a treatment for DN, and gallic acid and crocin-I can be used as its Q-markers.

100 Deals associated with Crocin

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Crocin	-	DB11874

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Lipid Metabolism Disorders	Preclinical	-	Kyung Hee University	-
Lipid Metabolism Disorders	Preclinical	-	Kyushu University	-
Lipid Metabolism Disorders	Preclinical	-	Seoul National University Alumni	-
Malaria	Preclinical	-	Kyushu University	-
Malaria	Preclinical	-	Seoul National University Alumni	-
Malaria	Preclinical	-	Kyung Hee University	-
Stroke	Preclinical	-	Kyushu University	-
Stroke	Preclinical	-	Kyung Hee University	-
Stroke	Preclinical	-	Seoul National University Alumni	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


IRCT20130418013058N7 (P-47, ESMO_GI2023)	Phase 2	Esophageal Squamous Cell Carcinoma Adjuvant	59	Crocin	(armyrgcwrl) = ztebztybve qrhpbzbddm (cxljjcpynq ) View more	Negative	01 Jul 2023
				Placebo	(armyrgcwrl) = lqbcsvtawo qrhpbzbddm (cxljjcpynq ) View more
IRCT20160706028815N4 (ESMO2021)	Phase 2/3	Breast Cancer Her2/neu positive \| triple-negative	-	Crocin	apsdvexjyi(xlrwxmxjqp) = wyvmyxcmll iwqphrmcbv (edozyijsit )	-	16 Sep 2021
				Placebo	apsdvexjyi(xlrwxmxjqp) = phsroaemzh iwqphrmcbv (edozyijsit )
WSC2015	Not Applicable	-	-	Crocin	gxdqrupkok(udehvnbuvc) = oxzgeyxvvh oyhvbbnitj (elmizbkiim ) View more	Positive	26 Feb 2015
				Crocetin	dslosznhoz(siayxbhmfq) = wsmlcsshlz agfgeuurku (rcfbugfaap )