27876-94-4Relevant articles and documents
Trans-crocin 4 is not hydrolyzed to crocetin following i.p. administration in mice, while it shows penetration through the blood brain barrier
Karkoula, Evangelia,Lemonakis, Nikolaos,Kokras, Nikolaos,Dalla, Christina,Gikas, Evagelos,Skaltsounis, Alexios-Leandros,Tsarbopoulos, Anthony
, p. 62 - 72 (2018)
A novel, fit-for-purpose, highly sensitive, analytical UPLC-PDA methodology was developed and fully validated, according to ICH, FDA and EMA guidelines, for the rapid and accurate quantification of trans-crocin 4 (TC4) and crocetin (CRC) in mice plasma and brain after i.p. administration. A PDA based methodology shows a wider applicability as it is cost effective and can be easily and seamlessly adopted by the pharma industry. The separation of the analytes was performed on a C18 Hypersil Gold column with 2.5 min run time, employing the internal standard (ISTD) methodology. The two methods were successfully applied for the determination of CRC and TC4 in mouse plasma and brain after i.p. administration of TC4 (50 mg/kg) in a time range of 0–240 min. Due to the selection of i.p. administration route, the first-pass metabolism and/or gastric hydrolysis were bypassed, a fact that enhanced the bioavailability of TC4. Furthermore, TC4 was found to be capable of crossing the Blood Brain Barrier (BBB) and build up levels in the mouse brain, regardless of its highly hydrophilic character. CRC was not detected in any plasma or brain sample, although it has been reported that TC4 quickly hydrolyzes to CRC after p.o. administration. Therefore i.p. administration could be used in the case of TC4 for the accurate determination of its biological role. Overall, the developed methodology offers important information about the bioavailability of TC4 in mouse plasma and for the first time, demonstrates the ability of TC4 to penetrate the BBB and localize inside the brain.
Crocetin diester compound as well as preparation method and application thereof
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Paragraph 0012; 0024-0026, (2021/03/30)
The invention belongs to the technical field of pesticides, and provides a crocetin diester compound as well as preparation and application thereof in plant protection. It is found for the first timethat natural products crocin-1 and crocin-2 show higher anti-plant virus activity level than commercial variety virazole, can be used as a novel botanical pesticide or used as a lead compound for development, and used as the lead to design and synthesize the crocetin diester compound. An anti-plant virus activity test shows that all the compounds show activity on tobacco mosaic viruses, and particularly, the activity level of the crocetin di (4-fluorophenyl ethyl) ester is higher than that of a lead compound.
The crocetin single-glucuronic acid synthesis method (by machine translation)
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Paragraph 0035; 0036, (2018/12/14)
The invention relates to a metabolism in vivo product synthesis method. The method comprises the following steps: from traditional Chinese medicine fructus Gardeniae extracting the separated crocin, and crocin hydrolyzed into crocetin, to west pertains as substrate of synthetic west pertains to the fluoro, with fluoro and for D - glucuronic acid reaction to produce the target compound - crocetin single-glucuronic acid. The synthesis method principle is simple, easy to operate, low requirements on equipment, which can be widely applied. (by machine translation)
