The Chemo-Enzymatic Synthesis of 8,9-Dihydrohydroxysafflor Yellow A and Its Neuroprotective Effects against Cerebral Ischemia-Reperfusion Injury.

IF 6.2 1区农林科学 Q1 AGRICULTURE, MULTIDISCIPLINARY

Journal of Agricultural and Food Chemistry Pub Date : 2025-10-12 DOI:10.1021/acs.jafc.5c10765

Li Yang,Jiahui Li,Yong Chen,Xueming Wu,Rui Tan,Ren Xiang Tan

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Abstract

Hydroxysafflor yellow A (HSYA), the principal bioactive compound of safflower, is clinically used for ischemic cerebrovascular disease. However, the current sources of HSYA are limited and inadequate for clinical applications. In this study, we synthesized 8,9-dihydrohydroxysafflor yellow A (dh-HSYA), an analogue of HSYA, via a chemo-enzymatic approach and investigated its neuroprotective activity. The precursor phloretin-di-C-glucoside (PDG) was biosynthesized de novo in yeast, reaching a titer of 301.15 mg L-1. Furthermore, efficient production of PDG was achieved by supplementing with phloretin, resulting in a titer of 2.39 g L-1. Subsequently, dh-HSYA was synthesized from PDG via chemical oxidation, with a yield of 29.02%. The dh-HSYA exerted protective effects on BV2 and HT22 cells under oxygen-glucose deprivation/reoxygenation (OGD/R) conditions and attenuated brain injury in a rat model of middle cerebral artery occlusion/reperfusion (MCAO/R). This study provides a promising strategy for the sustainable production of dh-HSYA, which could potentially serve as a more scalable substitute for HSYA.

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化学酶法合成8,9-二羟基红花黄A及其对脑缺血再灌注损伤的神经保护作用。

羟基红花黄A （HSYA）是红花的主要生物活性化合物，临床上用于缺血性脑血管病。然而，目前HSYA的来源有限，不适合临床应用。本研究采用化学-酶促法合成了HSYA类似物- 8,9-二羟基红花黄A (dh-HSYA)，并对其神经保护活性进行了研究。在酵母中重新合成了前体褐皮素-二c -葡萄糖苷（PDG），滴度为301.15 mg L-1。此外，通过添加根皮素实现了PDG的高效生产，其滴度为2.39 g L-1。随后，以PDG为原料，通过化学氧化法合成了dh-HSYA，收率为29.02%。dhh - hsya对脑中动脉闭塞/再灌注（MCAO/R）模型大鼠缺氧-葡萄糖剥夺/再氧化（OGD/R）条件下BV2和HT22细胞及脑损伤有保护作用。该研究为可持续生产dh-HSYA提供了一个有希望的策略，它可能作为HSYA的更可扩展的替代品。

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来源期刊

Journal of Agricultural and Food Chemistry 农林科学-农业综合

CiteScore

9.90

自引率

8.20%

发文量

1375

审稿时长

2.3 months

期刊介绍： The Journal of Agricultural and Food Chemistry publishes high-quality, cutting edge original research representing complete studies and research advances dealing with the chemistry and biochemistry of agriculture and food. The Journal also encourages papers with chemistry and/or biochemistry as a major component combined with biological/sensory/nutritional/toxicological evaluation related to agriculture and/or food.