Gastroprotective [6]-Gingerol Aspirinate as a Novel Chemopreventive Prodrug of Aspirin for Colon Cancer

Zhu, Yingdong; Wang, Fang; Zhao, Yantao; Wang, Pei; Sang, Shengmin

doi:10.1038/srep40119

Cited by 20 publications

(14 citation statements)

References 33 publications

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“…In particular, clinical studies have provided evidence that patients with IBD are at a higher risk of developing colorectal cancer (Itzkowitz and Yio, ; Samadder et al ., ). It is worth noting the anticancer activity of gingerols (Lv et al ., ; Zhu et al ., ) may provide insight into potential prevention of colorectal cancer. Hence, 6‐gingerol, 8‐gingerol, and 10‐gingerol represent promising alternative drug candidates in the therapy of colitis and prevention of IBD‐related colorectal cancer.…”

Section: Discussionmentioning

confidence: 99%

Therapeutic Effects of 6‐Gingerol, 8‐Gingerol, and 10‐Gingerol on Dextran Sulfate Sodium‐Induced Acute Ulcerative Colitis in Rats

Zhang

Gao

et al. 2017

Phytotherapy Research

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Ulcerative colitis is one of the most common types of inflammatory bowel disease and is multifactorial and relapsing. 6-Gingerol, a component of gingerols extracted from ginger (Zingiber officinale), has been reported to improve ulcerative colitis. The present study aims to investigate the therapeutic efficacy of two analogous forms of 6-gingerol, 8-gingerol, and 10-gingerol, on ulcerative colitis. Colitis was induced in rats through consumption of 5% (w/v) dextran sulfate sodium drinking water for 7 consecutive days. 6-Gingerol, 8-gingerol, and 10-gingerol were then given intraperitoneally at doses of 30 mg kg d for another 7 days, respectively. Body weight change, disease activity index, inflammatory cytokines, and oxidative stress indices were measured, and the colonic tissue injuries were assessed macroscopically and histopathologically. Results showed that all three gingerols attenuated colitic symptoms evoked by dextran sulfate sodium, significantly elevated superoxide dismutase activity, decreased malondialdehyde levels and myeloperoxidase activity in the colon tissue, and markedly reduced the content of tumor necrosis factor alpha and Interleukin 1 beta in the serum. Histological observations showed that all three gingerols obviously accelerated mucosal damage healing. It is concluded that 6-gingerol, 8-gingerol, and 10-gingerol, the three analogues, have a strong and relatively equal efficacy in the treatment of colitis. Copyright © 2017 John Wiley & Sons, Ltd.

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Section: Discussionmentioning

confidence: 99%

Therapeutic Effects of 6‐Gingerol, 8‐Gingerol, and 10‐Gingerol on Dextran Sulfate Sodium‐Induced Acute Ulcerative Colitis in Rats

Zhang

Gao

et al. 2017

Phytotherapy Research

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“…Research suggested that ginger constituents ameliorate low-dose aspirin-induced gastric ulceration in the gastrointestinal tract. Therefore, a novel prodrug of aspirin designed as 6-gingerol aspirinate reduced acute stomach injury induced by aspirin in mice [ 257 ]. It is proposed that the anti-ulcer and healing capacities of zinger, are achieved due to its strong thromboxane synthetase feature, inhibition of K + -ATPase, gastric H + , and H. pylori growth by phenolic antioxidants [ 252 ].…”

Section: Plant Mediated Treatment Of Ulcer and Inflammatory Diseasesmentioning

confidence: 99%

Therapeutic Promises of Medicinal Plants in Bangladesh and Their Bioactive Compounds against Ulcers and Inflammatory Diseases

Ahmed

Rabbee

Roy

et al. 2021

Plants

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When functioning properly, the stomach is the center of both physical and mental satisfaction. Gastrointestinal disorders, or malfunctioning of the stomach, due to infections caused by various biological entities and physiochemical abnormalities, are now widespread, with most of the diseases being inflammatory, which, depending on the position and degree of inflammation, have different names such as peptic or gastric ulcers, irritable bowel diseases, ulcerative colitis, and so on. While many synthetic drugs, such as non-steroidal anti-inflammatory drugs, are now extensively used to treat these diseases, their harmful and long-term side effects cannot be ignored. To treat these diseases safely and successfully, different potent medicinal plants and their active components are considered game-changers. In consideration of this, the present review aimed to reveal a general and comprehensive updated overview of the anti-ulcer and anti-inflammatory activities of medicinal plants. To emphasize the efficacy of the medicinal plants, various bioactive compounds from the plant extract, their experimental animal models, and clinical trials are depicted.

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“…阿司匹林酰氯与 [70] ; 与熊果酸取代制得的衍生物 83 对于 MCF-7 细胞的 IC 50 值为 70 μmol•L -1 , 活性明显高于阿司匹林 [71] ; 与薯蓣皂苷元发生取代制得衍生物 84 [72] , 该化合物能明显抑制血栓的形成, 其对血小板的抑制率为(29.42±3.1)%, 与阿司匹林相当 [73] . 此外, 衍生物 84 还具有抗炎活性, 其在剂量为 21.9 mg/kg 时对小鼠耳朵的肿胀抑制率为 18.03%, 并随剂量的增加抑制率不断上涨 [72] .…”

Section: 类似地在水杨醛和阿司匹林的基础上合成了四种unclassified

Advances in the Study of Structural Modification of Aspirin and Their Biological Activities

Zhang¹,

Gao²,

Zhang³

et al. 2020

Chin. J. Org. Chem.

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Aspirin (ASP), the first synthetic drug, is widely used as a non steroidal anti-inflammatory drug. It displays a variety of biological activities, such as anti-thrombosis, anti-inflammatory, anti-tumor, etc. A lot of works about the synthesis and related activity evaluation of its derivatives were reported. There are four kinds of derivatization methods: skeleton derivatization, prodrug derivatization, twin derivatization and metal coordination derivatization. According to the different modification sites, skeleton derivatization could be further divided into C(1)-COOH site modification, C(1)-COOH site and C(2)-OAc site simultaneous modification, C(2)-OAc site modification and benzene ring modification. NO-ASP is the main method to prepare antithrombotic derivatives, and metal coordination modification is the main synthesis scheme of anticancer derivatives. The structure modification and bioactivity research of aspirin in recent twenty years and the synthetic routes of 353 aspirin derivatives and the pharmacological activities of some derivatives are described, which provides a reference for the further development of aspirin derivatives.

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Gastroprotective [6]-Gingerol Aspirinate as a Novel Chemopreventive Prodrug of Aspirin for Colon Cancer

Cited by 20 publications

References 33 publications

Therapeutic Effects of 6‐Gingerol, 8‐Gingerol, and 10‐Gingerol on Dextran Sulfate Sodium‐Induced Acute Ulcerative Colitis in Rats

Therapeutic Effects of 6‐Gingerol, 8‐Gingerol, and 10‐Gingerol on Dextran Sulfate Sodium‐Induced Acute Ulcerative Colitis in Rats

Therapeutic Promises of Medicinal Plants in Bangladesh and Their Bioactive Compounds against Ulcers and Inflammatory Diseases

Advances in the Study of Structural Modification of Aspirin and Their Biological Activities

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