Effects of Thymoquinone on radiation enteritis in mice

Hou, Qinlian; Liu, Linlin; Dong, Yinping; Wu, Jing; Du, Liqing; Dong, Hao; Li, Deguan

doi:10.1038/s41598-018-33214-3

Cited by 112 publications

(17 citation statements)

References 42 publications

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“…TQ is also reported in other plants such as Nepeta Leucophylla, Tetraclinis articulata, Juniperus Cedrus, Callitris quadrivalvis, Monarda fistulosa etc. It has also been reported in genus Tetraclinis, Cupressus, and Juniperus of the Cupressaceae family (Hou et al, 2018).…”

Section: Source and Occurrence Of Thymoquinonementioning

confidence: 74%

“…Besides Ranunculaceae, where only minute quantities of TQ are found, its presence has also been confirmed in other genera of Laminaceae family like Agastache, Coridothymus, Monarda, Mosla, Origanum, Satureja, Thymbra, and Thymus (Hou et al, 2018) . In plants, TQ is found along with its dimeric and reduced forms dithymoquinone and thymohydroquinone, the latter being a compound with significant biological activities (Imran et al, 2018).…”

Section: Source and Occurrence Of Thymoquinonementioning

confidence: 83%

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Thymoquinone (2-Isopropyl-5-methyl-1, 4-benzoquinone) as a chemopreventive/anticancer agent: Chemistry and biological effects

Ahmad

Mishra

Vyawahare

et al. 2019

Saudi Pharmaceutical Journal

122

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Section: Source and Occurrence Of Thymoquinonementioning

confidence: 74%

Section: Source and Occurrence Of Thymoquinonementioning

confidence: 83%

Thymoquinone (2-Isopropyl-5-methyl-1, 4-benzoquinone) as a chemopreventive/anticancer agent: Chemistry and biological effects

Ahmad

Mishra

Vyawahare

et al. 2019

Saudi Pharmaceutical Journal

122

View full text Add to dashboard Cite

show abstract

“…Interestingly, there is a positive correlation between the number of Paneth cells and the number of Lgr5 + stem cells [ 39 ]. The hyperplastic cells of the small intestinal epithelium can be identified due to the expression of the proliferation marker protein Ki67 [ 40 ]. We found that HL-003 significantly prevented the irradiation-induced decrease in Lgr5 + ISCs, Ki67 + TACs, and lysozyme + Paneth cells, and it promoted the regeneration, differentiation, and proliferation of intestinal epithelial cells and maintained homeostasis of the intestinal epithelium.…”

Section: Discussionmentioning

confidence: 99%

Preclinical Evaluation of Safety, Pharmacokinetics, Efficacy, and Mechanism of Radioprotective Agent HL‐003

Liu

Miao

Tian

2021

Oxidative Medicine and Cellular Longevity

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Amifostine is a radioprotector with high efficacy but poor safety, short half-life, no oral formulation, and poor compliance, which limits its application. With the increasing risk of exposure to radiation, the development of new radioprotective agents is critical. We previously synthesized a new amifostine derivative, the small molecule compound HL-003. In this study, we focused on evaluating the radioprotective properties of HL-003. Using the in vitro 2,2-diphenyl-1-picrylhydrazyl assay, we initially confirmed HL-003 as a strong antioxidant and demonstrated that its free radical scavenging activity was stronger than that of amifostine. Then, we performed an acute toxicity test, a 28-day toxicity test, a 30-day survival rate test, and a pharmacokinetic study, all of which provided aggregate evidence that HL-003 functioned as a small molecule radioprotector with high efficacy, a favorable safety profile, a long half-life, and oral administration. The intestinal radioprotective mechanism of HL-003 was explored in male C57 mice after abdominal irradiation by analyzing intestinal tissue samples with hematoxylin-eosin staining, immunohistochemistry, TUNEL staining, and immunofluorescence detection. The results showed that HL-003 protected intestinal DNA from radiation damage and suppressed the expression of phosphorylated histone H2AX, phosphorylated p53, and the apoptosis-related proteins caspase-8 and caspase-9, which contributed to maintaining the normal morphology of the small intestine and provided insights into the mechanism of radioprotection. Thus, HL-003 is a small molecule radioprotector with a potential application in radiation medicine.

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“…As a result, IR can impair the structure of DNA, proteins and lipids, and eventually lead to deleterious consequences, including cell apoptosis and organ system dysfunction 6‐8 . Research has shown that hematopoietic tissues and the gastrointestinal (GI) tract are sensitive to IR, the former being the most sensitive, 9,10 and there are few effective methods to prevent or mitigate radiation‐induced injury of the GI tract 11,12 . Thus, finding remedies to protect these systems from radiation damage is of utmost importance 13,14 …”

Section: Introductionmentioning

confidence: 99%

Synthesis and radioprotective effects of novel hybrid compounds containing edaravone analogue and 3‐n‐butylphthalide ring‐opening derivatives

Wang

Miao

et al. 2021

J Cellular Molecular Medi

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As the potential risk of radiation exposure is increasing, radioprotectors studies are gaining importance. In this study, novel hybrid compounds containing edaravone analogue and 3‐n‐butylphthalide ring‐opening derivatives were synthesized, and their radioprotective effects were evaluated. Among these, compound 10a displayed the highest radioprotective activity in IEC‐6 and HFL‐1 cells. Its oral administration increased the survival rates of irradiated mice and alleviated total body irradiation (TBI)‐induced hematopoietic damage by mitigating myelosuppression and improving hematopoietic stem/progenitor cell frequencies. Furthermore, 10a treatment prevented abdominal irradiation (ABI)‐induced structural damage to the small intestine. Experiment results demonstrated that 10a increased the number of Lgr5+ intestinal stem cells, lysozyme+ Paneth cells and Ki67+ transient amplifying cells, and reduced apoptosis of the intestinal epithelium cells in irradiated mice. Moreover, in vitro and in vivo studies demonstrated that the radioprotective activity of 10a is associated to the reduction of oxidative stress and the inhibition of DNA damage. Furthermore, compound 10a downregulated the expressions of p53, Bax, caspase‐9 and caspase‐3, and upregulated the expression of Bcl‐2, suggesting that it could prevent irradiation‐induced intestinal damage through the p53‐dependent apoptotic pathway. Collectively, these findings demonstrate that 10a is beneficial for the prevention of radiation damage and has the potential to be a radioprotector.

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Effects of Thymoquinone on radiation enteritis in mice

Cited by 112 publications

References 42 publications

Thymoquinone (2-Isopropyl-5-methyl-1, 4-benzoquinone) as a chemopreventive/anticancer agent: Chemistry and biological effects

Thymoquinone (2-Isopropyl-5-methyl-1, 4-benzoquinone) as a chemopreventive/anticancer agent: Chemistry and biological effects

Preclinical Evaluation of Safety, Pharmacokinetics, Efficacy, and Mechanism of Radioprotective Agent HL‐003

Synthesis and radioprotective effects of novel hybrid compounds containing edaravone analogue and 3‐n‐butylphthalide ring‐opening derivatives

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