Antioxidant, anticancer, and toxicological evaluation of semi-synthetic curcumin benzothiazole analogue

被引:0
|
作者
Kannan, Manivel [1 ]
Thilagavathi, Ramasamy [2 ]
Selvam, Chelliah [3 ]
机构
[1] Karpagam Acad Higher Educ, Fac Pharm, Coimbatore, Tamil Nadu, India
[2] Karpagam Acad Higher Educ, Fac Engn, Dept Biotechnol, Coimbatore, Tamil Nadu, India
[3] Texas Southern Univ, Coll Pharm & Hlth Sci, Dept Pharmaceut Sci, Houston, TX USA
关键词
Antioxidant; Curcumin analogue; ABTS assay; Cytotoxic activity; Acute toxicity; ACUTE ORAL TOXICITY; MOLECULAR DOCKING; EXTRACTS; BREAST;
D O I
10.1007/s13530-022-00164-3
中图分类号
X [环境科学、安全科学];
学科分类号
08 ; 0830 ;
摘要
Objective Curcumin is the most important active component of the turmeric rhizomes (Curcuma longa L). Over the past few decades, research on curcumin and its analogues has increased due to their antioxidant, anti-inflammatory and anticancer activities. This study involved the synthesis of a curcumin benzothiazole analogue and evaluation of the compound's antioxidant properties, in vitro anticancer activity, and in vivo toxicity. Methods An analogue of curcumin benzothiazole was synthesized, and the antioxidant activity was assessed using the ABTS radical scavenging assay. The MTT assay was used to assess the cytotoxic activity against the lung cancer A549, cervical cancer HELA, and breast cancer MDA MB 231 cell lines. According to OECD guidelines, acute toxicity was assessed in albino wistar rats. Results Strong antioxidant activity was shown by the curcumin benzothiazole derivative. The curcumin benzothiazole analogue demonstrated the highest and most potent cytotoxic activity in the MTT assay when tested against MDA MB 231 breast cancer cells, at 88.60 +/- 0.26%. This was followed by moderate cytotoxicity against A549 lung cancer cells and HELA cancer cell lines. According to the OECD 423 recommendations, rats were fed the curcumin benzothiazole analogue at doses of 2000 mg/kg and 300 mg/kg during an acute toxicity experiment. Although no death was discovered at either level, kidney tubular necrosis was observed at the dose of 2000 mg/kg, and albino wistar rats were found to be unaffected by the 300 mg/kg dose. Conclusion According to the findings of this investigation, in vitro experiments showed that the curcumin benzothiazole analogue was a very potent antioxidant and anti-breast cancer candidate. Testing on albino wistar rats revealed that the substance was safe up to levels of 300 mg/kg. [GRAPHICS] .
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页码:85 / 97
页数:13
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