Lavandula angustifolia is the most widely cultivated Lavandula species for medicinal use. In this study, chemical and biological evaluation of L. angustifolia aqueous, methanol (MeOH), ethanol (EtOH), ethyl acetate (EtOAc), and chloroform (CHCl3) extracts were conducted. Phytochemically, the extracts’ total phenol and flavonoid contents and their antioxidant potential were evaluated. Ethanol extract was analyzed by LC-MS. All extracts were screened in vitro for their antitumor potential using human breast cancer cell lines MCF-7 and MDA-MB-23. For the first time, the antiproliferative potential of the EtOH extract was tested in vivo using mice with induced breast cancer. Ethanol extract exhibited the best cytotoxicity and safety profile of the tested extracts, with IC50 values of 104.1 µg/mL on MCF-7 and 214.5 µg/mL on MDA-MB-231 cell lines, respectively. In vivo, this extract revealed a reduction in tumor size by 43.29% in the treated group, compared to an increase in the tumor growth by 58.9% in the control group. Moreover, undetected tumor was found in 12.5% of the sample size. In conclusion, this study provides novel insight and evidence on the antiproliferative efficacy of L. angustifolia ethanol extract against breast cancer with potent anti-oxidant potential.
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