Cervical cancer is the fourth leading cause of malignancy-related mortality in women worldwide, and effective advanced-stage therapies are urgently required. Berberine is a quaternary ammonium compound extracted from traditional Chinese medicinal herbs, including Phellodendron spp., with antibacterial and antitumor activities. Matrine, the main active ingredient of Sophora flavescens rhizomes, has not only traditionally described health effects but is also widely used for its anticancer, anti-inflammatory, immunoregulatory, antiviral, and hepatoprotective effects. We investigated the antitumor activities of berberine and matrine against human cervical cancer HeLa and SiHa cells using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, along with flow cytometry and western blotting analyses, to assess the effect of the compounds on the cellular status and apoptosis- and cell cycle-related proteins. The 24 h half-maximal inhibitory concentrations (IC50) of berberine and matrine were 123.633 ± 4.278 µmol/L and 9.625 ± 0.245 mmol/L against HeLa cells and 105.067 ± 3.745 µmol/L and 8.50 ± 0.23 mmol/L against SiHa cells, respectively. Berberine plus matrine inhibited cancer cell growth and caused cell cycle arrest. We observed an increased stimulation of apoptosis, which was likely mediated by enhanced levels of caspase-3, caspase-9, and B-cell lymphoma 2 (Bcl-2)-associated X protein (Bax), as well as decreased Bcl-2 protein expression. Cell cycle arrest in the G1 phase was probably mediated by p21 upregulation and cyclin-dependent kinase (Cdk)-4, Cdk-6, and cyclin D1 suppression. Combination treatment with berberine and matrine effectively inhibited human cervical cancer cell proliferation, most likely by stimulating apoptosis and inducing cell cycle arrest.
Berberine (BBR) an active natural plant alkaloid extracted from Coptidis rhizoma, displays potent anticancer activity over a variety of cancer cell lines. The cytotoxic activity of BBR in cancer cells is attributed to persuade, programmed cell death characterized by the release of cytochrome c, accompanied by activation of caspase-3 and caspase-9. In the present study, we evaluated BBR significantly reduces the cell viability and clonogenic property of head and neck squamous carcinoma (HNSC) cells. Our results revealed that BBR simultaneously induces apoptosis and autophagy in HNSC cells. Mechanistically, BBR induces autophagy in HNSC cells which were confirmed by acridine orange (AO) staining by visualization of prominent orange red color acidic autophagosomes in the cytoplasm. However, immunoblotting shows the steady conversion of MAP-LC-3I to LC-3II with concomitant degradation of autophagy substrate protein SQSTM1/p62. Annexin V FITC staining analysis by flow cytometry revealed a significant induction of apoptosis at higher doses of BBR. Furthermore, the immunoblotting analysis revealed a prominent cleavage of proapoptotic proteins procaspase-3 and PARP1 at higher doses of BBR. Additionally, we found significant upregulation and downregulation of tumor suppressor microRNA-155 (miR-155) and oncogenic miR-21 respectively, when HNSC cells were exposed to higher doses of BBR. In conclusion, these results demonstrate that BBR exhibits a significant anti-proliferative effect with the simultaneous induction of autophagy and apoptosis and modulates miRNA expression in HNSC cells.
Berberys pospolity jest popularnym, dziko rosnącym krzewem krajów europejskich oraz krzewem ozdobnym na całym świecie. Roślina ta posiada walory dekoracyjne dzięki zimotrwałym, czerwonym jagodom. Prócz tego, korzeń i owoc berberysu zawierają liczne biologicznie aktywne związki, które umożliwiają stosowanie berberysu w terapii stanów zapalnych, zakażeń, chorób serca, dróg żółciowych i jelit. Najważniejszym związkiem aktywnym berberysu jest alkaloid berberyna, która jest naturalnym antybiotykiem. Ponadto, owoc berberysu stanowi cenne źródło witamin C i P.
EN
Berberis vulgaris L. is a wild shrub common in European countries and an ornamental shrub throughout the world. Its unusual decorative value is caused by red berries which do not fall during the wintertime. Besides, the barberry root and fruit contain various biologically active constituents. These compounds are used in phytotherapy as anti-inflammatory, antiseptic, cardiac, digestive and choleretic natural agents. The most important active compound of barberry is alkaloid berberine, a natural antibiotic. In addition, barberry fruit of is a good source of vitamins C and P.
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