Department of Pharmaceutics, Faculty of Pharmacy, Integral University, Kursi Road, Lucknow, India.
School of Medical & Allied Sciences, Department of Pharmaceutics, K.R. Mangalam University, Gurgaon, India.
Curr Drug Targets. 2018;19(1):70-80. doi: 10.2174/1389450118666170612095959.
BACKGROUND: Thymoquinone (TQ) is a bioactive phytoconstituent obtained from Nigella sativa (black seeds). It has promising potential in cancer prevention. OBJECTIVE: Previous studies have shown that TQ can modulate signaling pathways responsible for cancer progression, thus enhancing the efficacy and improving the safety profile of clinically used anticancer drugs. METHOD: TQ acts on cell cycle and inhibits progression from G1 to S phase by targeting various proteins (cyclin D1, cyclin E, and p27). It also exhibits histone deacetylase (HDAC) inhibitory effects, targets p21 and Maspin, and induces pro-apoptotic gene, Bax and downregulates anti-apoptotic gene Bcl-2. Breast cancer (BC) is reported as one of the most common malignancies in women. RESULTS: Despite the research and advancement, it remains one of the most common causes of cancer related deaths among women. Recent advancements in molecular screening of BC led to the identification of clinically challenging condition of triple negative breast cancer (TNBC). TNBC is characterized by the absence of targetable receptors viz. estrogen receptor (ER), progesterone receptor (PR) and human epidermal growth factor receptor 2 (HER2) expressions. It is also characterized by reduced or absence of phosphatase and tensin homolog (PTEN) expression, a tumor suppressor gene having diverse functions including regulation of apoptosis, cell cycle, and metastasis. CONCLUSION: Since TQ has been reported to up-regulate several growth factors such as vascular endothelial growth factor (VEGF), EGF and PTEN expression, the present review article discusses the targeting potential of TQ for therapeutic intervention against such types of breast cancer.
背景:百里醌(TQ)是从黑种草(黑种子)中获得的一种具有生物活性的植物成分。它在癌症预防方面具有很大的潜力。
目的:先前的研究表明,TQ 可以调节负责癌症进展的信号通路,从而提高临床使用的抗癌药物的疗效并改善其安全性。
方法:TQ 通过靶向各种蛋白质(细胞周期蛋白 D1、细胞周期蛋白 E 和 p27)作用于细胞周期并抑制从 G1 期到 S 期的进展。它还表现出组蛋白去乙酰化酶(HDAC)抑制作用,靶向 p21 和 Maspin,并诱导促凋亡基因 Bax 并下调抗凋亡基因 Bcl-2。乳腺癌(BC)被报道为女性中最常见的恶性肿瘤之一。
结果:尽管进行了研究和进展,但它仍然是女性癌症相关死亡的最常见原因之一。最近在 BC 的分子筛选方面的进展导致了三阴性乳腺癌(TNBC)的临床挑战性情况的确定。TNBC 的特征是缺乏可靶向的受体,即雌激素受体(ER)、孕激素受体(PR)和人表皮生长因子受体 2(HER2)的表达。它还表现为磷酸酶和张力蛋白同源物(PTEN)表达减少或缺失,PTEN 是一种肿瘤抑制基因,具有多种功能,包括调节细胞凋亡、细胞周期和转移。
结论:由于 TQ 已被报道可上调多种生长因子,如血管内皮生长因子(VEGF)、EGF 和 PTEN 表达,因此本综述文章讨论了 TQ 针对此类乳腺癌的治疗干预的靶向潜力。
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