Zhang Lei, Shamaladevi Nagarajarao, Jayaprakasha Guddadarangavvanahally K, Patil Bhimu S, Lokeshwar Bal L
Sheila and David Fuente Graduate Program in Cancer Biology, Sylvester Comprehensive Cancer Center, Miller School of Medicine, University of Miami, Miami, Florida, USA.
Departments of Urology and Radiation Oncology, Miller School of Medicine, University of Miami, Miami, Florida, USA.
Oncotarget. 2015 Jun 30;6(18):16379-95. doi: 10.18632/oncotarget.3834.
Bioactive compounds from edible plants have limited efficacy in treating advanced cancers, but they have potential to increase the efficacy of chemotherapy drugs in a combined treatment. An aqueous extract of berries of Pimenta dioica (Allspice) shows promise as one such candidate for combination therapy or chemoprevention. An aqueous extract of Allspice (AAE) was tested against human breast cancer (BrCa) cells in vitro and in vivo. AAE reduced the viability and clonogenic growth of several types of BrCa cells (IC50 ≤ 100 μg/ml) with limited toxicity in non-tumorigenic, quiescent cells (IC50 >200 μg/ml). AAE induced cytotoxicity in BrCa was inconsistent with apoptosis, but was associated with increased levels of autophagy markers LC3B and LC3B-positive puncta. Silencing the expression of autophagy related genes (ATGs) prevented AAE-induced cell death. Further, AAE caused inhibition of Akt/mTOR signaling, and showed enhanced cytotoxicity when combined with rapamycin, a chemotherapy drug and an inhibitor of mTOR signaling. Oral administration (gavage) of AAE into athymic mice implanted with MDA-MB231 tumors inhibited tumor growth slightly but not significantly (mean decrease ~ 14%, p ≥ 0.20) if mice were gavaged post-tumor implant. Tumor growth showed a significant delay (38%) in tumor palpability and growth rate (time to reach tumor volume ≥ 1,000 mm3) when mice were pre-dosed with AAE for two weeks. Analysis of tumor tissues showed increased levels of LC3B in AAE treated tumors, indicating elevated autophagic tumor cell death in vivo in treated mice. These results demonstrate antitumor and chemo-preventive activity of AAE against BrCa and potential for adjuvant to mTOR inhibition.
可食用植物中的生物活性化合物在治疗晚期癌症方面疗效有限,但它们有可能在联合治疗中提高化疗药物的疗效。多香果(Allspice)浆果的水提取物显示出作为联合治疗或化学预防的此类候选物的前景。对多香果水提取物(AAE)进行了体外和体内抗人乳腺癌(BrCa)细胞的测试。AAE降低了几种类型BrCa细胞的活力和克隆形成生长(IC50≤100μg/ml),而对非致瘤性静止细胞的毒性有限(IC50>200μg/ml)。AAE在BrCa中诱导的细胞毒性与凋亡不一致,但与自噬标志物LC3B和LC3B阳性斑点水平的增加有关。沉默自噬相关基因(ATGs)的表达可防止AAE诱导的细胞死亡。此外,AAE导致Akt/mTOR信号传导受到抑制,并且当与雷帕霉素(一种化疗药物和mTOR信号传导抑制剂)联合使用时显示出增强的细胞毒性。如果在接种肿瘤后给无胸腺小鼠灌胃AAE,口服AAE对植入MDA-MB231肿瘤的无胸腺小鼠的肿瘤生长有轻微但不显著的抑制作用(平均降低约14%,p≥0.20)。当小鼠预先服用AAE两周时,肿瘤生长在肿瘤可触及性和生长速率(达到肿瘤体积≥1000mm3的时间)方面出现显著延迟(38%)。对肿瘤组织的分析显示,AAE处理的肿瘤中LC3B水平升高,表明在体内治疗的小鼠中自噬性肿瘤细胞死亡增加。这些结果证明了AAE对BrCa的抗肿瘤和化学预防活性以及作为mTOR抑制佐剂的潜力。