Man Ding,Xuechen Zhang,Jiangying Shi,Kaili Cui,Ruipeng Yang,Fengming Liu,Shuhua Shan,Ghani Israr,Zhuoyu Li
Colorectal cancer (CRC) is one of the most common malignant tumors worldwide, occurring in the colon or rectum portion. Quinoa is a dicotyledonous plant, and the quinoa bran is the outer seed coat of quinoa. Functional molecules in plants play an important role in the treatment and alleviation of chronic diseases. In this study, quinoa bran was used as the raw material. The active components with an anti-colorectal cancer effect were extracted by acetone and separated with an AB-8 macroporous resin column, which was further identified as terpenoids by liquid-mass spectrometry (LMS), named Quinoa bran terpenoids (QBT). The yield of quinoa bran terpenoids was 0.77%. Moreover, the results showed that QBT significantly inhibited the proliferation of colorectal cancer cells DLD-1 and HCT-8 with a concentration gradient dependent manner. Respectively, the IC 50 values of DLD-1 and HCT-8 cells were 0.42 ± 0.02 and 0.54 ± 0.05 mg/mL. Further studies showed that QBT upregulated apoptosis-related proteins such as activated-caspase-3, 8, and 9. In addition, QBT decreased mitochondrial membrane potential , promoted the expression of the pro-apoptotic protein Bax, and inhibited the anti-apoptotic protein Bcl-2. The experiments showed that QBT significantly repressed the growth of tumors in nude mice . In conclusion, these results indicated that QBT largely inhibits the development of colorectal cancer to large extent through upregulation of caspase-3, 8, and 9 and reduction of mitochondrial membrane potential, and has great potential for anti-tumor progression.
Extracts from the bran of Chenopodium quinoa Willd. (QBE) were reported to be active in inhibiting α-glycosidase, a promising target for treatment of diabetes mellitus. However, the constituents responsible for the α -glucosidase-inhibiting activity of QBE have not been fully characterized. The present study aimed to set up a method for rapid identification of glycosidase inhibiting compounds from the quinoa bran. With surface plasmon resonance (SPR) coupled with liquid chromatography-mass spectrometry (LC-MS), we identified eight flavonoids and ten triterpenoid saponins that may bind to the α-glycosidase. Analysis of the interaction kinetics by molecular docking supported their α -glucosidase-inhibiting activity and revealed the potential mechanisms for the inhibitory effects. In summary, this study established a SPR and LC-MS-based method for rapid in vitro screening of α -glucosidase inhibitors and suggested the quinoa bran a potential natural source of α- glucosidase inhibitors.