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Phenolic Compounds potential health Benefits and toxicity
Published in Quan V. Vuong, Utilisation of Bioactive Compounds from Agricultural and Food Waste, 2017
Deep Jyoti Bhuyan, Amrita Basu
Apigenin, a flavone abundantly found in fruits and vegetables, is shown to possess anticancer properties against cancer of breast, cervix, colon, leukemia, lung, ovarian, prostate, skin, thyroid, gastric, liver and neuroblastoma, to name a few (Shukla and Gupta 2010). A study by Ruela-de-Sousa et al. (2010) suggested that apigenin can block proliferation in two types of leukemia cells—myeloid and erythroid subtypes through cell-cycle arrest in G2/M phase (myeloid HL60) and G0/G1 phase (erythroid TF1 cells). Choudhury et al. (2013) also showed that apigenin and curcumin can synergistically induce cell death and apoptosis and block cell cycle progression at G2/M phase of A549 lung epithelium cancer cells. They also established that both apigenin and curcumin can simultaneously bind at different sites of tubulin. Similarly, apigenin is also linked with inhibition of pancreatic cancer cell proliferation by G2/M cell cycle arrest, down regulation of the overexpressed protein geminin, increase in growth inhibitory effects of gemcitabine and abrogation of gemcitabine resistance in multiple reports (Ujiki et al. 2006, Salabat et al. 2008, Strouch et al. 2009). Another study by Gomez-Garcia et al. (2013) demonstrated that both potassium apigenin and carnosic acid have chemoprotective effects against 7,12-dimethyl benzanthracene (DMBA)-induced carcinogenesis in hamster. Moreover, the anti-proliferative and anti-angiogenic effects of the flavonoid, apigenin, were illustrated by Melstrom et al. (2011). They established that apigenin inhibits HIF-1α, GLUT-1, and VEGF mRNA and protein expression in pancreatic cancer cells in both normoxic and hypoxic conditions, proving its potential as a therapeutic agent for pancreatic cancer. Johnson et al. (2011) showed that citrus flavonoids, such as luteolin, apigenin and quercetin can inhibit glycogen synthase kinase-3β (GSK-3β), which leads to decreased cancer cell proliferation and survival by reducing NFκB activity. They made similar observations in vivo. Apigenin and luteolin were also shown to improve the efficacy of certain chemotherapeutic drugs—gemcitabine, cisplatin, 5-fluorouracil and oxaliplatin—in terms of their anti-proliferative activity against BxPC-3 human pancreatic cancer cells by Johnson and Gonzalez de Mejia in 2013. Moreover, Lee et al. (2008) made similar observations and proposed that gemcitabine in combination with apigenin resulted in enhanced apoptosis and growth inhibition by down-regulation of NFκB activity through suppression of AKT activation in pancreatic cancer cell lines in vitro.
Nanobodies targeting the interaction interface of programmed death receptor 1 (PD-1)/PD-1 ligand 1 (PD-1/PD-L1)
Published in Preparative Biochemistry & Biotechnology, 2020
Biyan Wen, Lin Zhao, Yuchu Wang, Chuangnan Qiu, Zhimin Xu, Kunling Huang, He Zhu, Zemin Li, Huangjin Li
The human domain antibody library (Source BioScience, Nottingham, UK) was used for phage screening. Escherichia coli DH5α (Merck, Darmstadt, Germany) was used for molecular cloning and E. coli BL21 (DE3) (Merck) was used as a host for human nanobody expression. The pET-21b vector (Merck) was used to clone the human nanobody gene. Ni-NTA, CM-Sepharose, Sephadex-G25, and Sephadex 75 columns were used for the purification of nanobodies (GE Healthcare, Buckinghamshire, UK). Human cervical carcinoma HeLa cells and human lung cancer A549 cells were purchased from the Chinese Academy Type Culture Collection. The human pancreas adenocarcinoma BxPC-3 cells and human mucoepidermoid pulmonary carcinoma NCI-H292 cells were purchased from the Chinese Jennio Biotech. DMEM, RPMI-1640, fetal bovine serum (FBS) and supplements were purchased from HyClone (Logan, UT). MPBS buffer is a PBS buffer supplemented with 5% marvel milk powder (w/v). PBST contained 0.1% Tween-20 in PBS buffer. 2 × YT medium was made by dissolving 16 g of bacto-tryptone, 10 g of yeast extract and 5 g of NaCl in 1 L of deionized water. Bacteria-tryptone (10 g), yeast extract (5 g), and NaCl (8 g) were dissolved in 800 mL of deionized water and mixed with 200 mL of 20% glucose solution (w/v). Ampicillin solution (1 mL) was then added to prepare TYE ampicillin glucose agar plates. For this, Ampicillin sodium salts were dissolved in deionized water to a concentration of 100 mg/mL and stored at −20 °C. PB consisted of NaH2PO4 and Na2HPO4 in deionized water.
Two mixed-ligand Cd(II)-coordination polymers: structural diversity and antitumor activity against human osteogenic sarcoma cells
Published in Inorganic and Nano-Metal Chemistry, 2020
Feng Han, Shun Cao, Hongwei Ding, Ziwei Chen, Qiang Zhang, Shi-Dong Xu
Cadmium(II) is a toxic metal ion which has lesser value in medicinal chemistry compared with other metal ions such as Co(II), Cu(II) and so on, but study on the drug activity of such compound would pave way to understand the structural requirements or the role of a metal ion in drugs.[14] Recent literatures have revealed that some Cd(II)-based coordination complexes showed promising anticancer activity. For instance, Baruah et al. have revealed that the Cd(II)-containing coordination complexes based on the benzothiazole ligands are cytotoxic in pancreatic cancer cell lines Mia Paca-2, BxPC-3 and Panc-1, whose IC50 values are as low as 16.0 μM[15]; Koizumi et al. have found that the Cadmium-coordinated supramolecule could suppress tumor growth of T-cell leukemia in mice.[16] In addition, Barszcz group found that the selection of suitable chelating ligand could greatly reduce the toxicity of the Cd(II) ion to the human normal cell lines.[17] The above results encourage us to study the anticancer activity of the Cd(II) complexes prepared in this work. After the synthesis of compounds 1 and 2, the inhibitory effect of the synthesized compounds on MG-63 human osteogenic sarcoma cell activity was evaluated firstly. Above all, CCK-8 method was recommended to determine the anti-cancer activity of the compounds. After exposed to serious dilutions of compounds 1 and 2, as well as the ligands H2opda, H2ppda, and metal cadmium ions, the cell viability of MG-63 cells was measured in a microplate reader. As the results showed in Figure 4, we can see that compound 1 could significantly reduce the viability of MG-63 cells, with the IC50 value of 3.78 ± 0.13 μg/mL. The anti-cancer activity of compound 2 was much slighter than compound 1. In addition to this, the ligands H2opda, H2ppda, and metal cadmium ions all showed no effect on the cancer cell viability.