Journal of Berry Research
·
2019
·Vol. 9
·期 1
·109-123
·
IF 2.379
Zhang Jiaojiao,Xiao Jianbo,Giampieri Francesca,Forbes-Hernandez Tamara Y.,Gasparrini Massimiliano,Afrin Sadia,Cianciosi Danila,Reboredo-Rodriguez Patricia,Battino Maurizio,Zheng Xiaodong
Anthocyanins are plant pigments widely present in fruits and vegetables that exert health benefits as part of human diet. They exist in not glycosylated forms (anthocyanidins) and glycosylated forms. Anthocyanins have been studied for their ability to inhibit polysaccharide metabolism enzymes (such as α-glucosidase) and, therefore, attenuate hyperglycemia and modulate type II diabetes. The aim of the present work was to compare the inhibitory activity of anthocyanins with that of acarbose, a common α-glucosidase inhibitor, by evaluating IC50 and Km, to compare the inhibitory capabilities among different compounds in an in vitro study. Our results showed that most of the anthocyanins studied presented lower IC50 values than acarbose; only Pn-3-glc presented IC50 value close to acarbose. Moreover, there was no difference in Km between complete competitive and complete non-competitive types of inhibition (T-test, p > 0.05). In conclusion, the anthocyanins and their degradation products work together on attenuating abilities of this sugar metabolism key enzyme, throughout competitive and non-competitive modes.
研究领域:
营养学
·
药理学
✓ 已验证
产品关联
DOI
高影响因子
TOXICOLOGY IN VITRO
·
2023
·
IF 3.2
Weiyi Ye,Zhen Wang,Xin Lv,Hang Yin,Lili Jiang,Zhe Wang,Yong Liu
Ponatinib is an efficient oral tyrosine kinase inhibitor (TKI) for T315I-positive Ph + ALL and T315I-positive chronic myeloid leukemia (CML) or BCR-ABL when no other TKIs can be prescribed. In this research, we evaluated the inhibitory effects of ponatinib on human recombinant UDP-glucuronosyltransferases (UGTs) and predicted the magnitude of potential drug-drug interaction (DDI) risk of co-treatment with ponatinib and UGTs substrates by using in vitro-in vivo extrapolation (IVIVE) method. Our study presented that ponatinib showed a broad-spectrum inhibition against UGTs. Particularly, ponatinib exhibited potent inhibitory effects towards UGT1A7, UGT1A1, and UGT1A9 with IC 50 values of 0.37, 0.41, and 0.89 μM, respectively, which might lead to clinically significant DDI.
研究领域:
药理学
·
临床医学
·
生物化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Natural Products and Bioprospecting
·
2017
·Vol. 7
·期 6
·461-469
·
IF 0
Mahal Ahmed,Wu Ping,Jiang Zi-Hua,Wei Xiaoyi
Abstract Tetrahydrocurcumin (THC) is a major metabolite of curcumin and plays an important role in curcumin-induced biological effects. THC is a promising preventive and chemotherapeutic agent for cancer. A series of new pyrazole derivatives of THC have been synthesized as potent anticancer agents. Direct condensation of THC with various substituted hydrazines leads to new pyrazole derivatives of THC ( 1 – 18 ). The prepared compounds have been evaluated via in vitro MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay for their cell proliferation-inhibitory activity against human lung adenocarcinoma (A549), human cervical carcinoma (HeLa) and human breast carcinoma (MCF-7) cells. Most derivatives show significantly higher anticancer activity against all three tested cancer cell lines than the parent compound THC. Several compounds ( 7 , 8 , 12 , 13 and 15 ) display promising anticancer activity against MCF-7 cell line with IC 50 values ranging from 5.8 to 9.3 µM. The most active compound ( 8 ) is substituted with 4-bromophenyl group at the pyrazole ring and inhibits the growth of all three tested cancer cell lines with an IC 50 values of (8.0 µM, A549), (9.8 µM, HeLa) and (5.8 µM, MCF-7). The obtained compounds can be a good starting point for the development of new lead molecules in the fight against cancer. Graphical Abstract
研究领域:
药物化学
·
肿瘤学
·
有机合成
✓ 已验证
DOI
PubMed
BIOORGANIC CHEMISTRY
·
2020
·
IF 4.831
Chao Liu,Hua Zhou,Xiao Bao Sheng,Xin Hua Liu,Fei Hu Chen
Telomerase has become one of the new popular targets for the development of anti-tumor drugs. Based on the structural characteristics of the BIBR1532 which has entered the stage of clinical research, six series total of 64 new compounds with diverse structural characteristics were designed and synthesized. The inhibitory activity against SGC-7901, MGC-803, SMMC-7721, A375 and GES cell lines and their telomerase inhibitory activity were tested. Among them, eight compounds showed good activity against cancer cells, among them compounds 56 , 57 and 59 also showed low toxicity. Some of them showed excellent telomerase inhibitory activity with IC 50 values ranging from 0.62 μM to 8.87 μM. Based on above, in depth structure-activity relationships were summarized, the compounds by replacing methyl group with cyanide and retaining amide moiety had good anti-tumor activity, moderate cytotoxicity, and better telomerase inhibitory activity. The results should be used for reference in BIBR1532-based structural optimization for further development of small molecule telomerase inhibitors.
研究领域:
药理学
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肿瘤学
·
药物化学
✓ 已验证
DOI
PubMed
高影响因子
Analytical Methods
·
2013
·Vol. 5
·期 21
·6106-6113
·
IF 1.855
Yajing Lei,Lizheng Fang,Muhammad Sajid Hamid Akash,Zhiming Liu,Weixing Shi,Shuqing Chen
Bisphenol A (BPA) is widely used to manufacture polycarbonate plastics and epoxy resins, which are in widespread use in China. Concerns about potential health impacts from exposure to BPA among the general population are increasing day by day. A sensitive and specific antibody was prepared to develop and compare direct and indirect competitive enzyme-linked immunosorbent assays (ELISAs) for the determination of BPA in human urine. The IC50 value and limit of detection (LOD) for the direct competitive ELISA were 5.5 ng mL−1 and 0.03 ng mL−1 respectively whereas, for the indirect competitive ELISA, the IC50 value and LOD were 7.0 ng mL−1and 0.08 ng mL−1, respectively. We found that the direct competitive ELISA was more specific and sensitive than the indirect competitive ELISA. The established immunoassays were also applied in the determination of BPA in human urine samples. The results from fortified samples and real samples indicated that the direct competitive ELISA was more sensitive and reliable for the measurement of BPA in human urine as compared to the indirect competitive ELISA.
研究领域:
环境健康
·
分析化学
·
毒理学
✓ 已验证
产品关联
DOI
高影响因子
INDUSTRIAL CROPS AND PRODUCTS
·
2024
·
IF 5.6
Yanju Lu,Fengqi Chen,Yuxiang Chen,Jing Wang,Shenlin Huang
Isopimaric acid is derived from a natural resource of pine resin, which is inherently biologically active. A series of seven novel isopimaric heterocyclic sulfonamides derivatives were synthesized using isopimaric acid as the lead compound to splice with the sulfonamides by chlorinated and amidated to screen out compounds with anti-tumor activity. And it was characterized using infrared spectrum (IR), nuclear magnetic resonance (NMR), and mass spectrometry. All of the compounds were screened for their antitumor activity against cervical cancer cells (Hela), breast cancer cells (MDA-MB-231), prostate cancer cells (PC-3), and hepatoma cells (HepG-2). Some of the test compounds showed potent antitumor activity. Among the isopimaric heterocyclic sulfonamides derivatives synthesized, compound 5a inhibited the growth of the four tumor cells mentioned above with IC 50 values in the range of 28.53–40.98 µM. In addition, compound 5c exhibits inhibitory activity toward these tumor cells with IC 50 values in the range of 56.27–60.62 µM. In conclusion, isopimaric heterocyclic sulfonamides derivatives may provide a basis for further research on anti-tumor drugs.
研究领域:
药物化学
·
肿瘤学
·
有机合成
✓ 已验证
产品关联
DOI
高影响因子
Natural Product Communications
·
2022
·
IF 1.496
Qing Liu,Ying Wei,Yongjia Hao,Jian Yang,Bowen Pan,Xiaosheng Yang,Ying Zhou,Xia Wang
Viral infection imposes a major threat to human health. To develop new potent antiviral agents, Hederagenin (HE), a known inhibitor of HIV-1 and HCV NS3/4A proteases, was used as a starting material to synthesize 4 types of HE derivatives, HE-3,23-diacyl, HES-3,23-diacyl, HES-3-acyl, and HES-3-oxo-23-acyl. We evaluated the in vitro inhibitory activities of the derivatives against HIV-1 and HCV NS3/4A proteases. (3β,23)-Di-O-diglutaryl-hederagenin (1b) and (3β,23)-di-O-(3′,3′-dimethylsuccinyl-hederagenin ethyl ester (2b) exhibited potent inhibitory activities against the HIV-1 and/or HCV NS3/4A proteases with IC50 values < 10 μM, but did not appreciably inhibit general human proteases renin and trypsin. The SARs showed that dicarboxylic acid hemiesters of HE significantly enhance the antiviral activities when C3 or C23 are linked with 6 carbon acyl chains.
研究领域:
药理学
·
病毒学
·
药物化学
✓ 已验证
产品关联
DOI
高影响因子
RSC Advances
·
2018
·Vol. 8
·期 72
·41377-41388
·
IF 2.936
Xiao-Qian Chi,Cheng-Ting Zi,Hong-Mei Li,Liu Yang,Yong-Feng Lv,Jin-Yu Li,Bo Hou,Fu-Cai Ren,Jiang-Miao Hu,Jun Zhou
In order to better understand the structure–activity relationship of mangostin, a series of xanthone derivatives based on α-mangostin were designed and synthesized. All the compounds were evaluated for their cytotoxicity against a panel of five human cancer cell lines (HL-60, SMMC-7721, A-549, MCF-7 and SW480) using MTT assays. Most of them showed cytotoxicity and most of all, compounds 1a and 2h showed the highest cytotoxic potency by HL-60 cancer cell lines with IC50 values of 5.96 μM and 6.90 μM respectively; compound 3e showed the highest cytotoxic potency against SMMC-7221 cancer cell line with IC50 values of 3.98 μM; compounds 2e and 2m showed lower cytotoxicity but higher selectivity than α-mangostin against HL-60 and SMMC-7221 cancer cell lines respectively. Structure–activity relationship analysis indicates that the maintenance of the isopentene group at C-8 is essential for the cytotoxic activity.
研究领域:
药物化学
·
肿瘤学
·
有机合成
✓ 已验证
DOI
PubMed
高影响因子
Molecular Medicine Reports
·
2015
·Vol. 12
·期 4
·6019-6024
·
IF 1.554
Zeliang Wei,Yuyan Liang,Limei Ma,Ke Li,Hai Niu,Wen Huang
Steroidal saponins have recently attracted attention due to their structural diversity and significant biological activities, including anti‑hyperlipidemic, antibacterial, anti‑inflammatory, immunomodulatory and anti‑HIV activities. In the present study, it was demonstrated that WRC3, a novel saponin derivative, can inhibit B16 cancer cells by inducing apoptotic cell death with an IC50 value of 12.09 µM. The inhibitory effect of WRC3 on B16 cells appears to occur in a time‑ and concentration‑dependent manner. The fluorescence distribution observed by confocal microscopy revealed that WRC3 entered cells and acted in the cytoplasm without causing genetic toxicity. Following administration of WRC3 (2.5, 5.0 and 7.5 g/kg body weight) once a day for 7 days, no obvious abnormalities were observed in the organs of the mice as demonstrated by hematoxylin and eosin staining. Compared with the normal control group, aspartate transaminase (AST), alanine transaminase (ALT), creatine and urea levels in the serum of mice treated with WRC3 (2.5‑7.5 µM) remained unchanged. In conclusion, it was demonstrated that WRC3 can induce cancer cell death without causing genetic toxicity, hepatotoxicity or nephrotoxicity.
研究领域:
药理学
·
肿瘤学
·
毒理学
✓ 已验证
DOI
PubMed
高影响因子
JOURNAL OF CHEMICAL RESEARCH
·
2025
·
IF 1.2
Yulan Zhu,Yuhang Ding
Twelve ferulic acid–based derivatives containing urea groups were synthesized and characterized by elementary analytical,1H and 13C nuclear magnetic resonance and electrospray ionization mass spectrometry spectra. Their hypoglycemic and aldose reductase inhibitory activities were evaluated, several of which showed hypoglycemic activities in vivo comparable with the positive drug glibenclamide. Furthermore, of the tested compounds, 7a and 7b displayed the most potent aldose reductase inhibitory activity in vitro, with an IC50 of 0.55 and 3.88 μM, respectively. Docking simulation indicated compound 7a mainly interact with aldose reductase 2 via three hydrogen bonds with ARG268, SER263, SER210, and one π–π stacking interaction with TYR209.
研究领域:
药物化学
·
生物化学
·
医学
✓ 已验证
DOI
高影响因子
STARCH-STARKE
·
2023
·
IF 2.3
Yijuan Xu,Weifeng Hua,Haoran Xu,Harold Corke,Wuyang Huang,Zhongquan Sui
Hulless barley (HB) grass is a potential resource of functional food. In this study, the proliferation inhibitory effect against cancer cells of an alkaline extracted polysaccharide (APP) from HB grass (HBG) is analyzed. The yield of crude alkaline extracted polysaccharide (APC) reaches 15.1%. After purification, the purity and polydispersity index (PDI) of the APP are 98.3% and 1.38, respectively. The molecular weight of APP is 5.1 × 10 5 Da, whereas the number-average molecular weight of APP is 3.7 × 10 5 Da. APP is composed of arabinose (37.8%), xylose (41.3%), glucose (4.6%), and galactose (16.3%). According to the infrared spectral analysis, APP is found to contain β-glycosidic bonds. Moreover, APP possesses significant cell proliferation inhibitory effects against various cancer cell lines, such as 4T1, HT29, Caco-2, and CT26.WT in a dose-dependent manner. Notably, the IC50 value of 4T1 reaches 7.56 mg mL −1 , which indicates that APP from HBG has a potential anti-cancer effect in vitro. It may be further investigated as an ingredient or nutraceutical for development and utilization in functional foods to prevent or treat cancer and related diseases.
研究领域:
食品科学
·
癌症研究
·
药理学
·
植物化学
✓ 已验证
产品关联
DOI
高影响因子
CYTOTECHNOLOGY
·
2011
·Vol. 64
·期 2
·157-163
·
IF 1.277
Yi Yu,Wang Zhuhuan,Li Min,Zhu Keyin,Ying Guoqing
Monoclonal antibodies (McAbs) against chloramphenicol (CAP) were produced to detect CAP residues, which could be toxic and possesses a potential threat to human health. The CAP-BSA conjugate was obtained by bovine serum albumin (BSA) coupled with CAP, and used to immunize the mice. The splenocytes from the immunized mice were fused with mouse myeloma cells SP2/0 to form hybridoma, which may secrete McAbs against CAP. Hybridomas 1D 1 and 3G 12 secreting McAbs against CAP were obtained by screening. Ascites containing McAbs were prepared by injecting 1 x 10 6 cells of hybridoma 1D 1 and 3G 12 into the abdomen of mice. Protein A affinity chromatography was used to purify McAbs against CAP in a single chromatographic step with recovery yield above 80% and purity above 95% and full recovery of antibody activity. Experiments showed that McAb 3G 12 was highly specific for CAP and had no cross-reactivity with analogues which have a structure similar to CAP. The IC 50 value was 50.8 ng/mL.
研究领域:
免疫学
·
药理学
·
毒理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）