A Review on Pretreatment and Analysis Methods of Polyether Antibiotics in Complex Samples.

Polyether antibiotics (PAs) are the anti-coccidiosis drugs used for treating and preventing coccidiosis. Studies show the residues of these antibiotics in food cause adversities and threaten human health. PAs thus need robust, rugged, and accurate methods for their analysis. This review encompasses pretreatment and detection methods of PAs in diverse matrices since 2010. Both conventional and developed methods are part of the pretreatments, such as dispersive liquid-liquid microextraction, solid-phase extraction, solid-phase microextraction, solvent front position extraction, QuEChERS (Quick Easy Cheap Effective Rugged and Safe), supercritical fluid extraction, and others. The analysis methods involve liquid chromatography coupled with detectors, sensors, etc. The pros and cons of various techniques for PAs have been discussed and future tendencies are proposed.

Progress of pretreatment and analytical methods for PAs are summarized.Comparisons between different mass analyzers are discussed in detail.Novel materials in microextraction methods are depicted.

[Multivariate correlation analysis of T1S and C7S].

OBJECTIVE: To determine whether C7 angles (C7 slope, C7S) could replace T1 angles (T1 slope, T1S) by correlation analysis of T1S and C7S. METHODS: A total of 442 patients from July 2015 to July 2020 in outpatient and inpatient department were enrolled retrospectively, and 259 patients who could identify the upper endplate of T1 were screened out . Of them, there were 145 males and 114 females, aged from 20 to 83 years old with an average of (58.6±11.2) years, including 163 patients with cervical spine surgery and 96 non-surgical patients. Patients were stratified by sex, age, cervical kyphosis, cervical alignment imbalance, and cervical spine surgery. These 259 patients included 145 cases in the male group, 114 cases in the female group;76 cases in the youth group (<40 years old), 109 cases in the middle-aged group (40 to 60 years old), and 74 cases in the elderly group(>60 years old); 92 cases in the cervical kyphosis group, 167 cases in the non-kyphosis group;51 cases in the cervical sequence imbalance group, 208 cases in the non-imbalance group;163 cases in the cervical surgery group, 96 cases in the non-operation group. The correlations of C7S and T1S in various modalities groups were analyzed. RESULTS: Of 442 patients, the recognition rate of upper endplate of T1 was 58.6%(259/442), and that of C7 was 90.7%. The mean T1S and C7S of the 259 patients were (24.5±8.0)° [(25.9±7.7)° in the male group and (23.7±6.9)° in the female group] and (20.8±7.3)° [(22.5±7.5)° in the male group and(19.7±5.8)° in the female group], respectively. The total correlation coefficient between C7S and T1S was r=0.89, R2=0.79, and the linear regression equation was T1S=0.91×C7S+4.35. In the above general information and the grouping of deformity factors, T1S was highly correlated with C7S(r value 0.85 to 0.92, P<0.05). CONCLUSION: There is a high correlation between T1S and C7S in different factor groups. For cases where T1S cannot be measured, C7S can be used to provide guidance and reference for evaluating the sagittal balance of the spine, analyzing the condition, and formulating surgical plans.

2-Styryl-4-aminoquinazoline derivatives as potent DNA-cleavage, p53-activation and in vivo effective anticancer agents.

Forty-eight analogues of CP-31398, an antitumor agent modulated the mutant p53 gene were synthesized and their cytotoxicities against four cancer cell lines with different p-53 status including bladder cell T24 (w-p53), gastric cell MGC-803 (m-p53), prostate cell DU145 (m-p53), prostate cell PC-3 (null-p53), lung cell A549 (w-p53) and normal liver cell line HL-7702 (w-p53) were examined. (E)-2-(4-Nitrostyryl)-4-(3-dimethylaminopropyl)-aminoquinazoline (10ah) was identified as the most potent compound in anti-proliferation against MGC-803 cells, with IC50 lowed to 1.73 µM, far potency than that of CP-31398. Molecular mechanism study revealed that 10ah and CP-31398 differ greatly in mechanism to exert their antitumor properties. 10ah could intercalate into DNA and resulted in significant DNA double-strand break. 10ah-treatment in MGC-803 cells increased the expression of p53, phosphorylated p53 (p-p53), CDK4, p21 to cause cell cycle arrest at G2/M phase, significantly up-regulated the levels of pro-apoptosis proteins Bak, Bax, Bim while down-regulated the anti-apoptosis proteins Bcl-2, Bcl-xL and the levels of cyclin B1, fluctuated the intracellular reactive oxygen species (ROS), Ca2+ and mitochondrial membrane potential, activated Caspase-9 and Caspase-3 to induce apoptosis. 10ah also displayed potent anticancer efficiency against MGC-803 xenograft tumors models, with tumor growth inhibition (TGI) up to 61.8% at 20 mg/kg without obvious toxicity.

Cryptolepine and aromathecin based mimics as potent G-quadruplex-binding, DNA-cleavage and anticancer agents: Design, synthesis and DNA targeting-induced apoptosis.

Thirty Cryptolepine and Aromathecin based mimics were designed and synthesized. Their cytotoxicity was evaluated in four human cancer cell lines (HepG-2, T24, NCI-H460 and MGC-803) and one normal human cell line (HL-7702). Most compounds exhibited potent anticancer activity with IC50 values from 0.31 to 11.97 µM. 8-Fluoro-10-(N-3-dimethylaminopropyl)amino-11H-indeno[1,2-b]quinoline (5b) was identified as the most promising candidate in view of its anticancer activity. Molecular mechanism studies suggested that 5b not only could strongly bind to G-quadruplex, but intercalate into supercoil DNA and resulted in significant DNA double-strand break as well. Furthermore, 5b caused cell cycle arrest at S/G2 phase and induced apoptosis. After treatment with 5b, pro-apoptotic proteins Bak, Bax and Bim were up-regulated, anti-apoptotic proteins Bcl-2 and Bcl-xL were down-regulated, and the effector caspase-3/9 was activated to initiate apoptosis. The anticancer activity of 5b was finally validated in a MGC-803 xenograft tumor model with tumor growth inhibition (TGI) up to 53.2%, while displaying no obvious toxicity. Taken together, these results suggest that 5b may be a potential candidate of cytotoxic antineoplastic drugs for cancer therapy.