Department of Pharmacognosy, College of Pharmacy, King Saud University, P.O. Box 2457, 11451 Riyadh, Saudi Arabia.
Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, 11451 Riyadh, Saudi Arabia.
Molecules. 2018 May 21;23(5):1232. doi: 10.3390/molecules23051232.
Three new transition metal complexes, Cu(II) , Co(II) , and Zn(II) with ligand “bimnap” derived from 1-methyl-2-aminobenzimidazole and 2-hydroxynapthaldehyde were synthesized and characterized. The structure of the ligand was determined by single X-ray crystallography. All the three complexes, ⁻ were examined for the mode of interaction with biomolecule viz., calf thymus-DNA (CT-DNA) using various spectroscopic methods. The nuclease activity was performed against pBR322 DNA that exhibited concentration-dependent degradation of the nucleic acid. The mechanism of DNA cleavage was studied by the electrophoretic pattern in the presence of the radical scavengers. Also, the complexes ⁻ were analyzed for groove binding affinity. Moreover, in vitro cytotoxicities of the complexes ⁻ were tested against the five human cancer cell lines, i.e., HeLa, SK-MEL-1, HepG2, HT108, and MDA-MB 231. Also, the cell adhesion and migration properties upon treatment of cell lines with complexes ⁻ and consequently, their cell death pathway via apoptosis and necrosis were analyzed. Further, complexes ⁻ were studied in vivo for their toxicities and tolerabilities in mice. In sum, the complexes ⁻ showed merits of an effective anticancer agent in cell lines⁻based study while minor side effects were observed in vivo.A green solvent extraction technology involving a microwave processing method was used to increase the content of minor ginsenosides from . This article aims to investigate the optimization of preparation of the minor ginsenosides by this microwave processing method using single-factor experiments and response surface methodology (RSM), and discuss the blood-enriching activity and hemostatic activity of the extract of microwave processed (EMPN) The RSM for production of the minor ginsenosides was based on a three-factor and three-level Box-Behnken design. When the optimum conditions of microwave power, temperature and time were 495.03 W, 150.68 °C and 20.32 min, respectively, results predicted that the yield of total minor ginsenosides (₉) would be 93.13%. The actual value of ₉ was very similar to the predicted value. In addition, the pharmacological results of EMPN in vivo showed that EMPN had the effect of enriching blood in -acetylphenylhydrazine (APH) and cyclophosphamide (CTX)-induced blood deficient mice because of the increasing content of white blood cells (WBCs) and hemoglobin (HGB) in blood. Hemostatic activity in vitro of EMPN showed that it had significantly shortened the clotting time in PT testing ( 0.05). The hemostatic effect of EMPN was mainly caused by its components of Rh₄, 20()-Rg₃ and 20()-Rg₃. This microwave processing method is simple and suitable to mass-produce the minor ginsenosides from .
三种新的过渡金属配合物 Cu(II)、Co(II)和 Zn(II),与由 1-甲基-2-氨基苯并咪唑和 2-羟基萘醛衍生的配体“bimnap”合成并进行了表征。通过单晶 X 射线衍射确定了配体的结构。使用各种光谱方法研究了所有三种配合物 ⁻ 与生物分子(小牛胸腺 DNA(CT-DNA))的相互作用模式。对 pBR322 DNA 的核酸酶活性进行了研究,结果表明该核酸酶表现出浓度依赖性的核酸降解。通过自由基清除剂存在下的电泳模式研究了 DNA 断裂的机制。此外,还分析了配合物 ⁻ 对沟结合亲和力。此外,在体外对配合物 ⁻ 对五种人癌细胞系(HeLa、SK-MEL-1、HepG2、HT108 和 MDA-MB 231)进行了细胞毒性测试。还研究了细胞系用配合物 ⁻ 处理后细胞黏附和迁移特性,以及通过细胞凋亡和坏死途径导致的细胞死亡途径。此外,还在体内研究了配合物 ⁻ 在小鼠中的毒性和耐受性。总的来说,配合物 ⁻ 在基于细胞系的研究中表现出有效的抗癌药物的优点,而在体内观察到轻微的副作用。一种涉及微波处理方法的绿色溶剂萃取技术用于从 中提高微量人参皂苷的含量。本文旨在通过单因素实验和响应面法(RSM)研究这种微波处理方法对微量人参皂苷的制备的优化,并探讨微波处理的 (EMPN)的补血和止血活性。生产微量人参皂苷的 RSM 基于三因素三水平 Box-Behnken 设计。当微波功率、温度和时间的最佳条件分别为 495.03 W、150.68°C 和 20.32 min 时,预测总微量人参皂苷(₉)的产率为 93.13%。实际的 ₉ 值与预测值非常接近。此外,EMPN 的体内药理结果表明,由于血液中白细胞(WBC)和血红蛋白(HGB)含量的增加,EMPN 对 -乙酰苯肼(APH)和环磷酰胺(CTX)诱导的血虚小鼠具有补血作用。EMPN 的体外止血活性表明,它在 PT 检测中明显缩短了凝血时间( 0.05)。EMPN 的止血作用主要是由其 Rh₄、20()-Rg₃ 和 20()-Rg₃ 成分引起的。这种微波处理方法简单,适合大规模生产 中的微量人参皂苷。