Synthesis and antitumor evaluation of sophocarpine-cinnamic acid ester derivatives as potential antitumor agents / 中草药

Objective: To synthesize sophocarpine-cinnamic acid ester derivatives and evaluate the in vitro antitumor activities of the derivatives. Methods: Taking sophocarpine as the starting material, the target compounds were synthesized by oxidation, esterification, N-alkylation, reduction, condensation, hydrolysis, and salification. Their antitumor activities in vitro were evaluated for HeLa, HepG2 and A-549 by MTT assay. Results: Eleven sophocarpine-cinnamic acid ester derivatives were synthesized and the structures were characterized by 1H-NMR, 13C-NMR and HRMS. MTT assay showed that some derivatives exhibited good antitumor activities. Compound 5g showed good antitumor activity against three human tumor cell lines, which was better than that of the positive control drug, cisplatin. Conclusion: Some derivatives showed promising antitumor activities and compound 5g was worth further studying.

Far-Infrared Optimization of the Fragrance-Improving Process with Temperature and Humidity Control for Green Tea.

In this study, a Box-Behnken design was used to explore the effect of a new technology on green tea fragrance improvement and to optimize fragrance-improving with a bilayer far-infrared fragrance-improving machine with temperature and humidity control. Based on the results of previous single-factor experiments, the main biochemical composition and sensory evaluation scores of the fragrance-improved samples were used as investigation indices. The new fragrance-improving technology was compared with the traditional far-infrared fragrance-improving process, roller pot fragrance improvement, and hot air rotary fragrance improvement. The results show that the optimal parameter combination of the new technology consists of a temperature of 128.00 °C, relative humidity of 70.00 g/h, and transmission speed of 435.00 r/min. With these process parameters, the amino acids, tea polyphenols, flavonoids, soluble sugar, catechins, and caffeine in the fragrance-improved samples reached 3.86%, 32.29%, 5.59%, 4.45%, 8.97%, and 2.75%, respectively. The quality material weight value was 11.72%. The shape, color, taste, and aroma of the fragrance-improved samples made using these parameters were found to be best, with a sensory quality score of 87.40, which is significantly higher than that of other fragrance-improving methods. The energy consumption was 0.19 RMB/kg, which was reduced by more than 50% compared with the other methods, and the production efficiency was more than 30% higher than the traditional methods. This new far-infrared fragrance-improving technology overcomes the yellowish and grayish color of fragrance-improved tea samples that is caused by the traditional fragrance-improving approach, and will provide technical guidance for actual green tea production. PRACTICAL APPLICATION: Our proposed approach innovatively integrates humidity and rotational speed as factors for fragrance improvement in Chinese tea process. The findings of this work provide new technical for fragrance improvement processes.

Characterization of the volatile components in green tea by IRAE-HS-SPME/GC-MS combined with multivariate analysis.

In the present work, a novel infrared-assisted extraction coupled to headspace solid-phase microextraction (IRAE-HS-SPME) followed by gas chromatography-mass spectrometry (GC-MS) was developed for rapid determination of the volatile components in green tea. The extraction parameters such as fiber type, sample amount, infrared power, extraction time, and infrared lamp distance were optimized by orthogonal experimental design. Under optimum conditions, a total of 82 volatile compounds in 21 green tea samples from different geographical origins were identified. Compared with classical water-bath heating, the proposed technique has remarkable advantages of considerably reducing the analytical time and high efficiency. In addition, an effective classification of green teas based on their volatile profiles was achieved by partial least square-discriminant analysis (PLS-DA) and hierarchical clustering analysis (HCA). Furthermore, the application of a dual criterion based on the variable importance in the projection (VIP) values of the PLS-DA models and on the category from one-way univariate analysis (ANOVA) allowed the identification of 12 potential volatile markers, which were considered to make the most important contribution to the discrimination of the samples. The results suggest that IRAE-HS-SPME/GC-MS technique combined with multivariate analysis offers a valuable tool to assess geographical traceability of different tea varieties.

Sensory quality evaluation for appearance of needle-shaped green tea based on computer vision and nonlinear tools.

Tea is one of the three greatest beverages in the world. In China, green tea has the largest consumption, and needle-shaped green tea, such as Maofeng tea and Sparrow Tongue tea, accounts for more than 40% of green tea (Zhu et al., 2017). The appearance of green tea is one of the important indexes during the evaluation of green tea quality. Especially in market transactions, the price of tea is usually determined by its appearance (Zhou et al., 2012). Human sensory evaluation is usually conducted by experts, and is also easily affected by various factors such as light, experience, psychological and visual factors. In the meantime, people may distinguish the slight differences between similar colors or textures, but the specific levels of the tea are hard to determine (Chen et al., 2008). As human description of color and texture is qualitative, it is hard to evaluate the sensory quality accurately, in a standard manner, and objectively. Color is an important visual property of a computer image (Xie et al., 2014; Khulal et al., 2016); texture is a visual performance of image grayscale and color changing with spatial positions, which can be used to describe the roughness and directivity of the surface of an object (Sanaeifar et al., 2016). There are already researchers who have used computer visual image technologies to identify the varieties, levels, and origins of tea (Chen et al., 2008; Xie et al., 2014; Zhu et al., 2017). Most of their research targets are crush, tear, and curl (CTC) red (green) broken tea, curly green tea (Bilochun tea), and flat-typed green tea (West Lake Dragon-well green tea) as the information sources. However, the target of the above research is to establish a qualitative evaluation method on tea quality (Fu et al., 2013). There is little literature on the sensory evaluation of the appearance quality of needle-shaped green tea, especially research on a quantitative evaluation model (Zhou et al., 2012; Zhu et al., 2017).

Multi-substituted N-phenyl-2, 2-dichloroacetamide analogues as anti-cancer drugs: design, synthesis and biological evaluation / 药学学报

Our earlier research has shown that mono-substituted N-phenyl-2, 2-dichloroacetamide exhibited much higher anti-cancer activity than the lead compound sodium dichloroacetate (DCA). In this paper, a variety of multi-substituted N-phenyl-2, 2-dichloroacetamides were synthesized and biologically evaluated. The results showed that 3, 5-disubstituted N-phenyl-2, 2-dichloroacetamide analogues had satisfactory potency. Among them, N-(3, 5-diiodophenyl)-2, 2-dichloroacetamide had an IC50 of 2.84 micromol x L(-1) against non-small cell lung cancer cell line A549 and could induce cancer cell apoptosis.

Curative effect of Xianling Qianggu koufuye on postmenopausal osteoporosis / 中国中药杂志

<p><b>OBJECTIVE</b>To study the curative effects of Xianling Qianggu koufuye (XLQG) on postmenopausal osteoporosis in ovariectomized female rats.</p><p><b>METHOD</b>Sixty female Sprague-dawley rats aged 12-months were used, 50 of them were ovariectomized and randomly divided into 5 groups: ovariectomized (OVX), OVX + Nylestriol, OVX + XLQG (high dose, middle dose, low dose), and the others were sham-operated group. Rats were treated with drugs starting at the 45 day after the operation for 90 days. Double in vivo fluorochrome labeling was administered to all rats. At the end-point of study, the blood was collected to detecte the contents of ALP and StrACP in serum, and the fourth lumar vertebra (LV4) and femur bone sections were cut and stained for bone histomorphometric analyses, biomechanical analyses and BMP analyses.</p><p><b>RESULT</b>XLQGKFY decreased greatly the StrACP content, increased BMP and bone stiffness, and improved the bone biomechanical property.</p><p><b>CONCLUSION</b>Xianling Qianggu koufuye has a curative effect on postmenopausal osteoporosis, which provides for clinical use.</p>