Study on law of quality value transmitting of Artemisiae Scopariae Herba standard decoction / 中草药

Objective: To study the law of quality value transmitting of Artemisiae Scopariae Herba (ASH) standard decoction. Methods: Fifteen batches of ASH standard decoction were prepared. Fingerprints of these 15 batches standard decoction and its raw pieces were determined by HPLC, the control fingerprints were established, the common peaks were calibrated and the similarity was evaluated. Components of common peaks were identified by Q-TOF/MS and the contents of components confirmed by reference substance were determined. The common peaks transfer number, peak area ratio, index components transfer rate and extraction rate were used to analyze the quality value transfer rule of standard decoction. Results: The similarity of fingerprints of ASH and its standard decoction were greater than 0.9, 16 and 15 common peaks were calibrated respectively, and the transfer rate of the common peaks number was 93.75%. Thirteen components of the common peaks were confirmed by reference substance, including 1-caffeoylquinic acid, neochlorogenic acid, chlorogenic acid, caffeic acid, cryptochlorogenic acid, p-hydroxyacetophenone, 1,3-dicaffeoylquinic acid, rutin, hyperoside, isoquercetin, 3,4-dicaffeoylquinic acid, 3,5-dicaffeoylquinic acid, 4,5-dicaffeoylquinic acid. Caffeoylquinic acid glucoside and a di-C-glycoside named apigenin 6,8-di-C-β-D-glucoside were first detected in ASH. The ratio of the common peaks area of ASH standard decoction to that of ASH raw pieces showed a good positive linear relationship with the components transfer rate. The average transfer rates of neochlorogenic acid, cryptochlorogenic acid, 1,3-dicaffeoylquinic acid and 3,4-dicaffeoylquinic acid were more than 100%, while the average transfer rates of chlorogenic acid and 3,5-dicaffeoylquinic acid were only 47.59% and 22.33% respectively, suggesting that the organic acid components may be transformed into each other during the preparation of standard decoction, and part of chlorogenic acid may be transformed into cryptochlorogenic acid and neochlorogenic acid; 3,5-dicaffeoylquinic acid may be partially converted into 1,3-dicaffeoylquinic acid and 3,4-dicaffeoylquinic acid. The average transfer rates of rutin and hyperoside were 31.36% and 28.36%, respectively, and that of other components were between 50% and 70%. The average extraction rate of standard decoction was 19.76%. Conclusion: The laws of quality value transmitting of ASH standard decoction revealed in this study laid a foundation for the establishment of the material reference of ASH formula granules and the classic prescriptions containing ASH.

Synthesis and antitumor activity of fluoroquinolon-3-yl-s-triazole sulfide ketones and their derivatives from ciprofloxacin / 药学学报

To discover an efficient strategy for the conversion of the antibacterial activity of fluoroquinolones into the antitumor activity, the three series of C-3 s-triazole-based derivatives including sulfide ketones (6a-6g), thiosemicarbazones (7a-7g) and fused heterocyclic thiazolotriazoles (8a-8g) were synthesized from ciprofloxacin (1), respectively. The structures were characterized by elemental analysis and spectral data. The antitumor activity was tested against three tumor cell lines (Hep-3B, Capan-1 and HL60) using the MTT assay. The three types of compounds all exhibited stronger anti-proliferative activities than ciprofloxacin in the test. The order of their activities was in compounds 7>8>6, and the order of selectivity against cancer cell lines was Capan-1, Hep-3B and HL60. Meanwhile, the SAR revealed that some compounds with electron-drawing group substituted such as fluoro- and nitro-phenyl compounds (6f, 7f, 8f) and (6g, 7g, 8g) displayed more significant activity than the control compounds, especially the IC50 values of thiosemicarbazone compounds 7f and 7g against Capan-1 was comparable to doxorubicin. Thus, a five-membered triazole as the C-3 bioisostere modified with the functionalized side-chain of sulfide-ketone thiosemicarbazone warrants special attention and further investigation.

Synthesis and anti-proliferative activity of fluoroquinolone C-3 fused heterocyclic α,β-unsaturated ketones derived from ciprofloxacin / 药学学报

To discover novel antitumor fluoroquinolone lead compounds from a rational modification for antibacterial fluoroquinolones, a fused heterocyclic ketone corresponding to thiazolo[2,3- b][1,2,4]triazolone used as a bioisosteric replacement of the C-3 carboxylic acid group of ciprofloxacin 1, and further modification by a Claisen condensation reaction with substituted benzaldehydes formed novel fluoroquinolone C-3 fuse heterocyclic α, β-unsaturated ketones as the title compounds (6a-6r), separately. The structures of eighteen title compounds were characterized by elemental analysis, 1H NMR and MS, and the in vitro anti-proliferative activity against human hepatoma Hep-3B cells, pancreatic Capan-1 cells and leukemia HL60 cells was evaluated by a MTT assay. The preliminary results showed that the title compounds not only had more significant anti-proliferative activity against three tested cancer cell lines than that of the parent ciprofloxacin 1, but also exhibited the highest activity against Capan-1 cells. In particular, compounds carrying an electron-withdrawing carboxyl (6k, 6m) or sulfonamide substituent (6q, 6r) attached to benzene ring were comparable to or better than constractive drug doxorubicin against Capan-1 cells. As such, it suggests that it is favorable for a fused heterocyclic α, β-unsaturated ketone scaffold instead of the C-3 carboxylic acid group to improve the antitumor activity of fluoroquinolones.

Synthesis and anti-proliferative activity of fluoroquinolone (rhodanine unsaturated ketone) amide derivatives / 药学学报

To discover novel antitumor rhodanine unsaturated ketones, a series of fluoroquinolone (rhodanine α, β-unsaturated ketone) amine derivatives (5a-5r) were designed and synthesized with fluoroquinolone amide scaffold as a carrier. The structures of eighteen title compounds were characterized by elemental analysis, 1H NMR and MS. The in vitro anti-proliferative activity against Hep-3B, Capan-1 and HL60 cells was evaluated by MTT assay. The results showed that the title compounds not only had more significant anti-proliferative activity against three tested cancer cell lines than that of the parent ciprofloxacin 1, but also exhibited the highest activity against Capan-1 cells. The SAR revealed that some compounds carrying aromatic heterocyclic rings or phenyl attached to an electron-withdrawing carboxyl or sulfonamide substituent were comparable to or better than comparison doxorubicin against Capan-1 cells. As such, it suggests that fluoroquinolone (rhodanine α, β-unsaturated ketone) amines are promising leads for the development of novel antitumor fluoroquinolones or rhodanine analogues.

The design of a cardiac monitoring and analysing system with low power consumption / 中国医疗器械杂志

The paper deals with a portable analyzing monitor system with liquid crystal display (LCD), which is low in power consumption and suitable for China's specific conditions. Apart from the development of the overall scheme of the system, the paper introduces the design of the hardware and the software. The 80196 single chip microcomputer is used as the central microprocessor to process and real-time electrocardiac signal data. The system have the following functions: five types of arrhythmia analysis, alarm, freeze, and record of automatic paperfeeding. The portable system can be operated by alternate-current (AC) or direct-current (DC). Its hardware circuit is simplified and its software structure is optimized. Multiple low power consumption and LCD unit are adopted in its modular designs.