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[Objectives] By clustering analysis of tissue distribution data of brucine and strychnine in gastric ulcer model rat, the impact of Zuota on tissue distribution of basic components was studied. [Methods] Based on system clustering method of SPSS19.0 statistical analysis software, using inter-group join method and squared Euclidean distance, brucine and strychnine contents of different tissues and organs in non- Zuota group and Zuota group were taken as characteristic variables for clustering analysis, and phylogenetic tree was established. [Results] When clustering distance was 1, (i) taking brucine content as the index, there were three kinds of convergences in non-Zuota group. A1 class: skin, liver, epididymitis and jejunum; A2 class: brain and uterus; A class: testis and muscle. Brucine contents of the three classes showed a A1 < A2 < A. There were two classes of convergences in Zuota group. B1 class : jejunum, epididymis, kidney, brain, skin and uterus; B2 class: muscle and (bottom) submandibular gland. Brucine contents of the two classes showed as B1 < B2. (ii) Taing strychnine content as the index, there were three classes of convergences in non-Zuota group. C1 class: muscle, testicle and oarrum; C2 class: heart and lung; C3 class: uterus and liver. Strychnine contents of the three classes showed a C3 <C1 < C2. There were two kinds of convergences in Zuota group. D1 class : kidney and heart; D2 class : brain tissue and uterus. Strychnine contents of the two classes showed as D1 > D2. [Conclusions] When clustering distance was 1, low-content tissues and orgas firstly clustered, and its toxicological eefect(or pharmacodynamic action)was insignificant, and this kind of tissues and organs were relatively safe. A1 class and A2 class in Zuota group were merged into B1 class, in which liver was replaced by kidney. It iilustrated that Zuota could decline the toxicity of kidney, and enlarged the safe action range of brucine. Kidney and heart in C2 class were clustered into D1 class, and average strychnine content in C2 class was higher than that of D1 class. It could be deduced that Zuota had the effect of protecting heat.

[Objectives] To explore the mechanism for the attenuate-synergistic effect of Zuota to Renqing Mangue, a contrasted study on the tissue distribution of Tibetan medicines Renqing Mangue compatible with Zuota was carried out. [Methods] The SD rats gastric ulcer model were made successfully, and then respectively were given Renqing Mangue compatible with Zuota or not according to the dose of 0.144 g/kg and normal saline by gavage administration, once a day. After 14 d of administration, various organs and tissue were isolated, including brain, heat, liver, spleen, lung, kidney, jejunum, skeletal muscle, fat, skin, submandibular gland, uterus and ovary (or testicle and epididymis). The LC-MS/MS methods were used for determining the contents of brucine and strychnine in various organs and tissue, and significant difference analysis, main target site analysis and clustering analysis were implemented. [Results] Between the Zuota group and non-Zuota group, there was extremely significat diference in the content of brucine in the liver, kidney, muscle, lung, ovary, and heart (P < 0.01), significant difference in the jeeunum (P <0.05), and no significant diference in the epididymis, testis, brain, skin and uterus (P > 0.05); the content of brucine in the submadibular gland, spleen, liver and ovary increased significantly, but significanty reduced in the kidney, muscle, jeeunum, lung and heart. And there was extremely significant diference in the content of strychnine in the liver, kidney, ovary, brain and heat (P <0.01), and no significat difference in the uterus (P > 0.05); the strychnine content increased significantly in the liver, spleen and ovary, and significanty decreased in the kidney, muscle, testis, lung, brain and heart. [Conclusions] Compatibility of Zuota can afect the distribution of brucine and strychnine in some tissue and organs, so a to achieve attenuate-synergistic effect of Zuota to Renqing Mague. [ABSTRACT FROM AUTHOR]

To provide insights into the mechanism for the attenuate-synergistic effect of Zuota to Tibetan medicine Renqing Mangjue, a contrasted study was carried out on the pharmacokinetics of brucine and strychnine in mice plasm, which are active and toxicant ingredient in the Tibetan medicine Renqing Mangjue. LC-MS/MS was used to detect simultaneously the concentrations of brucine and strychnine in mice plasm at-different time intervals after administration parallelly and randomly, and the pharmacokinetic software Kinetica 5. 0 was selected to non-compartmental analysis (NCA) for data, and statistical analysis software SPSS 19. 0 was used for significance test on the pharmacokinetic parameters. A reliable LC-MS/MS method was established for the determination of brucine and strychnine in blood plasma, which are consistent with the requirements of the preclinical pharmacokinetic study confirmed by the methodology. The linear concentration ranges of brucine and strychnine were 0.301-104.4 µg · L(-1) (r = 0.999 5) and 0.305-106 µg · L(-1) (r = 0.999 7), respectively; The intra-day and inter-day variable coefficients were both less than 10.0% with good precision; The average extraction recoveries of brucine and strychnine were 116.23% and 112.82%, and RSD were 3.2% and 2.3% separately;The average matrix effects of brucine and strychnine were 122.48% and 116.36%, and RSD were 7.7% and 4.4%, respectively. The pharmacokinetic results showed that AUCtot of brucine and strychnine in Zuota group were both increased remarkably (P < 0.05), and the Cmax of brucine in Zuota group was about 5.25-fold higher than that of brucine in non-Zuota group (P < 0.05). The Tmax of brucine and strychnine reduced to one-eighth and one-quarter respectively compared with those in Non-Zuota group. In addition, the eliminations of brucine and strychnine in vivo were accelerated after the compatibility of Zuota. A significant difference (P < 0.05) occurred at the MRT0-t, of brucine, while the MRT0-∞ and Lz of strychnine were statistically significant upon the inspection level α = 0.1. It was found that the absorption degree of brucine and strychnine in Zuota group increased in the range of the safe dose (or concentration), while their elimination rates were accelerated, which may be one of the mechanisms for attenuate-synergistic effect of Zuota to Tibetan medicine Renqing Mangjue.

A methanol extract of everlasting flowers of <i>Helichrysum arenarium</i> L. Moench (Asteraceae) was found to inhibit the increase in blood glucose elevation in sucrose-loaded mice at 500 mg/kg p.o. The methanol extract also inhibited the enzymatic activity against dipeptidyl peptidase-IV (DPP-IV, IC<sub>50</sub> = 41.2 μg/ml), but did not show intestinal <i>α</i>-glucosidase inhibitory activities. From the extract, three new dimeric dihydrochalcone glycosides, arenariumosides V-VII (<i>2</i>-<i>4</i>), were isolated, and the stereostructures were elucidated based on their spectroscopic properties and chemical evidence. Of the constituents, several flavonoid constituents, including <i>2</i>-<i>4</i>, were isolated, and these isolated constituents were investigated for their DPP-IV inhibitory effects. Among them, chalconaringenin 2′-<i>O</i>-<i>β</i>-D-glucopyranoside (<i>16</i>, IC<sub>50</sub> = 23.1 μM) and aureusidin 6-<i>O</i>-<i>β</i>-D-glucopyranoside (<i>35</i>, 24.3 μM) showed relatively strong inhibitory activities.

Zuotais regarded as the king of Tibetan medicine. However, the major starting material ofZuotais mercury, which is one very toxic heavy metal. This has aroused serious doubts on the biosafety ofZuotacontaining drugs. In this study, we quantified the Hg contents in fourZuotasamples, monitored the release of Hg in simulated gastric/intestinal juice and evaluated their cytotoxicity to Caco-2 cells. Our results showed that the Hg contents inZuotasamples were in the range of 566–676 mg/g. Fortunately, the release of Hg fromZuotasamples was very low in simulated gastric juice, and much lower in simulated intestinal juice. Direct contact ofZuotawith Caco-2 cells led to dose-dependent cytotoxicity, including activity loss and membrane leakage. The toxicity was closely related to apoptosis, because the caspase 3/7 levels of Caco-2 cells increased after the exposure toZuota. Interestingly,Zuotasamples inhibited the oxidative stress at low concentrations, but the toxicity could be relived by antioxidants. The possible toxicity should be attributed to the cellular uptake ofZuotaparticulates. Beyond the cytotoxicity, significant differences amongZuotasamples from different institutions were observed, suggesting that the preparation process ofZuotahad meaningful influence of its biosafety. The implications to the safety and clinical applications ofZuotaare discussed. [ABSTRACT FROM AUTHOR]