Phytochemical Analysis and Anti-Ascaris suum Activity of Different Zanthoxylum Species In Vitro and In Vivo.

Zanthoxylum plants (ZPs), including multiple Chinese prickly ash species, are dual-purpose functional foods favored by the general population around the world in foods, cosmetics, and traditional medicines and have antipruritic, insecticidal, and fungicidal bioactivities. For the first time, the anti-roundworm bioactivity of ZPs and the active ingredients were compared and investigated. Through nontarget metabolomics following targeted quantitative analysis, qinbunamides, sanshools, sanshooel, asarinin, and sesamin were found to be the main different components of Zanthoxylum species. Coincidentally, the 12 chemical components were also the dominant anti-roundworm ingredients of ZP extracts. The extracts of three species of Chinese prickly ash (1 mg/mL) decreased the hatchability of roundworm eggs significantly, and the ChuanJiao seed killed roundworms (insecticidal rate 100%) and alleviated the symptoms of pneumonia in mice. Furthermore, retention time-accurate mass-tandem mass spectrometry-ion ratio (RT-AM-MS/MS-IR) were modeled by assaying 108 authentic compounds of ZP extracts, and 20 metabolites were confidently identified in biological samples from ZP extract-treated mice by analyzing the m/z values and the empirical substructures. This study provides a good reference for the proper application of ZPs.

Orthogonal test design for optimizing culture medium for in vitro pollen germination of interspecific oil tea hybrids.

Oil Tea (Camellia oleifera) is an important woody edible oil plant in China. Oil Tea suffers from low rate of fruit set during production, which is related to poor pollination and fertilization. Pollen vigor is directly related to pollination and fertilization. Using the interspecific hybrid Y3 (C. grijsii × C. oleifera) as plant material, we studied the effects of sucrose, H3BO3, MgSO4, and IAA on pollen germination using an orthogonal design to determine the best culture medium. Results indicated that pollen germination rates were significantly affected by medium components and ranged from 29.13% to 56.84%. Pollen tube length was the longest in the T5 medium surpassing the control group by 489.36 µm. MgSO4 turned out to be the most important germination medium component having great effect on the pollen germination rate. The optimal culture medium to promote pollen tube growth of Oil Tea Y3 was: 1% agar, 150 g·L-1 sucrose, 0.15 g·L-1 H3BO3, 0.07 g·L-1 MgSO4, and 0.01 g·L-1 IAA. The results of this paper may provide information for foliar application of Mg and IAA, which can improve pollen tube growth of Oil Tea in practice.

Discovery of novel potent GPR40 agonists containing imidazo[1,2-a]pyridine core as antidiabetic agents.

Free fatty acid receptor 1 (FFA1 or GPR40) has been studied for many years as a target for the treatment of type 2 diabetes mellitus. In order to increase potency and reduce hepatotoxicity, a series of novel compounds containing imidazo[1,2-a]pyridine scaffold as GPR40 agonist were synthesized. Compound I-14 was identified as an effective agonist as shown by the conspicuous drop in blood glucose in normal and diabetic mice. It had no risk of hepatotoxicity compared with TAK-875. Moreover, good pharmacokinetic (PK) properties of I-14 were observed (CL = 27.26 ml/h/kg, t1/2 = 5.93 h). The results indicate that I-14 could serve as a possible candidate to treat diabetes.

Self-sterility in Camellia oleifera may be due to the prezygotic late-acting self-incompatibility.

In this report, self-sterility in Camellia oleifera was explored by comparing structural and statistical characteristics following self-pollination (SP) and cross-pollination (CP). Although slightly delayed pollen germination and pollen tube growth in selfed ovaries compared to crossed ovaries was observed, there was no significant difference in the percentages of pollen that germinated and pollen tubes that grew to the base of the style. There was also no difference in morphological structure after the two pollination treatments. However, the proportions of ovule penetration and double fertilization in selfed ovules were significantly lower than in crossed ovules, indicating that a prezygotic late-acting self-incompatible mechanism may exist in C. oleifera. Callose deposition was observed in selfed abortive ovules, but not in normal. Ovules did not show differences in anatomic structure during embryonic development, whereas significant differences were observed in the final fruit and seed set. In addition, aborted ovules in selfed ovaries occurred within 35 days after SP and prior to zygote division. However, this process did not occur continuously throughout the life cycle, and no zygotes were observed in the selfed abortive ovules. These results indicated that the self-sterility in C. oleifera may be caused by prezygotic late-acting self-incompatibility (LSI).

Hypoglycemic effect of polysaccharide enriched extract of Astragalus membranaceus in diet induced insulin resistant C57BL/6J mice and its potential mechanism.

Our previous studies found that Astragalus polysaccharide (APS) exerts insulin-sensitizing and hypoglycemic activities in type 2 diabetic (T2DM) rats. The present study was designed to further confirm the hypoglycemic effect of APS and to investigate its possible mechanism underlying the improvement of insulin resistance in vivo and in vitro. Diet-induced insulin resistant C57BL/6J mice treated with or without APS (orally, 700 mg/kg/d) for 8 weeks were analyzed and compared. Simultaneously, an insulin resistant C(2)C(12) cell model and an ER stressed HepG2 cell model were established and incubated with or without APS (200 microg/ml) for 24h respectively. Systematic insulin sensitivity was measured with an insulin-tolerance test (ITT) and an homeostasis model assessment (HOMA IR) index. Metabolic stress variation was analyzed for biochemical parameters and pathological variations. The expression and activity of protein tyrosine phosphatase 1B (PTP1B), which plays a very important role in insulin signaling and in the ER stress response, was measured by immunoprecipitation and Western blot. The ER stress response was analyzed through XBP1 transcription and splicing by real-time PCR. APS could alleviate insulin resistance and ER stress induced by high glucose in vivo and in vitro, respectively. The hyperglycemia, hypolipemia, and hyperinsulinemia status were controlled with APS therapy. Insulin action in the liver of insulin resistant mice was restored significantly with APS administration. APS enhanced adaptive capacity of the ER and promoted insulin signaling by the inhibition of the expression and activity of PTP1B. Furthermore, the anti-obesity effect and hypolipidemia effects of APS were probably due partly to decreasing the leptin resistance of mice, which would positively couple with the normalization of plasma insulin levels. We have shown that APS has beneficial effects on insulin resistance and hyperglycemia. The mechanism is related to the alleviation of ER stress and insulin resistance under hyperglycemia conditions.