Endogenous crude Scutellaria baicalensis polysaccharide robustly enhances one-pot extraction and deglycosylation of baicalin.

With the extensive application of baicalein in the treatment of cardiovascular and cerebrovascular diseases, its clinical and market demand has gradually expanded. But the natural yield of baicalein is very low, and it is mainly prepared by the deglycosylation of baicalin. However, the insolubility of baicalin in water significantly limits the deglycosylation of it under biocatalysis. To make biocatalysis of baicalin more efficient and environmental, a strategy was designed to enhance its water solubility through the solubilization mechanism of endogenous biological macromolecules, and the effect on the activity of glucuronidase was further explored. The results showed that wrapping with Scutellaria baicalensis polysaccharide (SBP) significantly improved the solubility of baicalin in water (the water solubility of baicalin increased by 23 times, BI/SBP = 1/12, w/w). It was not only contributed to the efficient production of baicalein by one-pot method, but also effectively improved the deglycosylation rate of baicalin (increase by 47.04 % in aqueous solution). With the help of the solubilization of endogenous polysaccharide on baicalin in aqueous solution, a green, low-cost and efficient method (one-pot method) was designed to simultaneously extract and enzymatic hydrolyze baicalin to prepare baicalein. Under the same conditions, the yield of one-pot method is 87.17 %, which was much higher than that of the conventional method (29.38 %). In addition, one-pot method with the aid of endogenous polysaccharide could simply and conveniently prepare aglycone of other insoluble natural flavonoids, which has a wide range of industrial application value.

Efficacy and initial dose determination of paricalcitol for treatment of secondary hyperparathyroidism in Chinese subjects.

AIM: Prevalence of secondary hyperparathyroidism (SHPT), a renal disease complication, is increasing in China. Available therapies may not optimally control SHPT, particularly in patients with hypercalcemia, hyperphosphatemia, and parathyroid hyperplasia. This study examined efficacy and safety of two dosing regimens of selective vitamin D receptor activator paricalcitol. MATERIALS AND METHODS: Subjects with SHPT (n = 216) undergoing hemodialysis were treated with paricalcitol i.v. for 12 weeks. One group was treated according to the EU paricalcitol package insert (PI) (initial µg dose based on iPTH/80), and the other was treated according to the US PI (initial dose of 0.04 µg/kg). Dose titration was based on iPTH and serum calcium (Ca) and phosphorus (P) levels. RESULTS: The primary endpoint of two consecutive ≥ 30% iPTH decreases was achieved by 88.6% and 55.9% of subjects in the EU and US PI groups, respectively. Noninferiority of the EU PI group vs. the US PI group was demonstrated (lower bound of the 1-sided 97.5% CI = 21.3%). Superiority of the EU PI group was shown (lower limit > 0%) and confirmed by Fisher's exact test (p < 0.001); both groups showed similar achievement of recommended KDIGO iPTH levels. Ca and P levels were relatively constant. CONCLUSION: Both EU and US PI paricalcitol dosing strategies effectively reduced iPTH levels in Chinese subjects with SHPT, with minimal impact on Ca and P levels.

[Effects of Astragalus on expression of renal angiopoietin receptor Tie-2 in diabetic rats].

OBJECTIVE: To study the expression of angiopoietin receptor Tie-2 in the renal tissue of diabetic rats and the effects of Astragalus. METHODS: SD rats were randomly divided into normal control group, diabetes group and Astragalus-treated group. The expression of receptor Tie-2 in the renal tissue was assessed by using real-time quantitative polymerase chain reaction and immunohistochemical method. RESULTS: Glomerule Tie-2 protein expression was significantly elevated in the diabetes group as compared with the normal control group (P<0.01). Glomerule Tie-2 protein expression in the Astragalus-treated group was decreased as compared with the diabetes group (P<0.01). CONCLUSION: Tie-2 may play an important role in the pathogenesis of the early stage diabetic renal injury. The reno-protection effect of Astragalus may be mediated by down-regulating the expression of Tie-2 in the kidney tissue of diabetic rats.