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Caesalpinia sappan (CS) has been commonly used in beverage and folk medicine in China and ASEAN countries because of its various therapeutic properties. Only the heartwood has long been used in traditional medicines due to the presence of high concentration of brazilin (one of the most important bioactive compounds), whereas the other parts are limited in use. Thus, this work aimed to investigate ways of utilizing other parts of CS. This information is important for further use of other CS parts to promote zero waste and hence sustainable resource utilization. Herein, the crude ethanolic (CEE) and crude aqueous (CAE) extracts from twelve parts of CS were evaluated for their biological activities for the first time. Our work demonstrates that not only the heartwood, but also other parts of CS exhibit interesting biological activities. CAE from heartwood of branches exhibits the highest antioxidant activity, which is higher than that of the positive control, butylated hydroxytoluene. CEE from florets shows the highest inhibitory effect against α-amylase, while CAE of barks shows better α-glucosidase inhibitory activity than the existing glucosidase inhibitor (acarbose). Molecular docking of brazilin (key bioactive compound) to both α-amylase and glucosidase can also confirm the tight binding of brazilin to α-glucosidase. [ABSTRACT FROM AUTHOR]

Diabetes is a chronic metabolic disease, whereas α-glucosidases are key enzymes involved in the metabolism of starch and glycogen. There is a long history of the use of mulberry leaf (the leaf of Morus alba) as an antidiabetic herb in China, and we found that chalcomoracin, one of the specific Diels–Alder adducts in mulberry leaf, had prominent α-glucosidase inhibitory activity and has the potential to be a substitute for current hypoglycemic drugs such as acarbose, which have severe gastrointestinal side effects. In this study, chalcomoracin was effectively isolated from mulberry leaves, and its α-glucosidase inhibition was studied via enzymatic kinetics, isothermal titration (ITC) and molecular docking. The results showed that chalcomoracin inhibited α-glucosidase through both competitive and non-competitive manners, and its inhibitory activity was stronger than that of 1-doxymycin (1-DNJ) but slightly weaker than that of acarbose. ITC analysis revealed that the combination of chalcomoracin and α-glucosidase was an entropy-driven spontaneous reaction, and the molecular docking results also verified this conclusion. During the binding process, chalcomoracin went into the "pocket" of α-glucosidase via hydrophobic interactions, and it is linked with residues Val544, Asp95, Ala93, Gly119, Arg275 and Pro287 by hydrogen bonds. This study provided a potential compound for the prevention and treatment of diabetes and a theoretical basis for the discovery of novel candidates for α-glycosidase inhibitors. [ABSTRACT FROM AUTHOR]

Background: The prevalence of diabetes mellitus remains high in China, and more cardiovascular and cerebrovascular adverse events due to diabetes mellitus are likely to occur in the future. Objective: To analyze the gap between the current pharmacotherapy management and the guidelines for inpatients with type 2 diabetes mellitus from the perspective of pharmacists so as to provide a reference for optimal pharmacotherapy management methods and models for patients with type 2 diabetes mellitus. Methods: The study was a cross-sectional observational study. The study was conducted by investigating and analyzing the use of glucose-lowering drugs, adjustment of blood pressure management strategy, lipid management, weight management, and application of antiplatelet drugs in type 2 diabetes inpatients. Results: A total of 1086 patients with type 2 diabetes were included. Metformin, glycosidase inhibitors, and basal insulin were the most used among type 2 diabetes inpatients. The use of SGLT-2, GLP-1 RAs, DPP-4, and metformin all showed significant increase. SGLT-2 inhibitors (SGLT-2i) showed the fastest increase from 2020 to 2021 (14.5% vs. 39.6%); However, the application rate of SGLT-2i was low among patients with combined ASCVD, renal insufficiency, and diabetic nephropathy (46.4%, 40.9%, and 45.8% respectively). For patients with substandard blood pressure at admission, the average rate of intervention by endocrinologists for adjusting the antihypertensive regimen during hospitalization was 55.6%, and the application rate of ACEI/ARB drugs reached 64.4%. The application rate of statins among patients with type 2 diabetes was still relatively high, at 78.8%. However, the overall intervention rate for patients with suboptimal LDL-c was only 24.1%. The application rate of antiplatelet agents for patients with ASCVD was 77.6%, which was higher than that for patients without ASCVD. Conclusion: There is still a gap between the practice of medication treatment management of Chinese inpatients with type 2 diabetes and the guidelines, especially in the application of GLP-1RAs and SGLT-2i in patients with concomitant ASCVD, diabetic nephropathy, and renal insufficiency. Meanwhile, physicians and pharmacists should pay more attention on achieving blood pressure and LDL-c standards in type 2 diabetic patients and provide timely interventions. [ABSTRACT FROM AUTHOR]

Summary: Objective: For severe, critical and fatal cases of 2009 H1N1 influenza in the winter in the Northern Hemisphere, the detailed features are not fully known. The aim of this study was to examine these features through describing these cases in Beijing, China in 2009. Methods: Data on severe, critical and fatal cases were collected via the Notifiable Disease Surveillance System and a designated surveillance system for managing 2009 H1N1 influenza cases in Beijing. The characteristics and risk factors of these cases were elucidated. Results: A total of 475 severe cases, 73 critical ones and 69 deaths were identified in 2009. The proportion of obesity was low, as well as pregnancy. About half of them had no underlying disease. Most of deaths had multi-organ failure, with a median interval from illness onset to death of ten days. Delay in visiting hospital, cardiovascular disease and allergy predicted a higher risk of severe disease, and cases aged 6–17 years were at lower risk. Cases not promptly receiving neuraminidase inhibitors were at increased risk of death. Conclusions: Age and underlying disease are significantly associated with severity of outcomes of 2009 H1N1 influenza; prompt presentation to hospital and use of neuraminidase inhibitor were protective. [ABSTRACT FROM AUTHOR]

As a by-product in the sericulture industry, mulberry branches are not currently utilized effectively. Jialing 20 is an artificial triploids mulberry that widely cultivated in southwest China. In this study, the chemical composition of the Jialing 20 mulberry branch extract (MBE) was first analyzed by UPLC-MS/MS, and 42 components, including alkaloids, flavonoids, and coumarins, were obtained. Then, the antioxidant activities, hypoglycemic effect, Alzheimer's disease inhibition, and cardiovascular protection of MBE were also evaluated in vitro. The IC50 values for the scavenging DPPH and ABTS radicals were, respectively, 31.23 ± 0.57 μg/mL and 8.88 ± 0.36 μg/mL (IC50 values of positive Vc were, respectively, 4.41 ± 0.19 μg/mL and 8.79 ± 0.41 μg/mL). The IC50 value for inhibiting α-glucosidase was 1.90 ± 0.05 μg/mL (IC50 value of positive acarbose was 0.03 μg/mL). The IC50 values for inhibiting acetylcholinesterase and butyrylcholinesterase were, respectively, 179.47 ± 0.38 μg/mL and 101.82 ± 3.37 μg/mL (IC50 values of positive berberine were, respectively, 1.27 ± 0.03 μg/mL and 57.41 ± 0.21 μg/mL). MBE (10 μg/mL and 40 μg/mL) significantly increased the survival rate of oxidized low-density lipoprotein- (ox-LDL) induced human umbilical vein endothelial cells (HUVECs) and significantly decreased the intracellular reactive oxygen species. These results suggest that the extracts of Jialing 20 mulberry branches could be used as a functional food additive. [ABSTRACT FROM AUTHOR]