Effects of a combination of Poria Cocos, Ziziphus spinose, and gamma‐aminobutyric acid (GABA) on sleep quality and skin health: A randomized double‐blind placebo‐controlled clinical trial

Article

Author: Hao, Yining ; Qu, Liping ; Song, Weimin

AbstractSleep is crucial for preserving both physical and mental health, including skin health. Presently, there is a burgeoning interest in the use of herbal and natural ingredients to mitigate the adverse effects of sleep disorders. In this 4‐week, randomized, double‐blind, controlled trial, 70 subjects with sleep disorders were randomly assigned to receive either a placebo or a Poria cocos, Ziziphus spinose, and GABA (PZG) supplement (10 mL per day). Total sleep duration was detected by wrist actigraphy, and sleep quality was assessed by the Pittsburgh Sleep Quality Index (PSQI). Skin conditions were evaluated based on assessments of skin hydration, glossiness elasticity, color, severity of wrinkles, and skin roughness. After 4 weeks, the total sleep duration significantly increased by 12.96% (p = .006) and the PSQI score notably decreased by 59.94% (p = .000) compared to the baseline. Notably, compared to the baseline conditions, skin hydration, radiance, elasticity, firmness, wrinkle severity, and roughness were significantly improved in the PZG group. In addition, the PZG group demonstrated significantly greater improvements than the placebo group in terms of changes from baseline in total sleep duration, PSQI score, skin hydration, wrinkle severity, and skin roughness. The present results demonstrated that the combined intake of herbs and GABA can improve sleep quality and enhance skin health without adverse effects.

15 Aug 2022·Reviews in Cardiovascular Medicine

The Remaining Conundrum of the Role of the Na+/H+ Exchanger Isoform 1 (NHE1) in Cardiac Physiology and Pathology: Can It Be Rectified?

Review

Author: Fliegel, Larry ; Karmazyn, Morris ; Pierce, Grant N

The mammalian __-mml:math xmlns:mml="http://www.w3.org/1998/Math/MathML"-__Na + __-mml:math xmlns:mml="http://www.w3.org/1998/Math/MathML"-__/H + exchanger (NHE) is a family of ubiquitous membrane proteins present in humans. Isoform one (NHE1) is present on the plasma membrane and regulates intracellular pH by removal of one intracellular proton in exchange for one extracellular sodium thus functioning as an electroneutral process. Human NHE1 has a 500 amino acid membrane domain plus a C-terminal 315 amino acid, regulatory cytosolic tail. It is regulated through a cytosolic regulatory C-terminal tail which is subject to phosphorylation and is modulated by proteins and lipids. Substantial evidence has implicated NHE1 activity in both myocardial ischemia and reperfusion damage and myocardial remodeling resulting in heart failure. Experimental data show excellent cardioprotection with NHE1 inhibitors although results from clinical results have been mixed. In cardiac surgery patients receiving the NHE1 inhibitor cariporide, subgroups showed beneficial effects of treatment. However, in one trial this was associated with a significantly increased incidence of ischemic strokes. This likely reflected both inappropriate dosing regimens as well as overly high drug doses. We suggest that further progress towards NHE1 inhibition as a treatment for cardiovascular disease is warranted through the development of novel compounds to inhibit NHE1 that are structurally different than those previously used in compromised clinical trials. Some novel pyrazinoyl guanidine inhibitors of NHE1 are already in development and the recent elucidation of the three-dimensional structure of the NHE1 protein and identity of the inhibitor binding site may facilitate development. An alternative approach may also be to control the endogenous regulation of activity of NHE1, which is activated in disease.

28 Feb 2018·Journal of Agricultural and Food ChemistryQ1 · AGRICULTURAL & FORESTRY SCIENCE

Novel RAS Inhibitors Poricoic Acid ZG and Poricoic Acid ZH Attenuate Renal Fibrosis via a Wnt/β-Catenin Pathway and Targeted Phosphorylation of smad3 Signaling

Q1 · AGRICULTURAL & FORESTRY SCIENCE

Article

Author: Liu, Dan ; Vaziri, Nosratola D. ; Guo, Yan ; Wang, Ming ; Zhao, Ying-Yong ; Chen, Dan-Qian ; Zhao, Hui ; Zhang, Zhi-Hao ; Cao, Gang ; Chen, Lin

Renal fibrosis is a common end point of the progression of chronic kidney disease (CKD). Suppressing the development and progression of renal fibrosis is essential in the treatment of kidney disease. Our previous study demonstrated that the ethyl acetate extract of the surface layer of Poria cocos exhibited beneficial antitubulointerstitial fibrosis. In this study, we isolated new diterpene (PZF) and triterpenes (PZG and PZH) and examined their antifibrotic effect. TGF-β1 upregulated the collagen I protein expression in HK-2 cells, and PZG and PZH treatment significantly inhibited the upregulated collagen I expression (TGF group 0.59 ± 0.08 vs TGF+PZG group 0.36 ± 0.08, P < 0.01; TGF+PZH group 0.39 ± 0.12, P < 0.01). Triterpenes, PZG and PZH, exhibited a stronger inhibitory effect on renal fibrosis and podocyte injury than PZF. PZG and PZH further showed a stronger inhibitory effect on the activation of the renin-angiotensin system (RAS) than PZF. Additionally, PZG and PZH markedly inhibited the activation of Wnt/β-catenin signaling, which played an important role in fibrogenesis. Interestingly, PZG and PZH suppressed the TGF-β/Smad pathway by selectively inhibiting the phosphorylation of Smad3 through blocking the interactions of SARA with TGFβI and Smad3. The analysis of the structure-activity relationship demonstrated that their antifibrotic effects were closely associated with the first six-membered ring structure and the number of carboxyl groups in this type of compounds. Additionally, fifteen known triterpenes were identified. These novel tetracyclic triterpenoid compounds provided the potential lead compounds for the research and development of antifibrosis drug, and they possessed the potential to be utilized as RAS inhibitors.

100 Deals associated with Pyrazinoylguanidine

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Indication	Highest Phase	Country/Location	Organization	Date
Diabetes Complications	Phase 2	US	SuperGen, Inc.	-
Diabetes Mellitus, Type 2	Phase 2	-	Pennsylvania State University College of Medicine	-
Diabetes Mellitus, Type 2	Phase 2	US	SuperGen, Inc.	-
Hyperlipidemias	Phase 2	US	SuperGen, Inc.	-
Diabetes Mellitus, Type 2	Preclinical	-	Astex Pharmaceuticals, Inc.	-

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