Month: December 2022

Li, Qiaofeng published the artcileA network pharmacology-based approach to explore the active ingredients and molecular mechanism of Lei-gong-gen formula granule on a spontaneously hypertensive rat model, COA of Formula: C10H18O, the main research area is Lei gong gen spontaneous hyertension NOS3 SRC; Centella asiatica (L.) Urb.; Eclipta prostrata (L.) L.; Hypertension; Network pharmacology; Smilax glabra Roxb..

Lei-gong-gen formula granule (LFG) is a folk prescription derived from Zhuang nationality, the largest ethnic minority among 56 nationalities in China. It consists of three herbs, namely Eclipta prostrata (L.) L., Smilax glabra Roxb, and Centella asiatica (L.) Urb. It has been widely used as health protection tea for hundreds of years to prevent hypertension in Guangxi Zhuang Autonomous Region. The purpose of this study is to validate the antihypertensive effect of LFG on the spontaneously hypertensive rat (SHR) model, and to further identify the effective components and anti-hypertension mechanism of LFG. The effects of LFG on blood pressure, body weight, and heart rate were investigated in vivo using the SHR model. The levels of NO, ANG II, and ET-1 in the serum were measured, and pathol. changes in the heart were examined by H&E staining. The main active components of LFG, their corresponding targets, and hypertension associated pathways were discerned through network pharmacol. anal. based on the Traditional Chinese Medicine Systems Pharmacol. (TCMSP), Traditional Chinese Medicine Integrated Database (TCMID), and the Bioinformatics Anal. Tool for Mol. Mechanism of Traditional Chinese Medicine (BATMAN-TCM). Then the predicted results were further verified by mol. biol. experiments such as RT-qPCR and western blot. Addnl., the potential active compounds were predicted by mol. docking technol., and the chem. constituents of LFG were analyzed and identified by UPLC-QTOF/MS technol. Finally, an in vitro assay was performed to investigate the protective effects of potential active compounds against hydrogen peroxide (H2O2) induced oxidative damage in human umbilical vein endothelial cells (HUVEC). LFG could effectively reduce blood pressure and increase serum NO content in SHR model. Histol. results showed that LFG could ameliorate pathol. changes such as cardiac hypertrophy and interstitial inflammation. From network pharmacol. anal., 53 candidate active compounds of LFG were collected, which linked to 765 potential targets, and 828 hypertension associated targets were retrieved, from which 12 overlapped targets both related to candidate active compounds from LFG and hypertension were screened and used as the potential targets of LFG on antihypertensive effect. The mol. biol. experiments of the 12 overlapped targets showed that LFG could upregulate the mRNA and protein expressions of NOS3 and proto-oncogene tyrosine-protein kinase SRC (SRC) in the thoracic aorta. Pathway enrichment anal. showed that the PI3K-AKT signaling pathway was closely related to the expression of NOS3 and SRC. Moreover, western blot results showed that LFG significantly increased the protein expression levels of PI3K and phosphorylated AKT in SHR model, suggesting that LFG may active the PI3K-AKT signaling pathway to decrease hypertension. Mol. docking study further supported that p-hydroxybenzoic acid, cedar acid, shikimic acid, salicylic acid, nicotinic acid, linalool, and histidine can be well binding with NOS3, SRC, PI3K, and AKT. UPLC-QTOF/MS anal. confirmed that p-hydroxybenzoic acid, shikimic acid, salicylic acid, and nicotinic acid existed in LFG. Pre-treatment of HUVEC with nicotinic acid could alleviate the effect on cell viability induced by H2O2 and increase the NO level in cell supernatants. LFG can reduce the blood pressure in SHR model, which might be attributed to increasing the NO level in serum for promoting vasodilation via upregulating SRC expression level and activating the PI3K-AKT-NOS3 signaling pathway. Nicotinic acid might be the potential compound for LFG antihypertensive effect.

Chinese Medicine (London, United Kingdom) published new progress about Antihypertensives. 124-76-5 belongs to class alcohols-buliding-blocks, name is rel-(1R,2R,4R)-1,7,7-Trimethylbicyclo[2.2.1]heptan-2-ol, and the molecular formula is C10H18O, COA of Formula: C10H18O.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Barasa, Stephen S. published the artcileRepellent activities of stereoisomers of p-menthane-3,8-diols against Anopheles gambiae (Diptera: Culicidae), Application In Synthesis of 42822-86-6, the main research area is menthanediol stereoisomer insect repellent Anopheles.

Four stereoisomers of p-menthane-3,8-diol, which make up the natural product obtained from Eucalyptus citriodora, were synthesized through stereoselective procedures. Repellency assays showed that all the four were equally active against Anopheles gambiae s.s. Racemic blends and the diastereoisomeric mixture of all the four isomers were also equally repellent. 1-α-Terpineol, with a single hydroxyl function at C-8 and unsaturation at C-8, and menthol, with a single hydroxyl function at C-3, were not repellent. The practical implication of these results is discussed.

Journal of Medical Entomology published new progress about Anopheles gambiae. 42822-86-6 belongs to class alcohols-buliding-blocks, name is 2-(2-Hydroxypropan-2-yl)-5-methylcyclohexanol, and the molecular formula is C10H20O2, Application In Synthesis of 42822-86-6.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Ciera, Lucy published the artcileElectrospinning repellents in polyvinyl alcohol-nanofibers for obtaining mosquito-repelling fabrics, Name: 2-(2-Hydroxypropan-2-yl)-5-methylcyclohexanol, the main research area is polyvinyl alc nanofiber repellent electrospinning mosquito repelling fabric; mech property; electrospinning; emulsion; micro-capsules; mosquito; repellent.

Recently, the use of repellents for preventing the transmission of mosquito-borne diseases is getting increasingly more attention. However, most of the current repellents are volatile in nature and must be frequently re-applied as their efficacy is only limited to a short period of time. Therefore, a slow release and abrasion-resistant mechanism is needed for prolonging the protection time of the repellents. The focus of this study is on the direct micro-encapsulation of repellents from an emulsion and integration of already encapsulated repellents into nanofibres via electrospinning. Different repellents were electrospun in polyvinyl alc. (PVA) nanofibrous structures, namely p-menthane-3,8-diol micro-capsules, permethrin, chilli and catnip oil. The repellents were successfully incorporated in the nanofibres and the tensile properties of the resulting samples did not have a significant change. This means that the newly created textiles were identical to current PVA nanofibrous textiles with the added benefit of being mosquito repellent. Principally, all incorporated repellents in the nanofibrous structures showed a significantly reduced number of mosquito landings compared to the control. Consequently, the currently described method resulted in a new and very effective repelling textile material that can be used in the prevention against mosquito-associated diseases.

Royal Society Open Science published new progress about Anopheles gambiae. 42822-86-6 belongs to class alcohols-buliding-blocks, name is 2-(2-Hydroxypropan-2-yl)-5-methylcyclohexanol, and the molecular formula is C10H20O2, Name: 2-(2-Hydroxypropan-2-yl)-5-methylcyclohexanol.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Wangrawa, Dimitri W. published the artcileEssential oils and their binary combinations have synergistic and antagonistic insecticidal properties against Anopheles gambiae s. l. (Diptera: Culicidae), Category: alcohols-buliding-blocks, the main research area is Cymbopogon Lantana Lippia Anopheles essential oil biopesticide synergism.

Botanical biopesticides have potential for use in mosquito control because they exhibit low mammalian toxicity, are readily biodegraded, show target specificity and insecticidal activity. As populations of mosquito species grow more resistant to currently used organic insecticides, a need for new and effective insecticides for vector control becomes more urgent. This study reports the effects of synergistic and antagonistic essential oils (EOs) from Cymbopogon schoenanthus, Lantana camara, Lippia chevalieri and Lippia multiflora and their binary combinations against Anopheles gambiae s. l. larvae and adults. EOs insecticidal properties were tested with third to fourth-instar larvae and, non-blood-fed 3-5-day old field-collected An. gambiae using WHO and CDC bottle bioassays, resp. Many compounds were found in the EOs mixtures All EOs showed larvicidal and adulticidal activities with mortality from 0 to 100% against An. gambiae which were concentration dependent and EOs specific. EO mixture from C. schoenanthus and L. multiflora showed synergistic effect with LC50 of 38 ppm and EOs from L. chevalieri and C. schoenanthus showed antagonistic effect against larvae with LC50 of 100.84 ppm. On the other hand, EOs combinations showed additive effect on all adults. This study describes the potential of using EOs and their synergistic mixtures as potential insecticide(s) as a safer alternative to synthetic insecticides.

Biocatalysis and Agricultural Biotechnology published new progress about Anopheles gambiae. 124-76-5 belongs to class alcohols-buliding-blocks, name is rel-(1R,2R,4R)-1,7,7-Trimethylbicyclo[2.2.1]heptan-2-ol, and the molecular formula is C10H18O, Category: alcohols-buliding-blocks.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Hoang, Van-Hai published the artcileDiscovery of Conformationally Restricted Human Glutaminyl Cyclase Inhibitors as Potent Anti-Alzheimer’s Agents by Structure-Based Design, Formula: C4H11NO2, the main research area is Alzheimer’s disease glutaminyl cyclase SAR conformational analysis.

Alzheimer’s disease (AD) is an incurable, progressive neurodegenerative disease whose pathogenesis cannot be defined by one single element but consists of various factors; thus, there is a call for alternative approaches to tackle the multifaceted aspects of AD. Among the potential alternative targets, we aim to focus on glutaminyl cyclase (QC), which reduces the toxic pyroform of β-amyloid in the brains of AD patients. On the basis of a putative active conformation of the prototype inhibitor 1, a series of N-substituted thiourea, urea, and α-substituted amide derivatives were developed. The structure-activity relationship analyses indicated that conformationally restrained inhibitors demonstrated much improved QC inhibition in vitro compared to nonrestricted analogs, and several selected compounds demonstrated desirable therapeutic activity in an AD mouse model. The conformational anal. of a representative inhibitor indicated that the inhibitor appeared to maintain the Z-E conformation at the active site, as it is critical for its potent activity.

Journal of Medicinal Chemistry published new progress about Alzheimer disease. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Formula: C4H11NO2.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Li, Wenwen published the artcileHonokiol Restores Microglial Phagocytosis by Reversing Metabolic Reprogramming, Category: alcohols-buliding-blocks, the main research area is honokiol restores microglial phagocytosis metabolic reprogramming; Honokiol; metabolic reprogramming; microglial phagocytosis; mitochondria.

Dysfunction of microglia has been increasingly recognized as a causative factor in Alzheimerprimes disease (AD); thus, developing medicines capable of restoring microglial functions is critically important and constitutes a promising therapeutic strategy. Honokiol is a natural neuroprotective compound extracted from Magnolia officinalis, which may play roles in AD therapy. This study aimed to evaluate the role and the underlying mechanisms of honokiol in microglial phagocytosis. MTT and flow cytometry were used to assess the cell viability and apoptosis, resp. Phagocytic capacity, mitochondrial reactive oxygen species production, and membrane potential were evaluated using fluorescence microscopy. Seahorse XF24 extracellular flux analyzer was for cell glycolysis and oxidative phosphorylation detection. Mass spectrometry was applied for metabolites measurement. Quant. real-time polymerase chain reaction and western blotting were performed to detect the mRNA and protein level of PPARgamma and PGC1alpha, resp. Honokiol alleviated Abeta42-induced BV2 neurotoxicity. Honokiol promoted phagocytic efficiency of BV2 cells through reversing a metabolic switch from oxidative phosphorylation to anaerobic glycolysis and enhancing ATP production Meanwhile, honokiol reduced mitochondrial reactive oxygen species production and elevated mitochondrial membrane potential. Moreover, honokiol increased the expression of PPARgamma and PGC1alpha, which might play pos. roles in energy metabolism and microglial phagocytosis. In this study, honokiol was identified as an effect natural product capable of enhancing mitochondrial function thus promoting microglial phagocytic function.

Journal of Alzheimer’s Disease published new progress about Alzheimer disease. 97-67-6 belongs to class alcohols-buliding-blocks, name is (S)-2-hydroxysuccinic acid, and the molecular formula is C4H6O5, Category: alcohols-buliding-blocks.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Tosatti, Jessica Abdo Goncalves published the artcileEffects of Resveratrol Supplementation on the Cognitive Function of Patients with Alzheimer’s Disease: A Systematic Review of Randomized Controlled Trials, Related Products of alcohols-buliding-blocks, the main research area is review resveratrol neuroprotective agent Alzheimers disease.

Alzheimers disease (AD) comprises 60-70% of diagnosed dementia cases, and is characterized by the deposition of β-amyloid peptide and the formation of neurofibrillary tangles of tau protein. Resveratrol is a neuroprotective agent acting in the prevention of redox impairment in addition to exerting anti-apoptotic actions on brain cells. An ability to reduce neuronal damage in patients with AD has been suggested by preclin. studies. Objectives: The aim of this systematic review was to investigate the evidence in the published literature from studies that evaluated the effects of supplementation with resveratrol, alone or in a solution with glucose and malate (RGM), on the functional and cognitive performance of patients with AD, as assessed by validated instruments. A systematic literature search was performed in MEDLINE, CENTRAL, Embase, CINAHL, Web of Science, and Scopus databases including articles published up to August 2021. Randomized, placebo-controlled, clin. trials that reported cognitive and functional performance, as measured by the Alzheimer’s Disease Assessment Scale-Cognitive Subscale (ADAS-cog), Cooperative Study of Alzheimers Disease-Activities of Daily Living (ADCS-ADL), or the Mini Mental State Examination (MMSE), in AD patients treated with resveratrol, alone or as RGM, were included. After 1855 studies were identified, 24 RCTs underwent full-text review, with 20 studies excluded because they did not meet the inclusion criteria. Thus, four RCTs were included in the qual. analyses. The findings demonstrate that there are still few studies in humans, but they showed that this polyphenol acts in the delay of cognitive impairment in patients with AD, when administered alone or in combination with glucose and malate. Supplementation with resveratrol seems to influence the progressive cognitive and functional decline in AD patients, when compared with a placebo group.

Drugs & Aging published new progress about Alzheimer disease. 97-67-6 belongs to class alcohols-buliding-blocks, name is (S)-2-hydroxysuccinic acid, and the molecular formula is C4H6O5, Related Products of alcohols-buliding-blocks.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Cheng, Zhi-Qiang published the artcileMolecular-docking-guided design and synthesis of new IAA-tacrine hybrids as multifunctional AChE/BChE inhibitors, Product Details of C4H11NO2, the main research area is indoleacetic acid tacrine synthesis antiAlzheimer pharmacokinetics acetylcholinesterase butyrylcholinesterase; Alzheimer’s disease; Dual AChE/BChE inhibitor; IAA-tacrine hybrids; Molecular docking; Neural network electrical activity.

A series of new indole-3-acetic acid (IAA)-tacrine hybrids as dual acetylcholinesterase (AChE)/butyrylcholinesterase (BChE) inhibitors were designed and prepared based on the mol. docking mode of AChE with an IAA derivative (1a), a moderate AChE inhibitor identified by screening our compound library for anti-Alzheimer’s disease (AD) drug leads. The enzyme assay results revealed that some hybrids, e.g. 5d and 5e, displayed potent dual in vitro inhibitory activities against AChE/BChE with IC50 values in low nanomolar range. Mol. modeling studies in tandem with kinetic anal. suggest that these hybrids target both catalytic active site and peripheral anionic site of cholinesterase (ChE). Mol. dynamic simulations and Mol. Mechanics/Poisson-Boltzmann Surface Area (MM-PBSA) calculations indicate that 5e has more potent binding affinity than hit 1a, which may explain the stronger inhibitory effect of 5e on AChE. Furthermore, their predicted pharmacokinetic properties and in vitro influences on mouse brain neural network elec. activity were discussed. Taken together, compound 5e can be highlighted as a lead compound worthy of further optimization for designing new anti-AD drugs.

Bioorganic Chemistry published new progress about Alzheimer disease. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Product Details of C4H11NO2.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Uliassi, Elisa published the artcileA Focused Library of Psychotropic Analogues with Neuroprotective and Neuroregenerative Potential, Recommanded Product: 2,2-Dimethoxyethanamine, the main research area is phenothiazin synthesis psychotropic neuroprotectant blood brain barrier neurodegenerative disease; Neurodegenerative diseases; neural regeneration; neuroprotection; phenothiazines; phenotypic screening; psychotropic agents.

Overcoming the lack of effective treatments and the continuous clin. trial failures in neurodegenerative drug discovery might require a shift from the prevailing paradigm targeting pathogenesis to the one targeting simultaneously neuroprotection and neuroregeneration. In the studies reported herein, we sought to identify small mols. that might exert neuroprotective and neuroregenerative potential as tools against neurodegenerative diseases. In doing so, we started from the reported neuroprotective/neuroregenerative mechanisms of psychotropic drugs featuring a tricyclic alkylamine scaffold. Thus, we designed a focused-chem. library of 36 entries aimed at exploring the structural requirements for efficient neuroprotective/neuroregenerative cellular activity, without the manifestation of toxicity. To this aim, we developed a synthetic protocol, which overcame the limited applicability of previously reported procedures. Next, we evaluated the synthesized compounds through a phenotypic screening pipeline, based on primary neuronal systems. Phenothiazine 2Bc showed improved neuroregenerative and neuroprotective properties with respect to reference drug desipramine (2Aa). Importantly, we have also shown that 2Bc outperformed currently available drugs in cell models of Alzheimer’s and Parkinson’s diseases and attenuates microglial activation by reducing iNOS expression.

ACS Chemical Neuroscience published new progress about Alzheimer disease. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Recommanded Product: 2,2-Dimethoxyethanamine.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Gorecki, Lukas published the artcilePhenothiazine-Tacrine Heterodimers: Pursuing Multitarget Directed Approach in Alzheimer’s Disease, COA of Formula: C4H11NO2, the main research area is phenothiazine tacrine heterodimer preparation Alzheimer’s cholinesterase inhibitor; Alzheimer’s disease; acetylcholinesterase; butyrylcholinesterase; multitarget directed ligands; phenothiazine; tacrine.

Since 2002, no clin. candidate against Alzheimer’s disease has reached the market; hence, an effective therapy is urgently needed. We followed the so-called “”multitarget directed ligand”” approach and designed 36 novel tacrine-phenothiazine heterodimers which were in vitro evaluated for their anticholinesterase properties. The assessment of the structure-activity relationships of such derivatives highlighted compound 1dC as a potent and selective acetylcholinesterase inhibitor with IC50 = 8 nM and 1aA as a potent butyrylcholinesterase inhibitor with IC50 = 15 nM. Selected hybrids, namely, 1aC, 1bC, 1cC, 1dC, and 2dC, showed a significant inhibitory activity toward τ(306-336) peptide aggregation with percent inhibition ranging from 50.5 to 62.1%. Likewise, 1dC and 2dC exerted a remarkable ability to inhibit self-induced Aβ1-42 aggregation. Notwithstanding, in vitro studies displayed cytotoxicity toward HepG2 cells and cerebellar granule neurons; no pathophysiol. abnormality was observed when 1dC was administered to mice at 14 mg/kg (i.p.). 1dC was also able to permeate to the CNS as shown by in vitro and in vivo models. The maximum brain concentration was close to the IC50 value for acetylcholinesterase inhibition with a relatively slow elimination half-time. 1dC showed an acceptable safety and good pharmacokinetic properties and a multifunctional biol. profile.

ACS Chemical Neuroscience published new progress about Alzheimer disease. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, COA of Formula: C4H11NO2.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts