Polyphenolic Compounds Activate SERCA1a and Attenuate Methylglyoxal- and Palmitate-Induced Impairment in Pancreatic INS-1E Beta Cells.

Sarco/endoplasmic reticulum Ca-ATPase (SERCA) is an important regulatory protein responsible for maintaining calcium homeostasis within cells. Impairment of SERCA associated with activity/expression decrease has been implicated in multiple chronic conditions, including cardiovascular diseases, diabetes, cancer, neurodegenerative diseases, and skeletal muscle pathologies. Natural polyphenols have been recognized to interact with several target proteins involving SERCA.

Correction: Agbadua et al. Oxidized Resveratrol Metabolites as Potent Antioxidants and Xanthine Oxidase Inhibitors. 2022, , 1832.

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Semisynthetic Ecdysteroid Cinnamate Esters and -Butyl Oxime Ether Derivatives with Trypanocidal Activity.

The parasite is the causative agent of Chagas disease, a neglected tropical disease that affects the lives of millions of indigenous people in Latin America. As medications to treat Chagas disease are limited to the application of benznidazole and nifurtimox, which are not ideal treatments for the chronic stage of the disease, the search for new antichagasic drug candidates is an important need. Ecdysone has previously been shown to interfere with the life cycle of .

Euphane and Tirucallane Triterpenes with Trypanocidal Activity from .

The phytochemical investigation of resulted in the isolation of 15 previously undescribed triterpenoids (desmondiins A, C-P) and 8 already described compounds. The structures of the isolated compounds were determined by extensive spectroscopic analyses. The compounds were identified as tirucallane and euphane triterpenes based on 7-keto-8-ene, 11-keto-8-ene, or 7,11-diketo-8-ene skeletons.

The significance of CD49f expression in pediatric B-cell acute lymphoblastic leukemia.

Objectives: CD49f is an adhesion molecule present on malignant lymphoblasts in B-cell acute lymphoblastic leukemia; it is associated with a poor prognosis. CD49f expression has been proposed as a marker for measurable residual disease (MRD) marker, but this marker has yet to be implemented in clinical practice.

Methods: In this study, we used flow cytometry to detect CD49f expression by leukemic blasts in paired bone marrow and cerebrospinal fluid samples at diagnosis and bone marrow at day 15 of treatment.

Phytochemical Investigation of Schreb. and ACE-Inhibitory Activity of Oligomer Stilbenes of the Plant.

Phenolic compounds are the main special metabolites of Cyperaceae species from phytochemical, pharmacological, and chemotaxonomical points of view. The present study focused on the isolation, structure determination, and pharmacological investigation of constituents from . Twenty-six compounds, including lignans, stilbenes, flavonoids, megastigmanes, chromenes, and phenylpropanoids, were identified from the methanol extract of the plant.

Preparation of Dearomatized p-Coumaric Acid Derivatives as DNA Damage Response Inhibitors with Potent In Vitro Antitumor Effect.

Our research group previously identified graviquinone (1) as a promising antitumor metabolite that is formed in situ when the antioxidant methyl caffeate scavenges free radicals. Furthermore, it exerted a DNA damaging effect on cancer cells and a DNA protective effect on normal keratinocytes. To expand and explore chemical space around qraviquinone, in the current work we synthesized 9 new alkyl-substituted derivatives and tested their in vitro antitumor potential.

Diterpenes Isolated from Three Different Species and Their Antiproliferative Activities against Gynecological and Glioblastoma Cancer Cells.

Fourteen diterpenes were isolated from methanol extracts of the aerial parts of, "Marginatus", and . The compounds belong to the abietane (-, -, and ), -clerodane (-), and -kaurane (, ) classes. Three new compounds were isolated from , including 3--acetylornatin G (), 3,12-di--acetylornatin G (), ornatin B methyl ester (), and ornatin F (), for which we proposed a revised structure.

17-Oxime ethers of oxidized ecdysteroid derivatives modulate oxidative stress in human brain endothelial cells and dose-dependently might protect or damage the blood-brain barrier.

20-Hydroxyecdysone and several of its oxidized derivatives exert cytoprotective effect in mammals including humans. Inspired by this bioactivity of ecdysteroids, in the current study it was our aim to prepare a set of sidechain-modified derivatives and to evaluate their potential to protect the blood-brain barrier (BBB) from oxidative stress. Six novel ecdysteroids, including an oxime and five oxime ethers, were obtained through regioselective synthesis from a sidechain-cleaved calonysterone derivative 2 and fully characterized by comprehensive NMR techniques revealing their complete 1H and 13C signal assignments.

Thymoquinone-protoflavone hybrid molecules as potential antitumor agents.

We describe herein the synthesis of eight new ester-coupled hybrid compounds from thymoquinone and protoflavone building blocks, and their bioactivity testing against multiple cancer cell lines. Among the hybrids, compound 14 showed promising activities in all cell lines studied. The highest activities were recorded against breast cancer cell lines with higher selectivity to MDA-MB-231 as compared to MCF-7.

Hybrid molecules of protoflavones and spirooxindole derivatives with selective cytotoxicity against triple-negative breast cancer cells.

The combination of compounds with complementary bioactivities into hybrid molecules is an emerging concept in drug discovery. In this study, we aimed to synthesize new hybrid compounds based on p53-MDM2/X protein-protein interaction spiropyrazoline oxindole-based inhibitors and ataxia telangiectasia and Rad3-related (ATR) protoflavone-based inhibitors through copper(i) catalysed azide-alkyne cycloaddition. Five new hybrids were prepared along with three representative reference fragments.

Five times over: 42 new species highlight Southeast Asia's rich biodiversity (Gastropoda, Stylommatophora, Hypselostomatidae).

The Southeast Asian genus , currently comprising 13 nominal species, encompasses the world's tiniest land snails. This work shows that there are far more species than previously suspected, and that this genus is in fact, a very speciose group of tiny snails widely distributed in Southeast Asia. is revised based on type material of known species as well as 211 samples newly collected in China, Laos, Myanmar, Thailand and Vietnam.

Preparation and Evaluation of 6-Gingerol Derivatives as Novel Antioxidants and Antiplatelet Agents.

Ginger () is widely used as a spice and a traditional medicine. Many bioactivities have been reported for its extracts and the isolated compounds, including cardiovascular protective effects. Different pathways were suggested to contribute to these effects, like the inhibition of platelet aggregation.

Highly Oxidized Ecdysteroids from a Commercial Root Extract as Potent Blood-Brain Barrier Protective Agents.

Ecdysteroid-containing herbal extracts, commonly prepared from the roots of , are marketed worldwide as a "green" anabolic food supplement. Herein are reported the isolation and complete H and C NMR signal assignments of three new minor ecdysteroids (compounds -) from this extract. Compound was identified as a possible artifact that gradually forms through the autoxidation of calonysterone.

Scavengome of an antioxidant.

The term "scavengome" refers to the chemical space of all the metabolites that may be formed from an antioxidant upon scavenging reactive oxygen or nitrogen species (ROS/RNS). This chemical space covers a wide variety of free radical metabolites with drug discovery potential. It is very rich in structures representing an increased chemical complexity as compared to the parent antioxidant: a wide range of unusual heterocyclic structures, new CC bonds, etc.

Synthesis and In Vitro Anticancer Evaluation of Flavone-1,2,3-Triazole Hybrids.

Hybrid compounds of flavones, namely chrysin and kaempferol, and substituted 1,2,3-triazole derivatives, were synthesized by click reaction of the intermediate -propargyl derivatives. 4-Fluoro- and 4-nitrobenzyl-1,2,3-triazole-containing hybrid molecules were prepared. The mono- and bis-coupled hybrids were investigated on 60 cell lines of 9 common cancer types (NCI60) in vitro as antitumor agents.

Oxidized Resveratrol Metabolites as Potent Antioxidants and Xanthine Oxidase Inhibitors.

Resveratrol is a well-known natural polyphenol with a plethora of pharmacological activities. As a potent antioxidant, resveratrol is highly oxidizable and readily reacts with reactive oxygen species (ROS). Such a reaction not only leads to a decrease in ROS levels in a biological environment but may also generate a wide range of metabolites with altered bioactivities.

Composition decipherment of Ficus pumila var. awkeotsang and its potential on COVID-19 symptom amelioration and in silico prediction of SARS-CoV-2 interference.

The jelly from achenes of Ficus pumila var. awkeotsang (FPAA) is a famous beverage ingredient in Taiwan. In this work, ficumarin (1), a new compound was obtained from its twigs (FPAT) and elucidated with comprehensive spectroscopic data.

Medicinal chemistry inspired by ginger: exploring the chemical space around 6-gingerol.

Ginger ( Roscoe) has been used as a spice and as a traditional remedy since ancient times, especially in traditional Chinese medicine. It has been applied as a treatment for many diseases either alone or in combination with other remedies. Many studies were conducted on ginger and its constituents and a wide array of bioactivities were reported, , antioxidant, anti-inflammatory, antiemetic, and anticancer activity.

C--Abietane and Three Abietane Diterpenoids from Leaves as P-Glycoprotein Modulators.

In this study, a bioguided fractionation of extract was performed by chromatographic methods. It yielded one new -abietane diterpene, mutabilol (), and three known abietanes, coleon-U-quinone (), 8α,9α-epoxycoleon-U-quinone (), and coleon U (). The abietane diterpenoid was also tentatively identified using HPLC-MS/MS.

Diversity-Oriented Synthesis Catalyzed by Diethylaminosulfur-Trifluoride-Preparation of New Antitumor Ecdysteroid Derivatives.

Fluorine represents a privileged building block in pharmaceutical chemistry. Diethylaminosulfur-trifluoride (DAST) is a reagent commonly used for replacement of alcoholic hydroxyl groups with fluorine and is also known to catalyze water elimination and cyclic Beckmann-rearrangement type reactions. In this work we aimed to use DAST for diversity-oriented semisynthetic transformation of natural products bearing multiple hydroxyl groups to prepare new bioactive compounds.

A review of the genus Möllendorff, 1899 (Gastropoda, Pulmonata, Camaenidae).

In this paper an overview of the species is provided, and the intraspecific variability of several species demonstrated on multiple shells. Páll-Gergely, and Páll-Gergely, are described based on specimens found in museum collections. Five new synonyms are recognized: Möllendorff, 1899 is a new synonym of Möllendorff, 1899, Möllendorff, 1899 is a new synonym of (H.

Microwave-assisted Phospha-Michael addition reactions in the 13α-oestrone series and antiproliferative properties.

Microwave-assisted phospha-Michael addition reactions were carried out in the 13α-oestrone series. The exocyclic 16-methylene-17-ketones as α,β-unsaturated ketones were reacted with secondary phosphine oxides as nucleophilic partners. The addition reactions furnished the two tertiary phosphine oxide diastereomers in high yields.