Ferlapioside: a new bromine substituted iridoid glycoside from the roots of Korovin.

One new bromine substituted iridoid glycoside, ferlapioside (), was isolated from the roots of Korovin, together with 10 known ones including seven iridoid glycosides (-) and three sesquiterpene lactones (-). Their structures were elucidated by extensive spectroscopic analyses, e.g.

Comparative metabolic profiling and quantitative analysis of metabolites in different tissues of Ajuga turkestanica by ESI-UHPLC-QqTOF-MS and NMR.

Ajuga turkestanica preparations are used as anti-aging cosmeceuticals and for medicinal purposes. Herein we describe the characterization and quantification of its metabolites in different organs using UHPLC-MS and NMR spectroscopy. A total of 51 compounds belonging to various phytochemical classes (11 flavonoids, 10 ecdysteroids, 9 diterpenes, 6 fatty acids, 5 iridoids, 3 phenylpropanoids, 3 sugars, 2 phenolics, 1 coumarin, 1 triterpene) were annotated and tentatively identified by UHPLC-ESI-QqTOF-MS/MS of methanolic extracts obtained separately from the organs.

New Tricyclic Aryl Quinazoline Derivatives by Suzuki-Miyaura Cross-Coupling.

A number of new deoxyvasicinone (2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-one) and mackinazolinone (6,7,8,9-tetrahydro-11H-pyrido[2,1-b]quinazolin-11-one) derivatives with aryl substituents at C7/C8 and at C5 are reported. These compounds are rare representatives of their kind and were prepared in high yields by Suzuki-Miyaura cross-coupling reactions between 7-bromo-2,3-dihydro[2,1-b]quinazoline-9-(1H)-one, 5,7-dibromo-2,3-dihydro[2,1-b]quinazoline-9-(1H)-one or 8-bromomackinazolinone and respective arylboronic acids with palladium acetate as the catalyst. The products were characterized spectroscopically and, in addition, by X-ray crystal structure analyses in six cases.

Quercetin and kaempferol from saffron petals alleviated hydrogen peroxide-induced oxidative damage in B16 cells.

Background: Saffron petals are usually considered as waste after saffron harvest. However, saffron petals contain many important phytochemical components (e.g.

Harnessing chickpea bacterial endophytes for improved plant health and fitness.

Endophytic bacteria live asymptomatically inside the tissues of host plants without inflicting any damage. Endophytes can confer several beneficial traits to plants, which can contribute to their growth, development, and overall health. They have been found to stimulate plant growth by enhancing nutrient uptake and availability.

Synthesis, crystal structure and Hirshfeld surface analysis of [1-(4-bromo-phen-yl)-1-1,2,3-triazol-4-yl]methyl 2-(4-nitro-phen-oxy)acetate.

The title compound, CHBrNO, was synthesized by a CuBr-catalysed Meldal-Sharpless reaction between 4-nitro-phen-oxy-acetic acid propargyl ether and -bromo-phenyl-azide, and characterized by X-ray structure determination and H NMR spectroscopy. The mol-ecules, with a near-perpendicular orientation of the bromo-phenyl-triazole and nitro-phen-oxy-acetate fragments, are connected into a three-dimensional network by inter-molecular C-H⋯O and C-H⋯N hydrogen bonds (confirmed by Hirshfeld surface analysis), π-π and Br-π inter-actions.

Experimental study of local anesthetic and antiarrhythmic activities of fluorinated ethynylpiperidine derivatives.

The chemical structure of piperidine has a unique ability to combine with other molecular fragments. This fact makes it possible to actively use it as an effective basis for the creation of new drug-like substances. Thus, the aim of the current investigation was to study the acute toxicity, local anesthetic potency, and antiarrhythmic activity of the two new synthesized piperidine derivatives under laboratory codes LAS-286 and LAS-294 (local anesthetic substances).

Synthesis of Substituted 1,2,4-Triazole-3-Thione Nucleosides Using Purine Nucleoside Phosphorylase.

1,2,4-Triazole derivatives have a wide range of biological activities. The most well-known drug that contains 1,2,4-triazole as part of its structure is the nucleoside analogue ribavirin, an antiviral drug. Finding new nucleosides based on 1,2,4-triazole is a topical task.

Therapeutic potential of boswellic acids: an update patent review (2016-2023).

Introduction: Boswellic acids (BAs) are a group of pentacyclic triterpenoids of the ursane and oleanane type. They have shown very interesting biological properties that have led to the development of a number of synthesis protocols. Both natural BAs and their synthetic derivatives may be useful in the treatment of a variety of cancers, viral infections and inflammatory diseases.

Phenolic constituents with potent α-glucosidase inhibitory and cytotoxic activities from Rumex nepalensis var. remotiflorus.

Quantitative analysis of Rumex nepalensis var. remotiflorus revealed that its roots contain rich anthraquinones, which has emodin, chrysophanol, and physcion contents of up to 0.30, 0.

Antimicrobial Action Mechanisms of Natural Compounds Isolated from Endophytic Microorganisms.

Infectious diseases are a significant challenge to global healthcare, especially in the face of increasing antibiotic resistance. This urgent issue requires the continuous exploration and development of new antimicrobial drugs. In this regard, the secondary metabolites derived from endophytic microorganisms stand out as promising sources for finding antimicrobials.

Chemical Composition of Artemisia Scoparia and Their Bioactivities.

Three undescribed sesquiterpenes (1-3), two enantiomeric pairs of monoterpenes (4a/4b-5a/5b), one alkyne (6), two known alkynes (7-8) and eight known coumarins (9-16) were isolated from the aerial parts extracts of Artemisia scoparia. The structures of these compounds were fully elucidated by their 1D and 2D NMR, HRESIMS spectral data analyses, and comparison with literature. The absolute configurations of compounds were determined by single-crystal X-ray crystallography (1), a comparison of experimental and calculated electronic circular dichroism (ECD) data (2-6).

Quantitative Structure-Permittivity Relationship Study of a Series of Polymers.

Dielectric constant is an important property which is widely utilized in many scientific fields and characterizes the degree of polarization of substances under the external electric field. In this work, a structure-property relationship of the dielectric constants (ε) for a diverse set of polymers was investigated. A transparent mechanistic model was developed with the application of a machine learning approach that combines genetic algorithm and multiple linear regression analysis, to obtain a mechanistically explainable and transparent model.

Bioactive Components and Biological Activities of L. Byproducts: A Comprehensive Review.

The production of saffron spice results in numerous byproducts, as only 15 g of spice can be produced from 1 kg of flowers, indicating that over 90% of the saffron flower material is eventually discarded as waste. In view of this, the paper reviews current knowledge on the natural active components in saffron byproducts and their biological activities, aiming to lay a theoretical and scientific foundation for the further utilization. Saffron byproducts contain a variety of phytochemical components, such as flavonoids, anthocyanins, carotenoids, phenolic acids, monoterpenoids, alkaloids, glycosides, and saponins.

Ruptured organosilica nanocapsules immobilized acetylcholinesterase coupled with MnO nanozyme for screening inhibitors from .

Abnormal expression of acetylcholinesterase (AChE) causes Alzheimer's disease (AD). Inhibiting AChE is a common strategy for reducing the degradation of neurotransmitter acetylcholine, in order to treat early-stage AD. Therefore, it is crucial to screen and explore AChE inhibitors which are safer and cause fewer side effects.

Bracteatinine and isogroenlandicine, two new isoquinoline alkaloids isolated from Corydalis bracteata and their effect on platelet function.

Two previously undescribed isoquinoline alkaloids, bracteatinine (1) and isogroenlandicine (2), together with four known alkaloids - coptisine (3), dehydrocorydaline (4), palmatine (5) and jatrorrhizine (6) were isolated from the aerial parts of Corydalis bracteata (Steph. Ex. Willd.

Four new phenolic constituents from the roots of Rumex dentatus L.

Four new phenolic compounds, including two naphthalenes, musizin-8-O-β-D-(6'-O-malonyl-3''-methoxy)glucopyranoside (1) and 2-acetyl-3-methyl-1,4-naphtho-quinone-8-O-β-D-glucopyranoside (2), one chromone, (2'R)-7-hydroxy-2-(2'-hydroxypropyl)-5-methyl acetate chromone (3), and one xanthone, 2,8-dimethyl-3,6-dihydroxyxanthone (4) were isolated from the roots of Rumex dentatus L. (Polygonaceae). In addition, five known including four naphthalenes (5-8) and one chromone (9) were also obtained.

Metal halide coordination compounds with quinazolin-4(3)-one.

Three coordination compounds of quinazolin-4(3)-one (; CHNO) with divalent group 12 halides are reported. In all complexes, coordination occurs the nitro-gen atom to the quinazolinone carbonyl group. In the two chain polymers with composition [ ()], .

Antimicrobial and Cytotoxic Activities of the Secondary Metabolites of Endophytic Fungi Isolated from the Medicinal Plant .

According to the World Health Organization, it is estimated that by 2050, drug-resistant infections could cause up to 10 million deaths annually. Therefore, finding a new generation of antibiotics is crucial. Natural compounds from endophytic fungi are considered a potential source of new-generation antibiotics.

Syntheses, crystal structures and Hirshfeld surface analysis of 2-(benzyl-sulfan-yl)-5-[4-(di-methyl-amino)-phen-yl]-1,3,4-oxa-diazole and 2-[(2-chloro-6-fluoro-benz-yl)sulfan-yl]-5-[4-(di-methyl-amino)-phen-yl]-1,3,4-oxa-diazole.

The title compounds were synthesized by alkyl-ation of 5-[(4-di-methyl-amino)-phen-yl]-1,3,4-oxa-diazole-2-thiol with benzyl chloride or 2-chloro-6-fluoro-benzyl chloride in the presence of potassium carbonate. The yields of 2-(benzyl-sulfan-yl)-5-[4-(di-methyl-amino)-phen-yl]-1,3,4-oxa-diazole, CHNOS (I), and 2-[(2-chloro-6-fluoro-benz-yl)sulfan-yl]-5-[4-(di-methyl-amino)-phen-yl]-1,3,4-oxa-diazole, CHClFNOS (II), were 96 and 92%, respectively. In the crystal structures of (I) and (II), C-H⋯π inter-actions are observed between neighboring mol-ecules.

Synthesis, Pharmacological Evaluation, and Molecular Modeling of Lappaconitine-1,5-Benzodiazepine Hybrids.

Diterpenoid alkaloids, originating from the amination of natural tetracyclic diterpenes, have long interested scientists due to their medicinal uses and infamous toxicity which has limited the clinical application of the native compound. Alkaloid lappaconitine extracted from various and species has displayed extensive bioactivities and active ongoing research to reduce its adverse effects. A convenient route to construct hybrid molecules containing diterpenoid alkaloid lappaconitine and 3-1,5-benzodiazepine fragments was proposed.

Syntheses, crystal structures and Hirshfeld surface analyses of -aryl-sulfonyl derivatives of cytisine.

By aryl-sulfonyl-ation of cytisine in the presence of tri-ethyl-amine, three new compounds have been obtained in good yields: (7,9)--[(4-ethyl-phen-yl)sulfon-yl]cytisine, CHNOS () {systematic name: (1,5)-3-[(4-ethyl-phen-yl)sulfon-yl]-1,2,3,4,5,6-hexa-hydro-8-1,5-methano-pyrido[1,2-][1,5]diazo-cin-8-one}, (7,9)--[(4-chloro-phen-yl)sulfon-yl]cytisine, CHClNOS () {systematic name: (1,5)-3-[(4-chloro-phen-yl)sulfon-yl]-1,2,3,4,5,6-hexa-hydro-8-1,5-methano-pyrido[1,2-][1,5]diazo-cin-8-one} and (7,9)--[(3-nitro-phen-yl)sulfon-yl]cytisine, CHNOS () {systematic name: (1,5)-3-[(3-nitro-phen-yl)sulfon-yl]-1,2,3,4,5,6-hexa-hydro-8-1,5-methano-pyrido[1,2-][1,5]diazo-cin-8-one}. The crystal structures of the compounds were determined on the basis of single-crystal X-ray diffraction data. The crystal structures of ()-() are distinguished by the arrangement of two fragments of the mol-ecule around the sulfonyl site.