Результаты поиска

BA inhibits LPS-stimulated inflammatory response and apoptosis in human middle ear epithelial cells by regulating the Nf-Kb/Iκbα axis.

Otitis media (OM) is a prevalent childhood ear disease characterized by inflammation of the middle ear cavity, which can lead to ear pain, fever, and hearing loss. The pathogenesis of OM is multifaceted, encompassing a variety of factors including bacterial or viral infections, host immune responses, and the function of middle ear epithelial cells. Boswellic acid (BA), a natural triterpene compound extracted from frankincense resin, has been proven to possess significant anti-inflammatory and immunomodulatory effects. This study aims to investigate the effects of BA on lipopolysaccharide (LPS)

Triterpenoids of Ganoderma lucidum inhibited S180 sarcoma and H22 hepatoma in mice by regulating gut microbiota.

In order to explore effect of natural plant extracts on anti-tumor and prevent tumor development. The study assessed the antitumor effect of triterpenoids of Ganoderma lucidum (TGL) on S180 and H22 tumor bearing mice. A triterpene compound, 2α, 3α, 23-trihydroxy-urs-12-en-28-oic acid, was successfully isolated and purified from G. lucidum. S180 and H22 cells were subcutaneously inoculated in the left axilla of mice to establish a transplantable tumor model. After, the mice were orally treated with TGL and evaluated by tumor inhibition rate, organ index, and the serum index. The Bax and Bcl-2 p

Genus Sophora: a comprehensive review on secondary chemical metabolites and their biological aspects from past achievements to future perspectives.

Sophora is deemed as one of the most remarkable genera of Fabaceae, and the third largest family of flowering plants. The genus Sophora comprises approximately 52 species, 19 varieties, and 7 forms that are widely distributed in Asia and mildly in Africa. Sophora species are recognized to be substantial sources of broad spectrum biopertinent secondary metabolites namely flavonoids, isoflavonoids, chalcones, chromones, pterocarpans, coumarins, benzofuran derivatives, sterols, saponins (mainly triterpene glycosides), oligostilbenes, and mainly alkaloids. Meanwhile, extracts and isolated compoun

Совпадение в полном тексте источника
… As tabulated in Tables 7 , 8 , 9 , 10 , 11 and 12 , stilbenes, oligomers, sterols, triterpenes, coumarins, alkaloids, phenolic acids, and other phenolated compounds were identified from different Sophora species. … Stigmasterol 3- O -glucoside | S. alopecuroides S. pachycarpa | | Wang et al. ( 2020b ) 221 | Campesterol | S. secundiflora S. tomentosa | | Aly et al. ( 2020a ) 222 | Lup-20(29)-ene-3, 28- diol (Betulin) | S. mollis S. tomentosa S. secundiflora | | Aly et al. ( 2020a ), Quradha et al. ( 2021 ) Table 10 Triterpenes …

Chemical profiling of Fufang-Xialian-Capsule by UHPLC-Q-TOF-MS and its antioxidant activity evaluated by in vitro method.

Fufang Xialian (FXL) capsule, a traditional Chinese medicine (TCM) formula, has been used for a long time to treat Chronic Atrophic Gastritis, but the pharmacodynamic material basis and mechanism of action are unclear. In this research, ferric-reducing antioxidant power (FRAP) method and DPPH scavenging method were utilized to evaluate the antioxidant activity of FXL in vitro. An ultra high-performance liquid chromatography coupled with Linear Ion Trap Mass Spectrometer (UHPLC-IT-MS) method and an ultra high-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrom

Oleanolic acid derivatives for pharmaceutical use: a patent review.

INTRODUCTION: Oleanolic acid belongs to the pentacyclic triterpene family. In China, oleanolic acid has been used as an over the counter (OTC) hepatoprotective drug for decades. Oleanolic acid and its derivatives present a wide variety of biological activities, supporting their pharmaceutical uses for multiple diseases. AREAS COVERED: Representative patent publications (1971-2015) covering the preparation, pharmaceutical compositions, and medical uses of oleanolic acid and its derivatives are analyzed, with focus on their anticancer, anti-osteoporosis, anti-obesity, anti-diabetic, lipid-lower

Mycochemical Investigation of the Turkey Tail Medicinal Mushroom Trametes versicolor (Higher Basidiomycetes): A Potential Application of the Isolated Compounds in Documented Pharmacological Studies.

The purpose of this study was to elucidate the chemical properties of the n-hexane, chloroform, and ethyl acetate extracts of the fruiting body of the medicinal mushroom Trametes versicolor. The study led to the isolation of 5 sterols, 2 triterpene derivatives, 1 hydroquinone-derived aromatic compound, and, finally, 1 cerebroside and 1 triglyceride derivative. These compounds were identified for first time in T. versicolor and were named as follows: 4-isobutoxyphenyl palmitate (5), N-D-2'-hydroxyheptanoic-1-O-β-D-glucopyranosyl-9-methyl-4,8-sphinga-dienine(cerebroside) (6), 3β-linoleyloxyergos

Conjugates of natural compounds with nitroxyl radicals as a basis for creation of pharmacological agents of new generation.

Synthesis and research of pharmacological properties of polyfunctional "hybrid" compounds containing fragments of nitroxyl radicals (NR) in a molecule (spin-labeled conjugates) is a rapidly developing area of medicinal chemistry. Many examples of various classes of natural compounds have shown that the introduction of nitroxyl fragment into a molecule leads to either strengthening of biological activity or its modification, decrease of general toxicity, or increase of selective cytotoxicity. The review of the published data on spin-labeled biologically active natural compounds has revealed tha

Antithrombotic effect of chikusetsusaponin IVa isolated from Ilex paraguariensis (Maté).

The triterpene chikusetsusaponin IVa was isolated from the fruit of Ilex paraguariensis. Using biochemical and pharmacological methods, we demonstrated that chikusetsusaponin IVa (1) prolongs the recalcification time, prothrombin time, activated partial thromboplastin time, and thrombin time of normal human plasma in a dose-dependent manner, (2) inhibits the amidolytic activity of thrombin and factor Xa upon synthetic substrates S2238 and S2222, (3) inhibits thrombin-induced fibrinogen clotting (50% inhibition concentration, 199.4 ± 9.1 μM), and (4) inhibits thrombin- and collagen-induced plat

Pistagremic acid from Pistacia integerrima as a natural multi-target candidate tackling crucial enzymes involved in Alzheimer's disease.

Natural products have crucial relevance both in traditional medicine as well as in modern drug discovery. Indeed, they inspire currently developed drugs, emphasizing the importance of biodiversity and sustainability. Alzheimer's disease (AD), a complex neurodegenerative disorder marked by amyloid plaques and neurofibrillary tangles, involves dysregulation of molecular pathways including increased cholinesterases and monoamine oxidase-B (MAO-B) activities, with enzyme inhibition remaining a key therapeutic strategy. This study investigates pistagremic acid, a triterpene from Pistacia chinensis

Nitric oxide initiates oxidative independent apoptosis-like death in Candida albicans by lupeol.

Lupeol, a dietary triterpene-type phytochemical flavonoid, was investigated for its mode of action in Candida albicans by assessing reactive species generation. While increased intracellular nitric oxide (NO) levels were detected, negligible levels were observed for other reactive oxygen species (ROS) and peroxynitrite(ONOO-). The major NO scavenger l-NAME was applied in further experiments to determine whether NO was responsible for the observed processes. DNA damage, including fragmentation and condensation, occurred when the NO concentration increased. Additionally, G1 to S phase cell cycle

A new triterpenoid pentaglycoside from Olax imbricata: isolation and in vitro, in silico studies on α-glucosidase.

Extensive fractionation of methanol extract from the dried powdered roots of Olax imbricata (Olacaceae) led to the isolation of a new oleanane-skeleton triterpene pentaglycoside, olaximpentaose (1). The chemical structure was elucidated using 1D and 2D NMR and HR-ESI-MS data analysis. The sugar subunits of olaximpentaose (1) were determined by acidic hydrolysis and 1H NMR chemical shifts, coupling constants, and integral ratios of the anomeric signals. Compound 1 exhibited the higher inhibition against α-glucosidase, with the IC50 = 97.19 ± 12.29 µM when compared with acarbose (IC50 = 126.62 ±

Identification of α-tubulin alpha-1B chain as a target of asiatic acid using chemical proteomics in HepG2 hepatoma cells.

Asiatic acid (AA) is a naturally occurring pentacyclic triterpene isolated from Centella asiatica and has various biological effects, most notably anticancer effects. While numerous investigations have demonstrated the possible mechanism underlying AA's anticancer action, the precise protein target of AA remains unclear. In this study, the protein target of AA in HepG2 hepatoma cells was identified using the AfBPP-based chemoproteomic approach. Initially, a diazirine and alkyne group modified AA photoaffinity probe was synthesized. Then, using mass spectrometry analysis, 13 putative target pro

GC-MS Analysis of Bioactive Compounds of Flower Extracts of Calycopteris floribunda Lam.: A Multi Potent Medicinal Plant.

Calycopteris floribunda Lam. is a potent medicinal woody climber that belongs to Combretaceae. This plant is usually found in dry deciduous tropical forests and is used in various medicinal practices like Ayurveda, Unani and Sidda. Whole plant and its different parts like leaves, flowers and stem are used in the treatment of diarrhoea, dysentery, jaundice and malaria. It is also have anthelminthic, anti-inflammatory, antifungal, hepatoprotective and anticancerous activities. Knowing its medicinal properties, the present study is undertaken to investigate the preliminary phytochemical constitue

Design, Synthesis and In Vitro Investigation of Novel Basic Celastrol Carboxamides as Bio-Inspired Leishmanicidal Agents Endowed with Inhibitory Activity against Leishmania Hsp90.

The natural triterpene celastrol (CE) is here used as lead compound for the design and synthesis of a panel of eleven CE carboxamides that were tested in vitro for their growth inhibitory activity against Leishmania infantum and L.tropica parasites. Among them, in vitro screening identified four basic CE carboxamides endowed with nanomolar leishmanicidal activity, against both the promastigotes and the intramacrophage Leishmania amastigotes forms. These compounds also showed low toxicity toward two human (HMEC-1 and THP-1) and one murine (BMDM) cell lines. Interestingly, the most selective CE

Synthesis and Antimicrobial Activity of Ursolic Acid Ester Derivatives.

Infections caused by microorganisms are a major cause of morbidity and mortality worldwide, and natural products continue to be important sources for the discovery of new antimicrobial agents. Ursolic acid is a triterpene with known antibacterial action, being naturally found in plants, such as Jaracanda oxyphylla and Jacaranda caroba (Bignoniaceae). Ursolic acid derivative esters have revealed potential biological activities, such as antitumor, antiviral, and antibacterial activity. In this study, sixteen esters (1-16) were synthesized from ursolic acid using DIC/DMAP and characterized by inf

Assessment of the Antiangiogenic and Anti-Inflammatory Properties of a Maslinic Acid Derivative and its Potentiation using Zinc Chloride.

Maslinic acid is a pentacyclic triterpene with a plethora of biological activities, including anti-inflammatory, antioxidant, antimicrobial, cardioprotective, and antitumor effects. New derivatives with improved properties and broad-spectrum activity can be obtained following structural changes of the compound. The present study was aimed to characterize a benzylamide derivative of maslinic acid-benzyl (2α, 3β) 2,3-diacetoxy-olean-12-en-28-amide (EM2)-with respect to the anti-angiogenic and anti-inflammatory effects in two in vivo experimental models. Consequently, the compound showed good tol

Ursolic Acid Causes Cell Death in PC-12 Cells by Inducing Apoptosis and Impairing Autophagy.

Ursolic acid (UA) is a natural pentacyclic triterpene that has various biological activities, including anticancer and anti-inflammatory effects. This study investigated the ability of UA to cause cell death in pheochromocytoma (PC-12) cells. UA was cytotoxic to PC-12 cells (half-maximum inhibitory concentration=53.2 μM) and significantly reduced the clonogenic ability of PC-12 cells. It also triggered apoptosis by reducing the level of B-cell lymphoma 2 (BCL2), activating caspase-3, and inducing cleavage of poly (ADP-ribosyl) polymerase. To investigate the effects of UA treatment on the induc

Cucurbitane triterpenoids from the fruit of Momordica charantia L. and their anti-hepatic fibrosis and anti-hepatoma activities.

Momordica charantia L. (Cucurbitaceae) is a popular vegetable and traditional folk medicine, that has been used for hundreds of years. In this study, three undescribed cucurbitane-type triterpene glycosides furpyronecucurbitane A, goyaglycoside I and charantagenin F along with nine known compounds were isolated from the immature fruit of Momordica charantia L. Their structures were identified on the basis of extensive 1D, 2D NMR and HRESIMS spectroscopy analysis. All isolated compounds were examined for their anti-hepatic fibrosis activity against murine hepatic stellate cells (t-HSC/Cl-6) and

Lupeol Isolated from Sorbus commixta Suppresses 1α,25-(OH)2D3-Mediated Osteoclast Differentiation and Bone Loss in Vitro and in Vivo.

Lupeol is a lupane-type triterpene isolated from Sorbus commixta, an oriental medicine used to treat arthritis and inflammatory diseases. However, the antiosteoporotic effects of S. commixta or any of its constituents have not been studied yet. In the present study, we have examined the effect of lupeol (a major active triterpenoid isolated from S. commixta) on osteoclastogenesis and sought to elucidate its underlying molecular mechanisms. We evaluated whether lupeol antagonized osteoclast differentiation and bone resorption. Lupeol markedly inhibited osteoclast differentiation and bone resorp

Structures of new triterpenoids and cytotoxicity activities of the isolated major compounds from the fruit of Momordica charantia L.

Two new cucurbitane-type triterpene glycosides, charantagenins D (1) and E (2), and one new sterol, 7-oxo-stigmasta-5,25-diene-3-O-β-d-glucopyranoside (3), were isolated from the fruit of Momordica charantia L. together with another eight known compounds. Their structures were determined on the basis of spectral analysis. Cytotoxicity activities of the isolated major compounds were evaluated against lung cancer cell line A549, glioblastoma cell line U87, and hepatoma carcinoma cell line Hep3B by using a 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) in vitro assay. Results