1,721,063 research outputs found
Oleanane derivatives for pharmaceutical use: a patent review (2000-2016)
No full textIntroduction: Oleanolic acid has been considered a good start molecule for synthetic exploitation. Thus hundreds of oleanane triterpenoids have been synthesized and patented. Also many oleanane saponins have been patented for their biological activities and possible pharmaceutical use. Areas covered: Patents reporting the biological activities of oleanane derivatives and saponins with oleanane-type aglycones were examined. Among the synthesized oleanane derivatives, the most promising seem to be 2-cyano-3,12-dioxoolean-1,9(11)-dien-28-oic acid derivatives which interfere with many pathways involved in inflammation, oxidative stress and cell proliferation. Regarding oleanane-type saponins, several patents claiming their antiproliferative activity or their possible use as adjuvants in vaccines, were reported. Expert opinion: Despite the great number of synthesized oleanane triterpenoids, only CDDO-Me entered clinical development as a possible drug for the treatment of chronic kidney disease (CKD) but a phase 3 clinical trial was terminated due to heart-related adverse effects. Further phase 2 clinical trials of CDDO-Me are in progress for the treatment of CKD and PAH (pulmonary arterial hypertension) patients without heart-related risk factors. Additional investigations leading to compounds with an improved activity/toxicity profile along with well-designed preclinical and clinical trials are needed. Regarding oleanane-type saponins, the real perspective seems to be as adjuvants in vaccines
Ruscus Genus: A Rich Source of Bioactive Steroidal Saponins
No full textThe genus Ruscus (Asparagaceae family) is native to the Mediterranean, Southern and Western Europe and is represented by perennial, rhizomatous, and evergreen shrubs. Among the approximately seven species spread throughout Europe up to Iran, Ruscus aculeatus L. (butcherʼs broom) is the most widely distributed and appreciated. This review provides an overview of the traditional use of Ruscus spp., the current knowledge of the chemistry of this genus, and the pharmacological studies carried out on Ruscus spp. extracts. The underground parts of Ruscus plants are a source of steroidal saponins that can be classified into two structural classes: the hexacyclic spirostanol saponins and the pentacyclic furostanol saponins. The main aglycones are ruscogenin and neoruscogenin. From the pharmacological point of view, the most studied Ruscus species is undoubtedly R. aculeatus, a very ancient phlebotherapeutic agent. Pharmacological investigations since the discovery of the vasoconstrictive and venotonic properties of ruscogenin and neoruscogenin in the underground parts of R. aculeatus are discussed. Preparations based on Ruscus species are currently used for the treatment of chronic venous insufficiency, varicose veins, haemorrhoids, and orthostatic hypotension. Finally, analytical techniques for the quality control of R. aculeatus extracts are reported
Fig. 1 in Scabiosa atropurpurea: A rich source of iridoids with α-glucosidase inhibitory activity evaluated by in vitro and in silico studies
No full textFig. 1. LC-MS profile (Base Peak chromatogram) in negative ion mode of Scabiosa atropurpurea methanol extract.Published as part of Kılınc, Hilal, Masullo, Milena, Lauro, Gianluigi, D'Urso, Gilda, Alankus, Ozgen, Bifulco, Giuseppe & Piacente, Sonia, 2023, Scabiosa atropurpurea: A rich source of iridoids with α-glucosidase inhibitory activity evaluated by in vitro and in silico studies, pp. 113471 in Phytochemistry (113471) 205 on page 2, DOI: 10.1016/j.phytochem.2022.113471, http://zenodo.org/record/816061
Garcinia mangostana L. fruits and derived food supplements: Identification and quantitative determination of bioactive xanthones by NMR analysis
No full textMangosteen (Garcinia mangostana L.), known as "the queen of fruits", is one of the most praised tropical fruit due to its delicious taste. In the last years, the use of mangosteen in functional products has been increasing, mainly in food beverages and nutraceutical formulations due to its biological activities related to the content of xanthones. The quantitative Nuclear Magnetic Resonance (qNMR) analysis, a rapid and accurate method used for simultaneous quantification of plant metabolites, was here employed to determine the amount of bioactive xanthones in the extracts of G. mangostana arils and shells obtained by using solvent of increasing polarity along with ''eco-friendly'' solvents like ethanol and ethanol-water. Furthermore, the content of xanthones was compared with that occurring in four selected commercial food supplements, among which tablets and capsules, and two fruit juices, based on mangosteen. Quantitative results highlighted a significant variability: the extracts of the shells displayed a higher amount of bioactive xanthones than those of the arils, in particular, of gamma-mangostin and alpha-mangostin, while beta-mangostin, demethylcalabaxanthone, mangostanin, 8-deoxygartanin occurred in higher amounts in arils. A certain variability in the amount of biologically active xanthones (i.e. alpha-mangostin and gamma-mangostin) could be observed in commercial food supplements
Iridoids, monoterpenoid glucoindole alkaloids and flavonoids from Vinca major
No full textA new secoiridoid glucoside,vinmajoroside (1),was isolated from the leaves of Vinca major L. along with 11 known compounds belonging to the secoiridoid ((7α)-7-. O-methylmorroniside,2),iridoid (loganin,loganic acid and 7-. O-. p-coumaroylloganin),monoterpenoid glucoindole alkaloid (5 (S)-5-carboxyvincoside and strictosamide),flavonoid (rutin,kaempferol 3-O-rutinoside and robinin),lignan (syringaresinol 4-. O-β-glucopyranoside) and phenolic acid (chlorogenic acid) groups. The structure elucidation of the isolates was accomplished by extensive 1D and 2D-NMR experiments as well as ESI-MS. Secoiridoids and lignan were encountered for the first time in the genus Vinca
Medicinal plants in the treatment of women's disorders: Analytical strategies to assure quality, safety and efficacy
No full textDuring last decades an increasing number of herbal products specifically targeting women's disorders has appeared in the worldwide marketplace. This growth highlights the need for a critical evaluation of quality, safety and efficacy of these products. Analytical techniques applied to the quality control of the main medicinal plants used for women health (relief of menopause and menstrual related symptoms) have been reviewed. Thanks to the innovation in analytical technology, identification and detection of secondary metabolites dramatically improved. In particular, hyphenated techniques have proved to be the most suitable for the rapid identification of compounds in plant matrix. Moreover, taking into account that differences in sample quality are not only found in the main compounds or in the chemical markers but also in the low-concentration compounds, fingerprint analysis might be a simple way for identification and quality control of herbal products containing a large number of low amounts of unknown compounds. Furthermore in several papers the informations obtained from the analysis of a plant have been processed by statistical elaborations. Medicinal plants here discussed are classified on the basis of the chemical markers used for their quality control
Comfreyns, arylnaphthalene lignans that inhibit pro-inflammatory gene expression, and pharmaceutic composition comprising them
No full textEffects of garcinol and guttiferone K isolated from Garcinia cambogia on oxidative/nitrative modifications in blood platelets and plasma
No full textIn depth LC-ESIMS n -guided phytochemical analysis of Ziziphus jujuba Mill. leaves
No full textZiziphus jujuba Mill. leaves are receiving a great attention for their ability to improve sleep, exerting beneficial effects for both the heart and the central nervous system. With the aim to obtain a comprehensive analysis of the specialised metabolites occurring in the leaves of Z. jujuba, a LC-ESI/(HR)Orbitrap/MS profile in negative ion mode of the methanol extract was carried out. The LC-MS profile guided the isolation of 42 compounds, of which the structures were elucidated by 1D and 2D-NMR experiments. Based on this approach, 2 previously unreported dammarane-type saponins have been characterized along with flavonoid derivatives, dammarane-type saponins and triterpenic acids. Dammarane-type saponins were tested for their cytotoxic activity against A549 and HeLa cancer cell lines. None of the tested compounds, in a range of concentrations between 12.5 and 100 μM, caused a significant reduction of the cell number. This work provides a deep insight on the chemistry of the leaves of Z. jujuba and could be useful for further biological studies aimed at identifying phytochemicals contributing to the health benefits attributed to this herbal drug
Identification and quantitative determination of the polar constituents in Helichrysum italicum flowers and derived food supplements
No full text- …
