New secoiridoid ester of swertiamarin and secoxyloganic acid with hepatoprotective activity from Centaurium spicatum L.

Context: Centaurium spicatum (L.) Fritsch (Gentianaceae) is an annual herb occurring in Southern Europe and Northern Africa where it is used in traditional medicine for treatment of numerous illness. Aims: To isolate compounds from C. spicatum having hepatoprotective activity. Methods: Structure elucidation of the new compound was established on the basis of 1D and 2D NMR analyses including 1H-, 13C- NMR, DEPT-135 NMR, HMQC, HMBC and H- H HOHAHA experiments in addition to FAB+ and HRFAB+ Mass spectrometry. In vivo transaminases inhibition activity was carried out. Results: A new ester of swertiamarin and secoxyloganic acid (1) was isolated from C. spicatum in addition to its known components secoiridoids swertiamarin (2) and secoxyloganic acid (3). All tested secoiridoids have transaminases inhibition activity with different values for each compound 1, 2, 3 (86, 83, 81%) for SGOT and (96, 93, 91%) for SGPT, respectively. Conclusions: The new ester compound from C. spicatum has hepatoprotective activity over than its components

Effect of polyphenols from <i>Vicia faba</i> L on lipase activity and melanogenesis

<p>Two new flavonoid glycosides, kaempferol 3-<i>O</i>-<i>α</i>-L-rhamnopyranosyl (1→6) (3′′-acetyl)-<i>β</i>-D-galactopyranoside <b>1</b> and kaempferol 3-<i>O</i>-<i>α</i>-L-arabinopyranosyl-5-<i>O</i>-<i>α</i>-L-rhamnopyranoside <b>2</b>, along with six known ones <b>3–8</b> were isolated from the flowers of <i>Vicia faba</i> L. (Fabaceae). Methanol extract and the isolated compounds were tested against lipase and melanogenesis inhibition activities and resulted in that compound <b>2</b> showed 53 and 77% lipase inhibition activity in concentrations of 400 and 800 μg/mL, respectively. For melanogenesis, compounds <b>2</b>, <b>3</b> and <b>4</b> exhibited potent melanogenesis inhibition activity where the melanin content in melanoma cells was decreased to be about 57.5, 56 and 61%, respectively, with no obvious melanocytotoxicity. The rest of compounds showed weak to moderate activity. The results of melanogenesis inhibition activity of this study suggested the potential use of <i>Vicia faba</i> flowers as a skin-whitening agent and reveal the flowers to be a rich source of important phytochemicals with antilipase and melanogenesis inhibitory activity.</p

Mangostanaxanthone VIII, a new xanthone from <i>Garcinia mangostana</i> and its cytotoxic activity

<p>A new prenylated xanthone, mangostanaxanthone VIII (<b>7</b>) and six known metabolites: gartanin (<b>1</b>), 1,3,8-trihydroxy-2-(3-methyl-2-butenyl)-4-(3-hydroxy-3-methylbutanoyl)-xanthone (<b>2</b>), rubraxanthone (<b>3</b>), 1,3,6,7-tetrahydroxy-8-prenylxanthone (<b>4</b>), garcinone C (<b>5</b>), and xanthone I (9-hydroxycalabaxanthone) (<b>6</b>) were separated from the EtOAc-soluble fraction of the air-dried pericarps of <i>Garcinia mangostana</i> (Clusiaceae). Their structures have been verified on the basis of spectroscopic data analysis as well as comparison with the literature. The cytotoxic activity of <b>7</b> was assessed against MCF7, A549, and HCT116 cell lines using sulforhodamine B (SRB) assay. Compound <b>7</b> showed significant cytotoxic potential against MCF7 and A549 cell lines with IC₅₀s 3.01 and 1.96 μM, respectively compared to doxorubicin (0.06 and 0.44 μM, respectively). However, it exhibited moderate activity towards HCT116 cell line.</p

Chemical Review of Gorgostane-Type Steroids Isolated from Marine Organisms and Their ¹³C-NMR Spectroscopic Data Characteristics

Gorgostane steroids are isolated from marine organisms and consist of 30 carbon atoms with a characteristic cyclopropane moiety. From the pioneering results to the end of 2021, isolation, biosynthesis, and structural elucidation using 13C-NMR will be used. Overall, 75 compounds are categorized into five major groups: gorgost-5-ene, 5,6-epoxygorgostane, 5,6-dihydroxygorgostane, 9,11-secogorgostane, and 23-demethylgorgostane, in addition to miscellaneous gorgostane. The structural diversity, selectivity for marine organisms, and biological effects of gorgostane steroids have generated considerable interest in the field of drug discovery research

Forsskamide, a new ceramide from aerial parts of <i>Forsskaolea tenacissima</i> Linn.

<p>Although the various folk medicine uses and the biological activity of <i>Forsskaolea tenacissima</i> L., few chemical constituents of this plant have been reported, this provoked us to make our study. Forsskamide, a new ceramide was isolated from aerial parts of <i>F. tenacissima</i> L. (Urticaceae). The chemical structure was established by different spectroscopic methods (¹H, ¹³C-NMR, HMBC, HSQC, ROESY, FAB-MS and HR-FAB-MS). Forsskamide showed a moderate cytotoxic activity by (MTT) method against human colorectal carcinoma cell line (HCT-116) with IC₅₀ 33.25 μM in comparison with 5-fluorouracil IC₅₀ 26.42 μM. While, it did not show any activity against human hepatocarcinaoma cell line (HepG-2).</p

A Comprehensive In Silico Study of New Metabolites from Heteroxenia fuscescens with SARS-CoV-2 Inhibitory Activity

Chemical investigation of the total extract of the Egyptian soft coral Heteroxenia fuscescens, led to the isolation of eight compounds, including two new metabolites, sesquiterpene fusceterpene A (1) and a sterol fuscesterol A (4), along with six known compounds. The structures of 1&ndash;8 were elucidated via intensive studies of their 1D, 2D-NMR, and HR-MS analyses, as well as a comparison of their spectral data with those mentioned in the literature. Subsequent comprehensive in-silico-based investigations against almost all viral proteins, including those of the new variants, e.g., Omicron, revealed the most probable target for these isolated compounds, which was found to be Mpro. Additionally, the dynamic modes of interaction of the putatively active compounds were highlighted, depending on 50-ns-long MDS. In conclusion, the structural information provided in the current investigation highlights the antiviral potential of H. fuscescens metabolites with 3&beta;,5&alpha;,6&beta;-trihydroxy steroids with different nuclei against SARS-CoV-2, including newly widespread variants