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Background: Nepeta deflersiana (Lamiaceae) is a perennial herb used in the Saudi and Yemeni folk medicine as an anti-inflammatory, carminative, and antirheumatic agent.Purpose: This study explores the phytochemistry of the plant and the cardioprotective effect of N. deflersiana ethanolic extract (NDEE) against isoproterenol (ISP)-induced myocardial injury in rats.Design/methods: Cardiac function, serum cardiac enzymes, myocardial antioxidants, inflammatory, and apoptotic biomarkers, and histopathological parameters were studied in ISP-injured Wistar rat heart tissues.Results: To the best of our knowledge, this is the first study to report the isolation of nine secondary metabolites from this plant: 1α-hydroxy-7α,14α,18-triacetoxy-isopimara-8,15-diene (1), β-sitosterol (2), lupeol (3), ursolic acid (4), 2,3-dihydroxy ursolic acid (5), caffeic acid (6), methyl rosmarinate (7), rosmarinic acid (8), and an irridoid glucoside 8-epi-7-deoxyloganic acid (9). To explain the mechanisms underlying the cardioprotective effect of NDEE, we evaluated the redox-sensitivity of NDEE in ISP-induced cardiac injury. The oral administration of NDEE (50 and 100 mg/kg b.w) prevented the depletion of endogenous antioxidants (CAT, SOD, NP-SH, and NO) and myocyte injury marker enzymes and inhibited lipid peroxidation (MDA, MPO). Moreover, NDEE downregulated the expression of pro-inflammatory cytokines (TNFα, IL-6, and IL-10) and apoptotic markers (caspase-3 and Bax) and upregulated the anti-apoptotic protein Bcl2. Furthermore, NDEE pretreatment significantly downregulated cardiac NF-κB (p65) expression, NF-κB-DNA binding activity, and MPO activity. Histological data showed that NDEE pretreatment reduced myonecrosis, edema, and infiltration of inflammatory cells and restored the architecture of cardiomyocytes.Conclusion: NDEE demonstrated strong antioxidant, cardioprotective, anti-inflammatory, and anti-apoptotic potential against myocardial damage. This further endorses the use of N. deflersiana in Yemeni folk medicine against cardiovascular diseases. [ABSTRACT FROM AUTHOR]

Abstract: Two new flavane gallates were isolated from the leaves of Plicosepalus curviflorus. The structure of the new compounds was established as 2S,3R-3,3′,4′,5,7-pentahydroxyflavane-5-O-gallate (1) and 2S,3R-3,3′,4′,5,5′,7-hexahydroxyflavane-4′,5-di-O-gallate (2), respectively. In addition, seven known compounds (−)-catechin (3), quercetin (4), lupeol (5), β-sitosterol (6), pomolic acid (7), β-sitosterol 3-O-β-d-glucopyranoside (8) and 4-methoxycinnamic acid (9) were reported for the first time from the genus Plicosepalus. Compounds 1, 2 and 3 were investigated for their hypoglycemic activity and showed significant hypoglycemic activity in Swiss Albino mice. [Copyright &y& Elsevier]

Abstract: The present article describes the synthesis of some novel 4-(2-amino-3-cyano-4-(substituted-aryl)-5-oxo-5,6,7,8-tetrahydroquinolin-1(4H)-yl)benzenesulfonamide (23–41) starting with 4-(3-oxo-cyclohex-1-enylamino)benzenesulfonamide (3). All the newly synthesized compounds were evaluated for their in vitro antitumor activity. Compounds 32, 25, 41, 35, 33, and 37 with IC50 values (2.5, 3, 5, 10, 12, and 12.5μg/mL) are more potent and efficacious than Doxorubicin (CAS-23214-92-8) as reference drug with (IC50 value=37.5μg/mL). Also, compounds 28, 30, 31, and 34 (with IC50 values=25μg/mL) are nearly as active as Doxorubicin. [Copyright &y& Elsevier]

Abstract: Some novel quinolines and pyrimido[4,5-b]quinolines have been synthesized. The structures of which were confirmed by elemental analyses and spectral data. All the target compounds were subjected to in-vitro antitumor activity against Ehrlich Ascites Carcinoma (EAC) cells. Compounds 24, 19 and 12 showed higher activity with IC50 values (5.5, 6.9, 7μg/ml) when compared with Doxorubicin as a reference drug (IC50 value 38μg/ml). [Copyright &y& Elsevier]

Abstract: A large number of antimitotic drugs, derived from natural sources or chemically synthesized, have been identified and shown to interfere with the tubulin system. Inhibition of tubulin polymerization is among the important targets useful in the cancer therapy. The present work reports the synthesis of some novel quinoline derivatives bearing a trimethoxyphenyl moiety. The trimethoxybenzene moiety has been reported to be crucial to obtain relevant cytotoxic and antitubulin responses. All the newly synthesized compounds were evaluated for their in vitro anticancer activity. Several compounds showed interesting cytotoxic activities compared to the used reference drug. [Copyright &y& Elsevier]

• Precautionary measurements taken by the Kingdom of Saudi Arabia (KSA) and their results on the outcome of the nCOVID-19. • An overview on the pandemic related data during the curfews congregate from Saudi's Ministry of Health (MoH). • Services released by the KSA government toward nCOVID-19 including; smartphone-based apps and others. Coronavirus (nCOVID-19) cases are increasing not only daily but also hourly worldwide. Therefore, it is important to look into how developed countries are managing this pandemic and also observe their experiences and estimations in dissimilar consequences. In this study, we compared the results of the precautionary measurements taken by the Kingdom of Saudi Arabia (KSA) and higher officials on the outcome of the nCOVID-19. We examined all the current pandemic related data, including the total number of cases, total recovered, total deaths with the curfew phases, and the various actions taken by Saudi's Ministry of Health, World Health Organization, Web of Science, Sci Finder, MEDLINE, and the Worldometer. The total number of cases, recovered cases, deaths, and peak days were templated using Microsoft Excel sheets and graphs. During this pandemic, the KSA government released many services such as smartphone-based apps and media campaigns to control the spread and contact of the virus among people. All these early extreme precautionary measures and services implemented by the KSA government reduce the number of deaths from the nCOVID-19 in Saudi Arabia. The curfew phases enforced by the government recorded few deaths during the first two phases, whereas a noticeable increase in the number of deaths and the total number of cases were recorded during Phase 3. All these limitations and precautionary measures, including the different phases of curfew, assumed a significant role in restricting the spread of nCOVID-19 and reducing the number of cases and deaths among people. Coronavirus (nCOVID-19) outbreak has shocked the world causing more cases than the latest global epidemics. It is necessary to specify how developed countries managing this pandemic outbreak. In this study, we lined up to compare the results of the precautionary measurements taken by the Kingdom of Saudi Arabia (KSA) on the outcome of the nCOVID-19. All current pandemic related data: total cases, total recovered, total deaths and actions were congregate from Saudi's Ministry of Health (MoH), World Health Organization (WHO). Total number of cases, recovered cases and deaths were templated by using Microsoft Excel sheets and graphs. The KSA government had released many services including smartphone-based apps, and media campaigns to control the spread and contact to the nCOVID-19 positive persons. All these limitations and precautionary measures including different phases of curfew assumed a significant role in restricting the spread of nCOVID-19 and reduce cases and deaths numbers. [ABSTRACT FROM AUTHOR]

Anvillea garcinii is a medicinal plant used in the Arab region for intestinal diseases, lungs and liver diseases, digestive problems, and as an anti-diabetic. Repeated chromatographic purifications of A. garcinii leaves led to the isolation of two undescribed guaiane sesquiterpene lactones (1 – 2), along with four known germacranolides (3–6). The structures of the new compounds were established using spectroscopic (1D, 2D NMR) and spectrometric methods (ESIMS). Compounds 1 and 2 were shown to possess hydroxyl substituents at position 9, a structural feature rarely reported in guaianolide-type sesquiterpenes. The antimicrobial activity of 1 – 6 was screened against five different gram-positive/negative bacteria and the fungi Candida albicans and C. parapsilosis. Compounds 1 and 2 displayed remarkable antifungal effect against C. albicans and C. parapsilosis and potent antibacterial activities against Staphylococcus aureus. Unlabelled Image [ABSTRACT FROM AUTHOR]

Phytochemical investigation of Penicillium sp. RO-11 strain, collected from the sediments of a hydrothermal spring located in the southwestern area of Saudi Arabia, afforded, along with previously isolated compounds, the undescribed polyketides penicillactonin (1), penipyranicin D (4) and isopyrenulin B (5) and the undescribed meroterpenoid preaustinoid C (7). The structures of these compounds were elucidated based on data from mass spectrometry, 1D and 2D NMR, and comparison between experimental and calculated ECD spectra. Penicillactonin and preaustinoid C bring unprecedented structural features, for which a biosynthetic rationale is proposed, further extending the chemodiversity associated to Penicillium fungi. Preaustinoid C showed significant activity against LPS-induced NO production and selective effect on IL-2 and IFN-γ gene regulation in activated Jurkat cells. [Display omitted] [ABSTRACT FROM AUTHOR]

Crocosmia × crocosmiiflora (montbretia) flowers yielded four esters (montbresides A–D) of a new sucrose-based tetrasaccharide, 3- O -β- d -glucopyranosyl-4´- O -α- d -rhamnopyranosyl-sucrose [β- d -Glc-(1 → 3)-α- d -Glc-(1↔2)-β- d -Fru-(4 ← 1)-α- d -Rha]. All four possess O - p -coumaroyl residues on C-3 of fructose and C-4 of α-glucose, plus O -acetyl residues on C-2 and C-3 of rhamnose and C-6 of fructose. Montbresides A and B are additionally O -acetylated on C-1 of fructose. The p -coumaroyls are trans- in montbresides A and C and cis- in B and D. Elemental compositions were determined from MS data, and structures from 1D and 2D NMR spectra. Monosaccharide residues were identified from selective 1D TOCSY spectra and TLC, and acylation sites from 2D HMBC spectra. Enantiomers were distinguished by enzymic digestion. Montbretia flower extracts were cytotoxic against six human cancerous cell-lines, but purified montbresides lacked cytotoxicity. Each montbreside displayed antibacterial activity against Staphylococcus aureus (minimal inhibitory concentration ~6 μg/ml). Montbretia is a potential source of new cytotoxins and antibacterial agents. Unlabelled Image • Four novel p -coumaroylated, acetylated tetra saccharides were isolated. • Their structures were identified by spectroscopic analysis. • Sugar linkages were deduced from 2D HMBC data and enzymic digestion. • Significant cytotoxicity was observed from montbretia flower extract. • Potent antibacterial activities of isolated compounds. [ABSTRACT FROM AUTHOR]