Metabolomics combined to chemometrics reveals the putative α-glucosidase and α-amylase inhibitory metabolites of ground cherry (Physalis pruinosa L.).

In this work, metabolic profiling of the different parts of ground cherry (P. pruinosa) including fruits, calyces, leaves, stems and roots using UPLC-MS/MS analysis combined to chemometric analysis was attempted. A total of 82 chromatographic peaks belonging to different metabolite classes were identified including terpenes, flavonoids genin and glycosides, withanolides, physalins, sucrose esters, fatty acids and other miscellaneous compounds with withanolides being the most predominant class. Roots extracts possessed the highest relative content of the identified 5ß,6ß-epoxy withanolides and intermediate withanolides, while sucrose esters and flavonoidal glycosides were found in a great abundance in calyces extracts. Moreover, physalins were found in all extracts except for roots extracts. Studying the coefficients plots revealed that terpenes and physalins (physanicantriol, loliolide, physalisitin C) were responsible for discrimination of fruits extracts. Calyces, leaves and stems extracts were found to possess antioxidant activity and higher inhibition of α-glucosidase activity. In an attempt to identify the compounds responsible for the hypoglycemic activity using both α-amylase and α-glucosidase inhibition assays, OPLS models coefficient plots were constructed which indicated that physangulide B, physaperuvin G, neophysalin A, and acylsucroses were positively correlated to α-glucosidase inhibition, while guaiacyl-primeveroside, phyperunolide C, physalactone, physalolactone C and perulactone, were positively correlated to α-amylase inhibitory activity.

Chemical constituents, Antibacterial and Acetylcholine esterase inhibitory activity of Cupressus macrocarpa leaves.

The chemical constituents of Cupressus macrocarpa were investigated. A new neolignan glycoside (1) in addition to nine known compounds were isolated. The acetylcholinesterase (AChE) inhibitory activity and antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA) of different fractions and isolates of C. macrocarpa were evaluated. The light petroleum fraction showed the highest activity in both assays with IC50 value of 88.79 µg/ml and 152.58 µg/ml for the AChE inhibitory activity and MRSA antibacterial activities, respectively. Weak to moderate activity were detected for the isolated compounds.

Acylated pregnane glycosides from Caralluma tuberculata and their antiparasitic activity.

Five pregnane glycosides were isolated from Caralluma tuberculata (1-5), in addition to a known one (russelioside E, 6). The structures of the isolated compounds were elucidated by the analysis of NMR data and FAB-MS experiments. All the isolated compounds were tested for their antimalarial and antitrypanosomal activities as well as their cytotoxicity against human diploid embryonic cell line (MRC5).

Chemical composition, antimicrobial and insecticidal activities of the essential oils of Conyza linifolia and Chenopodium ambrosioides.

Two essential oil-containing plants growing wildly in Egypt: Conyza linifolia (Willd.) Täckh. (Asteraceae) and Chenopodium ambrosioides L. (Chenopodiaceae) were subjected to essential oil analysis and biological investigation. The essential oils from both plants were prepared by hydrodistillation, and GC/MS was employed for volatiles profiling. This study is the first to perform GC/MS analysis of C. linifolia essential oil growing in Egypt. C. linifolia essential oil contained mainly sesquiterpenes, while that of C. ambrosioides was rich in monoterpenes. Ascaridole, previously identified as the major component of the latter, was found at much lower levels. In addition, the oils were investigated for their antimicrobial activity against two Gram positive and two Gram negative bacteria, and one fungus. The insecticidal activities of both oils, including mosquitocidal and pesticidal potentials, were also evaluated. The results of biological activities encourage further investigation of the two oils as antimicrobial and insecticidal agents of natural origin.

Chemical constituents from Tribulus terrestris and screening of their antioxidant activity.

Two oligosaccharides (1,2) and a stereoisomer of di-p-coumaroylquinic acid (3) were isolated from the aerial parts of Tribulus terrestris along with five known compounds (4-8). The structures of the compounds were established as O-ß-D-fructofuranosyl-(2→6)-α-D-glucopyranosyl-(1→6)-ß-D-fructofuranosyl-(2→6)-ß-D-fructofuranosyl-(2→1)-α-D-glucopyranosyl-(6→2)-ß-D-fructofuranoside (1), O-α-D-glucopyranosyl-(1→4)-α-D-glucopyranosyl-(1→4)-α-D-glucopyranosyl-(1→2)-ß-D-fructofuranoside (2), 4,5-di-p-cis-coumaroylquinic acid (3) by different spectroscopic methods including 1D NMR ((1)H, (13)C and DEPT) and 2D NMR (COSY, TOCSY, HMQC and HMBC) experiments as well as ESI-MS analysis. This is the first report for the complete NMR spectral data of the known 4,5-di-p-trans-coumaroylquinic acid (4). The antioxidant activity represented as DPPH free radical scavenging activity was investigated revealing that the di-p-coumaroylquinic acid derivatives possess potent antioxidant activity so considered the major constituents contributing to the antioxidant effect of the plant.

Antihyperglycaemic and hypolipidaemic effects of the methanolic extract of Caralluma tuberculata in streptozotocin-induced diabetic rats.

The antihyperglycaemic and hypolipidaemic effects of the methanolic extract of Caralluma tuberculata were investigated in streptozotocin (STZ)-induced diabetic rats. The antihyperglycaemic activity was assessed by the reduction in fasting blood glucose (54% at 4th week) and the peak of blood glucose at 120?min of an oral glucose tolerance test in diabetic rats. Further, the tested extract also increased plasma insulin by 206.8%. The hypolipidaemic action of the extract was evident by the significant decrease in the levels of total cholesterol, triglycerides and LDL-cholesterol by 41.5%, 36.7% and 49.1%, respectively, compared to diabetic rat values. Interestingly, the extract increased the cardio-protective lipid HDL-cholesterol by 147.97% as compared to diabetic rat value. The present data suggests that the methanolic extract of C. tuberculata has both antihyperglycaemic and hypolipidaemic effects in STZ-induced diabetic rats that may need further studies to be used in the management of diabetes and associated hyperlipedaemia.

Chemical composition, insecticidal and insect repellent activity of Schinus molle L. leaf and fruit essential oils against Trogoderma granarium and Tribolium castaneum.

Fruit and leaf essential oils of Schinus molle showed insect repellent and insecticidal activity against Trogoderma granarium and Tribolium castaneum. In these oils, 65 components were identified by GC-MS analysis. Hydrocarbons dominated the oil composition with monoterpenes occurring in the largest amounts in fruits and leaves, 80.43 and 74.84%, respectively. p-Cymene was identified as a major component in both oils. The high yield and efficacy of S. molle essential oil against T. granarium and T. castaneum suggest that it may provide leads for active insecticidal agents.

Antihepatotoxic effect of marrubium vulgare and withania somnifera extracts on carbon tetrachloride-induced hepatotoxicity in rats.

Marrubium vulgare and Withania somnifera are used in folk medicine of several countries. Many researches showed that they are used for the treatment of variety of diseases due to their antioxidant effects. The present aim of this study was to evaluate the antihepatotoxic and antioxidant activities of the both extracts against carbon tetrachloride (CCl4)-induced hepatic damage in rats. Both extracts were given orally in a dose of 500 mg/kg/day for 4 weeks along with CCl4 started at the 7th week of induction of hepatotoxicity. The antihepatotoxic activity was assessed by measuring aspartate transaminase (AST), alanine transaminase (ALT), lactate dehydrogenase (LDH), alkaline phosphatase (ALP), glutathione peroxidase (GPx), glutathione reductase (GR), glutathione-S-transferase (GST), reduced glutathione (GSH), tissue content and malondialdehyde (MDA) as well as histopathological examination. Both extracts showed a significant antihepatotoxic effect by reducing significantly the levels of AST, ALT and LDH. However, ALP levels were decreased non-significantly. Regarding the antioxidant activity, they exhibited significant effects by increasing the GPx, GR and GST activities with increased GSH tissue contents and decreased production of MDA level. Furthermore, both extracts alleviated histopathological changes in rats' liver treated with CCl4. M. vulgare and W. somnifera protect the rats' liver against CCl4-induced hepatotoxicity. This effect may be attributed, at least in part, to the antioxidant activities of these extracts.

Iridoid glycosides from Barleria trispinosa.

A new iridoid glycoside and three known iridoid glycosides were isolated from the aerial parts of Barleria trispinosa. The structure of the new compound was determined as 6-alpha-L-rhamnopyranosyl-8-O-acetylshanzihiside methyl ester. The known compounds were identified as 6,8-O,O-diacetylshanhiside methyl ester (acetyl barlerin), 8-O-acetylshanzhiside methyl ester (barlerin) and shanzhiside methyl ester, which were isolated from the plant for the first time. The structures of the isolated compounds were elucidated by spectroscopic evidence, mainly one- and two-dimensional proton and carbon-13 NMR spectroscopy.

Antiplasmodial and antitrypanosomal activity of plants from the Kingdom of Saudi Arabia.

The antiplasmodial and antitrypanosomal activity of the methanol extracts of 42 plants collected from the Kingdom of Saudi Arabia and some fractions obtained thereof were evaluated. The antiplasmodial activity was tested in vitro against chloroquine-resistant strain (K1) and sensitive strain (FCR3), and the antitrypanosomal activity was tested in vitro against Trypanosoma brucei brucei GUTat 3.1 strain. For host cells, the cytotoxicity of the active extracts was also evaluated against the MRC5 human cell line. Only extracts of three samples demonstrated good antiplasmodial activity (IC(50) < 12.5 and > 1.56 microg/ml, score 2), the methanol extracts of Lycium shawii, Heliotropium zeylanicum and the petroleum ether-soluble fraction of the methanol extract of Caralluma tuberculata, while extracts of the remaining 42 plants were inactive (IC(50) > 12.5 microg/ml, score 1). As for the antitrypanosomal activity, the methanol extract of Solanum schimperianum demonstrated the highest activity (IC(50) 0.061 microg/ml), followed by the petroleum ether-soluble fraction of the methanol extract of C. tuberculata (IC(50) 0.5 microg/ml). The chloroform-soluble fraction of the methanol extract of C. tuberculata was moderately active (IC(50) 3.5 microg/ml), with low cytotoxicity (IC(50) 62.6 microg/ml) and moderate selectivity index (SI 17.9). The methanolic extracts of 34 plants showed good activity with score 2 (IC(50) < 12.5 and > 1.56 microg/ml), while the extracts of seven plants were inactive (IC(50) > 12.5 microg/ml, score 1).