Morus macroura Miq. Fruit extract protects against acetic acid-induced ulcerative colitis in rats: Novel mechanistic insights on its impact on miRNA-223 and on the TNFα/NFκB/NLRP3 inflammatory axis.

Nod-like receptor pyrin domain-1 containing 3 (NLRP3) inflammasome/tumor necrosis factor alpha (TNFα)/nuclear factor kappa B (NFκB) inflammatory pathway is known to be involved in the pathogenesis of ulcerative colitis (UC). Inversely, miRNA-223 can exert counter-regulatory effect on NLRP3 expression. The mulberry tree (Morus macroura) fruit is attaining increased importance for its antioxidant and anti-inflammatory activity in addition to its high safety profile. Accordingly, we attempted to explore the possible protective effect of mulberry fruit extract (MFE) in acetic acid (AA)-induced UC rat model. Phytochemical constituents of MFE were characterized using high performance liquid chromatography coupled to mass spectrometry (HPLC-MS). In the in vivo study, three doses of MFE were orally given for seven days before intra-rectal induction of UC by AA on day eight. Screening study revealed that MFE (300 mg/kg) significantly reduced macroscopic and microscopic UC scores. Biochemically, MFE ameliorated oxidative stress, levels of TNFR1, NLRP3, p-NFκB p65, TNFα, IL-1ß, and IL-18, caspase-1 activity, but enhanced miRNA-223 expression. In conclusion, our study provided a novel protective impact for MFE against UC, in which miRNA-223 and TNFα/NFκB/NLRP3 pathway are involved. These results provide a promising step that might encourage further investigations of MFE as a protective agent in UC patients.

Chemical composition and biological evaluation of the volatile constituents from the aerial parts of Nephrolepis exaltata (L.) and Nephrolepis cordifolia (L.) C. Presl grown in Egypt.

The essential oil from the aerial parts of Nephrolepis exaltata and Nephrolepis cordifolia obtained by hydro-distillation were analyzed by gas chromatography/ mass spectrometry. The essential oils exhibited potential antibacterial and antifungal activities against a majority of the selected microorganisms. NEA oil showed promising cytotoxicity in breast, colon and lung carcinoma cells. The results presented indicate that NEA oil could be useful alternative for the treatment of dermatophytosis. Comparative investigation of hydro-distilled volatile constituents from aerial parts (A) of Nephrolepis exaltata (NE) and Nephrolepis cordifolia (NC) (Family Nephrolepidaceae) was carried out. Gas chromatography/mass spectrometry revealed that oils differ in composition and percentages of components. Oxygenated compounds were dominant in NEA and NCA. 2,4-Hexadien-1-ol (16.1%), nonanal (14.4%), ß-Ionone (6.7%) and thymol (2.7%) were predominant in NEA. ß-Ionone (8.0%), eugenol (7.2%) and anethol (4.6%) were the main constituents in NCA. Volatile samples were screened for their antibacterial and antifungal activities using agar diffusion method and minimum inhibitory concentrations. The cytotoxic activity was evaluated using viability assay in breast (MCF-7), colon (HCT-116) and lung carcinoma (A-549) cells by the MTT assay. The results revealed that NEA oil exhibited potential antimicrobial activity against most of the tested organisms and showed promising cytotoxicity.

Flavonoids with acetylated branched glycans and bioactivity of Tipuana tipu (Benth.) Kuntze leaf extract.

The new acetylated kaempferol tetraglycoside, kaempferol-3-O-[2″(4-acetylrhamnopyranosyl)-3″-galactopyranosyl] robinobioside (1), was isolated from the aqueous methanolic leaf extract of Tipuana tipu Benth. The known kaempferol 3-[2″-(4-acetyl-rhamnosyl)] robinobioside (2), kaempferol 3-O-2″-rhamnopyranosylrutinoside (3), rutin (4), kaempferol 3-O-rutinoside (5), kaempferol 3-O-glucopyranoside (6), kaempferol 3-O-galactopyranoside (7), quarcetin 3-O-glucopyranoside (8), kaempferol (9) and quercetin (10) together with the chlorogenic acid (11) were also isolated and characterised. Structures were established on the basis of chemical and spectroscopic analysis including (1)H NMR, (13)C NMR, 2D NMR and ESI-MS. The methanol extract exhibited moderate antioxidant activity, IC50 28.96 µg/mL, compared with ascorbic acid (1.83 µg/mL) and tertiary-butylhydroquinone (1.92 µg/mL). The methanol and chloroform extracts exhibited potent cytotoxic activity; the former was found to be active against larynx and liver cell lines, while the latter being active against intestine and liver cell lines.

Two new flavonol glycosides and biological activities of Diplotaxis harra (Forssk.) Boiss.

Two new flavonol glycosides, isorhamnetin 3-O-ß-glucopyranoside-4'-O-ß-xylopyranoside (1) and kaempferol 3-O-ß-glucopyranoside -4'-O-ß-xylopyranoside (2), were isolated from the defatted aqueous methanol extract of the whole plant Diplotaxis harra along with 12 known flavonols (3-14). They were characterised by chemical and spectral methods. The 70% aqueous methanol, chloroform and defatted aqueous methanol plant extracts exhibited significant antioxidant effects (nitroblue tetrazolium reduction method). Their cytotoxic activity was carried out against 11 tumour cell lines (sulphorhodamine B assay). The three extracts expressed the greatest antiproliferative activity against colon 38, P388 and MKN-28 with GI50 (0.45, 0.4, 0.07 µg/mL) and against P388 [3-(4,5-dimethylthiazol-2yl)-2,5-diphenyltetrazolium bromide assay] with IC50 (0.26, 0.24, 0.25 µg/mL), respectively. The chloroform extract showed the highest activity as eukaryotic DNA topoisomerase II inhibitors of P388 with IC50 0.24 µg/mL. Antiviral screening of the extracts and the pure compounds against foot-and-mouth disease virus types A and O revealed a prominent inhibition of its cytopathic effect.

1H-NMR assay of papaverine hydrochloride and formulations.

A precise and specific 1H-NMR method has been developed for the assay of papaverine hydrochloride (1) as a bulk drug, as well as in tablet and injection dosage forms. The assay depends upon the integration of the 12 protons of the four methoxy groups of 1 relative to that of the three methyl protons of acetanilide (internal standard). In addition to the accurate quantitative determination of 1, the method provides a specific means of identifying 1 as well as detecting other alkaloids or impurities.

Acylated flavonol diglucosides from Lotus polyphyllos.

Three acylated flavonol diglucosides, kaempferol 3-O-beta-(6"-O-E-p-coumaroylglucoside)-7-O-beta-glucoside; quercetin 3-O-beta-(6"-O-E-p-coumaroylglucoside)-7-O-beta-glucoside; isorhamnetin 3-O-beta-(6"-O-E-p-coumaroylglucoside)-7-O-beta-glucoside were isolated from the whole plant aqueous alcohol extract of Lotus polyphyllos. The known 3,7-di-O-glucosides of the aglycones kaempferol, quercetin and isorhamnetin were also characterized. All structures were established on the basis of chemical and spectral evidence.