Hepatoprotective and TNF-α inhibitory activity of Zosima absinthifolia extracts and coumarins.

Zosima absinthifolia (ZA) extracts and the coumarins (+)-columbianadin and (-)-deltoin were evaluated for their potential hepatoprotective and antiinflamatory effects in a CCl(4)-induced hepatotoxicity assay in rats and by the inhibition of TNF-α production on LPS-stimulated THP-1 macrophages, respectively. Both the ZA extracts and the coumarins showed hepatoprotective activity confirmed by monitoring the ALT/AST levels and by histopathological examination. The antiinflamatory activity, proved by the inhibition of TNF-α production, was found to be higher for the n-hexane root extract than for coumarins, suggesting synergic potential of the extract.

Multidisciplinary approach on characterizing a mechanochemically activated composite of vinpocetine and crospovidone.

Significant improvement of solubilization kinetics of poorly soluble vinpocetine was obtained through a mechanochemical activation process in presence of micronized crospovidone. Drug-to-polymer weight ratio and milling time variables resulted to have statistically significant impacts on the activation of the product. The complete amorphization was obtained in the coground with the highest crospovidone contents (>80% wt), milled for the longest time (180 min).

Identification of non-alkaloid acetylcholinesterase inhibitors from Ferulago campestris (Besser) Grecescu (Apiaceae).

Inhibition of Acetylcholinesterase (AChE) is still considered as a strategy for the treatment of neurological disorders such as Alzheimer's disease. Many plant derived alkaloids (such as galantamine and rivastigmine) are known for their AChE inhibitory activity. Recently, other classes of natural compounds such as terpenoids, sesquiterpene glycosides and coumarins have been studied as new AChE inhibitors, with the aim to discover less toxic compounds compared to alkaloidal ones.

The phototoxicity of fluvastatin, an HMG-CoA reductase inhibitor, is mediated by the formation of a benzocarbazole-like photoproduct.

In this paper, we have investigated the mechanism of phototoxicity of fluvastatin, an 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor, in human keratinocytes cell line NCTC-2544. Fluvastatin underwent rapid photodegradation upon Ultraviolet-A (UVA) irradiation in buffered aqueous solution as shown by the changes in absorption spectra. Interestingly, no isosbestic points were observed but only a fast appearance of a spectral change, indicative of the formation of a new chromophore.

Erythroid induction of chronic myelogenous leukemia K562 cells following treatment with a photoproduct derived from the UV-A irradiation of 5-methoxypsoralen.

Induction of terminal erythroid differentiation can be an efficient strategy to inhibit proliferation of chronic myelogenous leukemia cells. Psoralens, well-known photo-chemotherapeutic agents, were found to be efficient at inducing erythroid differentiation of K562 cells, an in vitro cell line isolated from the pleural effusion of a patient with chronic myelogenous leukemia in blast crisis. The effects of crude pre-irradiated solutions of 5-methoxypsoralen on erythroid differentiation of human leukemic K-562 cells were evaluated.

Analgesic compounds from Scorzonera latifolia (Fisch. and Mey.) DC.

Ethnopharmacological Relevance: A traditional mastic named yaki sakizi prepared from the roots of Scorzonera latifolia (Fisch. and Mey.) DC.

Evaluation of cytotoxic activity of Schisandra chinensis lignans.

Using exhaustive chromatographic separation we have isolated (-)-tigloyl-deangeloyl-gomisin F as a novel dibenzocyclooctadiene lignan from schisandra chinensis. With the help of HPLC, we further isolated (+)-schisandrin, (+)-deoxyschisandrin, (+)-γ-schisandrin, (-)-gomisin J, (+)-gomisin A, (-)-gomisin N, (-)-tigloyl-gomisin P, (-)-wuweizisu C, (-)-gomisin D, rubrisandrin A, (-)-gomisin G, (+)-gomisin K (3) and (-)-schisantherin C. A full NMR description of (-)-schisantherin C was carried out with the aim to confirm previous reports of its structure.

Chemical composition and biological properties of Rhododendron anthopogon essential oil.

The essential oil of Rhododendron anthopogon was investigated by GC-MS, and seventeen compounds (representing approximately 98% of the oil) were identified. The major components of the aerial parts of the oil were the monoterpenes alpha-pinene, beta-pinene, limonene and the sesquiterpene delta-cadinene. Biological studies revealed a weak topical anti-inflammatory activity; a significant killing effect against some Gram-positive reference strains: Staphylococcus aureus, Enterococcusfecalis, Bacillus subtilis was measured; Mycobacterium tuberculosis reference strain and a clinical isolate of Candida, C.

Evaluation of the antiradical activity of Schisandra chinensis lignans using different experimental models.

The in vitro antiradical activity of Schisandra chinensis lignans was investigated using DPPH, ABTS+, Fenton reaction inhibition and tyrosine-nitration inhibition assays, as were the in vivo antidiabetic activities of selected lignans in an animal model of alloxan-induced diabetes. Different degrees of antiradical activity were found, depending upon the structural parameters of the tested compounds. Unfortunately, the compounds showed no antidiabetic activity in concentration range tested.

Cytotoxic activities of several geranyl-substituted flavanones.

Nine geranylated flavanones isolated from the fruits of Paulownia tomentosa (4-12) and two from the roots of Morus alba (13 and 14) were examined for cytotoxicity to selected human cancer cell lines and normal human fibroblasts. Cytotoxicity was determined in vitro using a calcein AM cytotoxicity assay. Cytotoxicity for the THP-1 monocytic leukemia cell line was tested using erythrosin B cell staining.

Triterpene glycosides with in vitro anti-inflammatory activity from Cyclamen repandum tubers.

A new triterpene glycoside, repandoside (1) was isolated together with six known saponins (2-7) from the methanol extract of Cyclamen repandum tubers. The isolated saponins were characterized by high resolution mass spectrometry and both 1D and 2D NMR experiments. The in vitro effect of saponins on LPS-induced IL-8 and TNF-alpha mRNA level (by quantitative RT-PCR) and protein release (by ELISA) was evaluated in human THP-1 macrophages.

Phytochemical composition and antioxidant activity of Laurus nobilis L. leaf infusion.

Laurus nobilis L. (laurel) leaves are frequently used as a spice for cooking purposes. Folk medicine in many countries uses the infusion of the plant in stomachic and carminative remedies, as well as for the treatment of gastric diseases.

Glycosylated nervogenic acid derivatives from Liparis condylobulbon (Reichb.f.) leaves.

Three new nervogenic acid glycosides, 1-O-alpha-L-rhamnopyranosyl 3,5-bis(3-methyl-but-2-enyl)-4-O-[alpha-L-rhamnopyranosyl-(1-->2)-beta-D-glucopyranosyl]-benzoate, 3,5-bis(3-methyl-but-2-enyl)-4-O-[alpha-L-rhamnopyranosyl-(1-->2)-beta-D-glucopyranosyl]-benzoic acid, and bis{3,5-bis(3-methyl-but-2-enyl)-4-O-[alpha-L-rhamnopyranosyl-(1-->2)-beta-D-glucopyranosyl]-benzoyl} 1,2-O-beta-d-glucopyranose, which we named condobulbosides A-C, were isolated from a methanol extract of the leaves of Liparis condylobulbon together with an apigenin C-glycoside, schaftoside. Their structures were established on the basis of spectral techniques, namely, UV, IR, HR-MS spectroscopy, both 1D and 2D NMR experiments, and chemical reactions.

Essential oil of Lindera neesiana fruit: chemical analysis and its potential use in topical applications.

The composition of the essential oil of Lindera neesiana Kurz fruit was examined by GC-MS, (1)H, (13)C and bidimensional NMR techniques (HMQC, HMBC, COSY, TOCSY). Forty compounds were identified, representing approximately 86% of the oil: Z-citral (15.08%), E-citral (11.

In vitro estrogenic activity of Asplenium trichomanes L. extracts and isolated compounds.

Ethnopharmacological Relevance: Asplenium trichomanes was used as an expectorant, anti-cough remedy, laxative, emmenagogue, abortifacient and for irregular menses.

Aim Of The Study: To investigate the in vitro estrogenic activity of Asplenium trichomanes extracts and isolated compounds and their ability to activate ERalpha and ERbeta.

Materials And Methods: Leaves infusion (IF), decoction (DC) and methanol extract (ME) were prepared.

Two phenolic glycosides from Curculigo orchioides Gaertn.

One new glycoside derivative from syringic acid and one new phenol glycoside, curculigoside E (1) and orchioside D (2), were isolated and characterized from the rootstock of Curculigo orchioides collected in the Nawalparasi District (Nepal). The structures of the new isolated compounds were elucidated by means of spectroscopic methods such as 1D, 2D NMR and MS.

DNA binding ellipticine analogues: synthesis, biological evaluation, and structure-activity relationships.

In connection with our interest in the synthesis and study of the biological properties of ellipticine analogues as anticancer agents, some 7H-pyrido[2,3-c]carbazoles (7H-PyC) and their corresponding tetrahydro derivatives (7H-THPyC) were synthesized. A common multistep pathway characterized by conventional reactions involving carbazole Fischer and Conrad-Limpach quinoline syntheses yielded the tetracyclic compounds. With the aim to improve the cytotoxic activity of the new 7H-PyC derivatives, we provided them with one or two diethylaminoethyl side chains.

Xanthones from Polygala alpestris (Rchb.).

Bioactivity-guided fractionation of Polygala alpestris L. (Rchb.) extracts led to the identification of two new xanthones, 1,3,7-trihydroxy-2,6-dimethoxyxanthone (1) and 2,3-methylenedioxy-4,7-dihydroxyxanthone (2).

Cytotoxic activity of C-geranyl compounds from Paulownia tomentosa fruits.

The newly discovered 5,7-dihydroxy-6-geranylchromone ( 1) was isolated from PAULOWNIA TOMENTOSA fruit and subsequently characterized. The structure of the isolated compound was elucidated on the basis of extensive NMR experiments including HMQC, HMBC, COSY, and NOESY, as well as HR-MS, IR, and UV. The cytotoxicity of 1 was evaluated using a plant cell model represented by tobacco BY-2 cells.

UVB photolysis of hydrocortisone 21-acetate.

Hydrocortisone 21-acetate (HCA) in methanol solution undergoes photodegradation under UVB light, as monitored by HPLC. Five main photoproducts have been isolated and characterized by means of NMR and mass spectroscopy. One of them derives from a Norrish I photoreaction which cleaves the C17-C20 bond of the steroid yielding the andro-derivative, a second product comes from a Yang-type photorearrangement which links C18 to C20 yielding a cyclobutane adduct.

Effect of sugar cane policosanol on lipid profile in primary hypercholesterolemia.

Policosanol, a mixture of long-chain aliphatic primary alcohols, is used as a cholesterol-lowering supplement. The effectiveness of policosanol is still questionable. To determine the lipoprotein-lowering effects of Cuban sugar cane-derived policosanol a double-blind, randomized, placebo controlled trial was performed.

Steroidal glycosides from Hoodia gordonii.

Ten new C21-steroidal derivatives, namely gordonosides A-L (1-10) were isolated from a chloroform extract of the aerial parts of Hoodia gordonii, a plant widely used in the nutraceutical market as an ingredient of weight loss supplements. Compounds (2-10) are based on 3beta,14beta-dihydroxy-pregn-5-en-17-betaone aglycone (1). Their structures were characterized on the basis of HR-MS spectrometry and both 1D and 2D NMR techniques.

Analgesic and antiinflammatory activity of Cyclamen repandum S. et S.

According to folk medicine some species belonging to the genus Cyclamen were used for their biological activities. Early investigation of the different species of the genus resulted in the isolation of triterpenic saponins. No phytochemical and biological data are available on C.

Polyphenols from Polygala spp. and their antioxidant activity.

Members of Polygalaceae are known to contain a variety of different polyphenolic compounds such as xanthones, flavonoids, and biphenyl derivatives. Here, we report the isolation and structural characterization of two new phenol derivatives, named alpestrin (= 3,3',5'-trimethoxy[1,1'-biphenyl]-4-ol; 10) and alpestriose A (= 6-O-benzoyl-1-O-{6-O-acetyl-3-O-[(4-hydroxy-3,5-dimethoxyphenyl)prop-2-enoyl]-beta-D-fructofuranosyl}-alpha-D-glucopyranoside; 11), and of four known compounds (12-15) from the MeOH extract of Polygala alpestris. The relative in vitro antioxidant activities of these compounds, in comparison with other phenolic substances from Polygala vulgaris, were evaluated by means of the Briggs-Rauscher (BR) oscillating reaction, a method based on the inhibitory effects of antioxidant free-radical scavengers.

Deoxypodophyllotoxin content and antioxidant activity of aerial parts of Anthriscus sylvestris Hoffm.

Deoxypodophyllotoxin content of the aerial parts of Anthriscus sylvestris Hoffm. growing at different altitudes was evaluated in comparison to the roots. The lignan accumulation in ground parts was at least double compared to aerial ones.