Sinteza i spektroskopska analiza 5beta-kolan derivata

The facile synthesis and spectroscopic data analyses of three 5beta-cholane derivatives, 3beta-tosyloxy-5beta-cholan-24-ol (3), 5beta-cholan-24-ol (4) and 5eta-cholan-24-yl tosylate (5), have been described.Opisana je jednostavna sinteza i spektroskopska analiza tri derivata 5beta-kolana, 3beta-tosiloksi-5beta-kolan-24-ol (3), 5beta-kolan-24-ol (4) i 5beta-kolan-24-il tosilat (5)

Sinteza i spektroskopska analiza 5beta-kolan derivata

The facile synthesis and spectroscopic data analyses of three 5beta-cholane derivatives, 3beta-tosyloxy-5beta-cholan-24-ol (3), 5beta-cholan-24-ol (4) and 5eta-cholan-24-yl tosylate (5), have been described.Opisana je jednostavna sinteza i spektroskopska analiza tri derivata 5beta-kolana, 3beta-tosiloksi-5beta-kolan-24-ol (3), 5beta-kolan-24-ol (4) i 5beta-kolan-24-il tosilat (5)

In-vitro antioxidant activities of the fruits peel of citrus macroptera Mont. Var. Annamensis

In-vitro antioxidant activities of the fruit peels of Citrus macroptera were studied in the present work. Ferric reducing antioxidant power (FRAP) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assays were performed to evaluate the antioxidant properties of the fractions from n-hexane and methanol crude extracts from the fruit peels of this plant. Results suggested that all fractions from methanol crude extract showed good antioxidant activities. Meanwhile, all fractions from n-hexane extract exhibited as weak antioxidant properties. The results were comparable with standard ascorbic acid. The potency of antioxidant activities of the fruits peel of C. macroptera depends on the type of extracts

Derivati feniloctene kiseline s antioksidativnim učinkom iz sjemenki biljke Ilex aquifolium

Reversed-phase preparative HPLC analysis of the methanol extract of the seeds of Ilex aquifolium afforded two antioxidant phenylacetic acid derivatives, 2,4-dihydroxyphenylacetic acid (1) and 2,4-dihydroxyphenylacetic acid methyl ester (2). The structures were determined by spectroscopic methods. In the DPPH assay for antioxidant activity, the IC50 values of 1 and 2 were 1.50 x 10-3 and 2.55 x 10-3 mg mL-1, respectively, compared to 2.88 x 10-5 mg mL-1 of quercetin, a natural antioxidant.Reverzno-faznom preparativnom HPLC analizom metanolnog ekstrakta sjemenki biljke Ilex aquifolium izolirana su dva derivata feniloctene kiseline s antioksidativnim učinkom, 2,4-dihidroksifeniloctena kisleina (1) i metilni ester 2,4-dihidroksifeniloctene kiseline (2). Njihove strukture određene su spektroskopskim metodama. U DPPH testu na antioksidativno djelovanje, IC50 vrijednosti spojeva 1 i 2 bile su 1.50 x 10-3 i 2.55 x 10-3 mg mL-1, dok je IC50 prirodnog antioksidansa kvercitina bila 2.88 x 10-5 mg mL-1

Derivati feniloctene kiseline s antioksidativnim učinkom iz sjemenki biljke Ilex aquifolium

Reversed-phase preparative HPLC analysis of the methanol extract of the seeds of Ilex aquifolium afforded two antioxidant phenylacetic acid derivatives, 2,4-dihydroxyphenylacetic acid (1) and 2,4-dihydroxyphenylacetic acid methyl ester (2). The structures were determined by spectroscopic methods. In the DPPH assay for antioxidant activity, the IC50 values of 1 and 2 were 1.50 x 10-3 and 2.55 x 10-3 mg mL-1, respectively, compared to 2.88 x 10-5 mg mL-1 of quercetin, a natural antioxidant.Reverzno-faznom preparativnom HPLC analizom metanolnog ekstrakta sjemenki biljke Ilex aquifolium izolirana su dva derivata feniloctene kiseline s antioksidativnim učinkom, 2,4-dihidroksifeniloctena kisleina (1) i metilni ester 2,4-dihidroksifeniloctene kiseline (2). Njihove strukture određene su spektroskopskim metodama. U DPPH testu na antioksidativno djelovanje, IC50 vrijednosti spojeva 1 i 2 bile su 1.50 x 10-3 i 2.55 x 10-3 mg mL-1, dok je IC50 prirodnog antioksidansa kvercitina bila 2.88 x 10-5 mg mL-1

DICHLOROMETHANE EXTRACT OF THE LEAVES OF ARBUTUS PAVARII PAMP. EXHIBITS CYTOTOXICITY AGAINST THE PROSTATE CANCER CELL LINE PC3: A BIOASSAY-GUIDED ISOLATION AND IDENTIFICATION OF ARBUTIN AND BETULINIC ACID METHYL ESTER

Background: Arbutus pavarii Pamp. (fam. Ericaceae), commonly known as “Shmeri”, “Shmar” and “Libyan Strawberry”, is an endemic Libyan medicinal plant, growing almost exclusively in the Al-Jabel Al-Akhdar mountainous region in Libya. Aims: To assess the cytotoxicity of A. pavarii against human cancer cell lines and to carry out bioassay-guided isolation and identification of compounds. Materials and Methods: Shed-dried and ground leaves of A. pavarii were Soxhlet-extracted, successively, with n-hexane, dichloromethane (DCM) and methanol (MeOH), and assessed for cytotoxicity against several human cancer cell lines using the MTT assay. The cytotoxicity of the DCM extract against the normal human prostate cell line PNT2 was also assessed to determine the selectivity index (SI). The DCM extract was subjected to vacuum liquid chromatography (VLC) to produce eight fractions. A reversed-phase preparative HPLC analysis of the active VLC fraction was carried out to purify the major compounds present in the active fraction, and the structures of the compounds were elucidated by spectroscopic means. Results: The DCM extract was more cytotoxic against the PC3 cell line (IC50= 26 mg/mL) but less to the normal human prostate cell line PNT2 (IC50 = 90 mg/mL) with a selectivity index of 3.5. VLC analysis produced 8 fractions, with fraction VLC-5 most active against PC3 cells. Prep-HPLC-based purification of VLC-5 afforded the isolation of arbutin (1) and betulinic acid methyl ester (2), the structures of which were elucidated by spectroscopic means. Conclusion: The DCM extract of the leaves of A. pavarii exhibited significant cytotoxicity to PC3 cells, but much less cytotoxicity against normal human prostate cell line. The isolated compounds from the active fraction, arbutin (1) and betulinic acid methyl ester (2), which were previously shown to possess cytotoxic properties, could be responsible for the cytotoxicity of the DCM extract

Naturally Occurring Calanolides: Occurrence, Biosynthesis, and Pharmacological Properties Including Therapeutic Potential.

Calanolides are tetracyclic 4-substituted dipyranocoumarins. Calanolide A, isolated from the leaves and twigs of Calophyllum lanigerum var. austrocoriaceum (Whitmore) P. F. Stevens, is the first member of this group of compounds with anti-HIV-1 activity mediated by reverse transcriptase inhibition. Calanolides are classified pharmacologically as non-nucleoside reverse transcriptase inhibitors (NNRTI). There are at least 15 naturally occurring calanolides distributed mainly within the genus Calophyllum, but some of them are also present in the genus Clausena. Besides significant anti-HIV properties, which have been exploited towards potential development of new NNRTIs for anti-HIV therapy, calanolides have also been found to possess anticancer, antimicrobial and antiparasitic potential. This review article provides a comprehensive update on all aspects of naturally occurring calanolides, including their chemistry, natural occurrence, biosynthesis, pharmacological and toxicological aspects including mechanism of action and structure activity relationships, pharmacokinetics, therapeutic potentials and available patents

2D NMR spektroskopske analize arhangelicina iz sjemenki biljke Angelica archangelica

A total of six coumarins, bergapten (1), xanthotoxin (2), imperatorin (3), isoimperatorin (4), phellopterin (5) and archangelicin (6), have been isolated from an n-hexane extract of the seeds of Angelica archangelica. The results of comprehensive 2D NMR analyses of archangelicin are discussed.Iz n-heksanskog ekstrakta sjemenki biljke Angelica archangelica izolirano je šest kumarina, bergapten (1), ksantotoksin (2), imperatorin (3), izoimperatorin (4), felopterin (5) i arhangelicin (6). U radu su detaljno analizirani 2D NMR spektri arhangelicina