Muhammad Ali Versiani

Bioassay-guided studies on Bombax ceiba leaf extract: isolation of shamimoside, a new antioxidant xanthone C-glucoside

Bioassay-guided isolation studies on the methanolic extract of the leaves of Bombax ceiba employing DPPH antioxidant assay led to the isolation of a new xanthone C-glucoside, shamimoside (2), along with three known constituents, mangiferin (1), stigma-5-en-3-O-β-glucoside, and β-amyrin. The structure of shamimoside has been elucidated through extensive spectroscopic methods, including 1D and 2D NMR experiments, as 4-C-β-D-glucopyranosyl-1,3,6,8-tetrahydroxy-7-O-(p-hydroxybenzoyl)-9H-xanthen-9-one (2). It is the first naturally occurring xanthone containing a benzoate moiety directly attached to an aromatic ring. Polar extracts and fractions demonstrated better antioxidant activity, and 1 was found to be more potent than 2 in this assay.

New dammarane and ursane-type triterpenoids from the flower of Ixora coccinea Linn.

Two new esters of dammarane triterpenoids ixorene isovalerate (1), ixorene 3′,8′-dimethyloctanoate (2) and a new ursane-type triterpenoids Ixoroid acid (3) were isolated from the methanolic extract of flowers of Ixora coccinea Linn., along with the three known constituents. The structures of compounds 1 and 3 were elucidated on the basis of extensive 1D,2D NMR studies and mass spectrometry as 17β-dammara-12,20-diene-3β-isovelarate and 3β-hydroxy-18β-urs-12ene-29β-oic acid, respectively, whereas 2 was identified as 17β-dammara-12,20-diene-3β-3′,8′-dimethyloctanoate through 1H NMR and mass spectral data. Compounds 1, 2, 4 and 5 were evaluated for their in vitro cytotoxic activity, which exhibited weak activity against the 3T3, PC3 and HeLa cell lines with the IC50 value >30 μM. Antioxidant results of 1 – 5 revealed that only compound 5 showed antioxidant activity in DPPH radical scavenging inhibition with the IC50 1.31 × 10− 6 ± 0.005 μm mL− 1. Both activities are the first records of these isolated compounds from the flowers of Ixora coccinea Linn.

Antibacterial activity of flower of Melia azedarach Linn. and identification of its metabolites

Constituents of eight different extracts and fractions, obtained from flowers of Melia azedarach, were identified by gas chromatography–mass spectrometry and mass spectral library search. Altogether, 38 phytochemicals were identified, all for the first time from the flowers. Only 14 of these were known from parts of M. azedarach other than flowers, while 24 are reported for the first time from any part of the plant. These metabolites included branched and n-hydrocarbons, aromatics, a polyisoprenoid, fatty acids, fatty acid methyl esters, and fatty alcohols, which were found to be different from its essential oil constituents. One major constituent 4-hydroxybenzoic acid (4) was not only identified but also isolated as a pure compound from ethyl acetate extract. Extracts, compound 4 and its derivatives gallic acid and methyl gallate were tested for antimicrobial potential. Gallic acid and methyl gallate exhibited antibacterial activity against Staphylococcus saprophyticus. Methyl gallate also showed some activity against Corynebacterium diphtheriae and Corynebacterium. hofmannii. Among the extracts, only methanol extract exhibited activity against Pseudomonas sp. The extracts only inhibited the growth of dermatophytic fungi.

Loasins A and B, new flavonoids from Eremostachys loasifolia.

Loasins A (1) and B (2), new flavonoids, have been isolated from the ethyl acetate soluble sub-fraction of the ethanolic extract of Eremostachys loasifolia along with apuleisin (3) and apuleidin (4), isolated for the first time from this species. Their structures were assigned on the basis of their spectral data including 1D and 2D NMR.

Synthesis, Spectroscopic Characterization and Antimicrobial Activities of Benzoxazolone Derivatives

: Background: Pathogenic microbial diseases are now the key virulence in our daily life. Significant research has been carried out in order to trigger the bacterial infections. Amongst the organic molecules, oxazolone and derivatives were found to have excellent bioactivities including antimicrobial activities. METHODS By keeping in mind the considerable antimicrobial activities of class benzoxazolones, a series of benzoxazolone derivatives 3-16 have been synthesized. Out of which five compounds 10, 11, 14, 15, and 16 were new synthetic derivatives whereas compounds 9, 12, and 13 were already known compounds. These compounds have been synthesized by refluxing of amino phenol and 1,1-carbonyldiimidazole1 (C3H3N2)2CO) (CDI) in a dry THF and then treated with commercially available acid chloride. The structures of the compounds were elucidated on the basis of 1H-NMR, EIMS and elemental analysis. All the compounds were screened for their antibacterial activities and tested by agar well diffusion method. RESULTS Compounds 14 and 16 showed good activity against S. aureus. Compound 5 showed good while 14 and 16 were found to be most active against E. coli using cefuroxime as a standard. Antifungal activities were carried out by using standard drug nystatin and compounds 4, 5, 9, 11 and compound 12 were found to be active against C. albicans. Compounds 4, 5, 9 and compound 10 showed good while 7, 11, and compound 13 showed excellent activities against Chrysosporium sp. Compounds 6, 7 and compound 12 were found to be most active against A niger and A. flavus, respectively. CONCLUSION A number of derivatives were identified to have potent antimicrobial activities and may serve as lead compounds for future research.

Cytotoxic Cardiac Glycoside from the Parasitic Plant Cuscuta reflexa

Bioassay guided fractionation of the cytotoxic extract of the plant Cuscuta reflexa, employing cytotoxic assay against a panel of 60 cell lines, led to the isolation of 13 compounds identified as odoroside H (1), 21-hydroxyodoroside H (2), neritaloside (3), strospeside (4), 16-β-hydroxydigitoxin (5), N-trans and cis feruloyl tyramines (6 and 7), ethyl caffeate (8), coumarins (9 and 10), ursolic acid (11), β-sitosterol glucoside (12), and 4-O-p-coumaroyl-β-D-glucoside (13). Compound 2 was found to be a new natural product while 1, 3, 4, 5, 6, 7, 10, and 11 are known compounds isolated from this source for the first time. Compounds 1, 3, and 4 possessed very good cytotoxic activity against renal and prostate cancer cell lines. Of these compounds, 1 showed a positive hollow fiber test and was selected for in vivo xenograft testing. The structures of compounds 1–5 have been established through chemical and spectral studies including UV, IR, mass, NMR (1H and 13C), and 2D NMR (COSY-45°, NOESY, HMQC, HMBC, and J-resolved) experiments.

Host-Plant Effect on the Chemical Constituents of Cuscuta reflexa

0009-3130/17/5303-054

Chemical Constituents and Biological Activities of Adenium obesum (Forsk.) Roem. et Schult.

Contents1. Introduction2. Chemical Constituents2.1. Cardiac Glycosides2.2. Pregnanes2.3. Triterpenes2.4. Flavonoids2.5. Carbohydrate3. Biological Activities of Extracts and Pure Compounds3.1. As Biological Pesticides3.2. Pharmacological Activities3.2.1. Antibacterial Activity3.2.2. Antitumor Activity3.2.3. Antiviral Activity3.2.4. Immunomodulatory Activity3.2.5. Toxicity3.2.6. Other Effects4. Concluding Remarks1. Introduction. – Adenium obesum, which is commonly known as desert rose,belongstothefamilyApocynaceae,andoccursalloverAfricaandcultivatedinAsia.Itisaxerophytewiththickstemandratherfleshyleavesandusedasanornamentalplant.Name of its genus was derived from Aden, the former name of Yemen and nowadaysthecapitaltownofthecountry,whilethetermobesumreferstotheswellingofthestemin its basal parts. The plant has several synonyms such as Nerium obesum Forssk.,A.arabicum Balf.f., and A. tricholepis Chior, and more than one vernacular names like,Ombo gaduud, Obbe, Karya, and Locombolo based on different dialects used in thearea [1–9]. Various parts of A. obesum had long been used as traditional medicines forthe treatment of skin problems, wound, ear ache, rhinitis, skin lumps, gonorrhea, andinfectious diseases. It is also a poisonous and toxic plant, and therefore used as a

In vitro Studies of Interaction Between Dexamethasone and NSAIDS by Using RP-High Performance Liquid Chromatography

Abstract Non-steroidal anti-inflammatory drugs (NSAIDS) are commonly used because of their remarkable cure over mild and moderate pain including osteoarthritis and rheumatoid arthritis. Medical doctors commonly prescribe steroidal drugs in combination with the NSAID’s therefore we have developed a method to evaluate the percent availability of these two classes of drugs and analyzed their possible interactions. The proposed method is validated according to the International Conference on Harmonization (ICH) guide lines on RP-HPLC (Reverse Phase High Performance Liquid Chromatography). A good chromatographic separation was achieved using a mobile phase containing methanol-water (80:20 v/v) at pH = 3.2 with a flow rate of 1.0 mL/min (detection at 265 nm with a UV-vis detector). The in-vitro interaction study was conducted at physiological conditions (i.e. temperature 37°C and stomach pH = 3.2). The method provided a very good percent recovery of different molecules. The percent recovery of Piroxicam, Naproxen sodium, Flurbiprofen and Ibuprofen are 100.539, 100.373, 99.683 and 100.840 respectively. The results indicated that percent availability of all NSAIDs and dexamethasone reduced during the time interval 2.5 h which is likely due to the formation of charge transfer complexes. We can conclude that simultaneous administration of these drugs may alter their bio-availability.

Cytotoxic cardiac glycosides from the fruit (pods) of Adenium obesum (Forssk.) Roem. & Schult

Abstract Phytochemical investigation of methanolic extract of Adenium obesum led to the isolation of 42 (1–42) compounds belongs to cardiac glycosides, triterpenoids and steroids. The chemical structures of isolated compounds were elucidated by spectral techniques UV, IR, NMR and FAB MS. The cardiac glycosides were tested against three human cell lines, 3T3 (normal cells), HeLa (Human cervical cancer cell lines) and PC-3 (Human prostate cancer cell lines). The cardiac glycoside, honghelin (4), obeside B (5) and obeside C (6) showed significant effects against cell lines Hela, 3T3 and PC-3 compared to standard drug doxorubicin. Compounds 4, 5 and 6 exhibited very low IC50 (μM) against the PC3 human cell line. 4 and 6 also showed least IC50 against the HeLa human cell lines as compared to the standard drug doxorubicin whereas these three compounds showed effect on 3T3 cell line with high IC50 values compared to drug cycloheximide.