Nematicidal constituents of the aerial parts of Lantana camara.

Two new constituents, lantanoside (1) and lantanone (2), and the known compounds linaroside (3) and camarinic acid (4) were isolated from the aerial parts of Lantana camara. Compounds 1, 3, and 4 were tested for nematicidal activity against root-knot nematode Meloidogyne incognita and showed 90, 85, and 100% mortality, respectively, at 1.0% concentration.

Two insecticidal tetranortriterpenoids from Azadirachta indica.

Two new triterpenoids, 6 alpha-O-acetyl-7-deacetylnimocinol [24,25,26,27-tetra-norapotirucalla-(apoeupha)-6 alpha-acetoxy-7 alpha-hydroxy-1,14,20,22-tetraen-21,23-epoxy-3-one] (1) and meliacinol [24,25,26,27-tetranorapotirucalla-(apoeupha)-1 alpha-trimethylacryloxy-21,23-6 alpha,28-diepoxy-16-oxo-17-oxa-14,20,22-trien-3 alpha,7 alpha-diol] (2) were isolated from the methanolic extract of the fresh leaves of Azadirachta indica (neem). Their structures have been elucidated through spectral studies, including 2D-NMR (COSY-45, NOESY, HMQC and HMBC). The bioactivity of these as well as of nimocinol, reported earlier from the same source, is reported.

Potential mechanisms for failure to eradicate group A streptococci from the pharynx.

Objective: To investigate the relative efficacy of orally administered cefadroxil and penicillin V in the treatment of group A streptococcal (GABHS) pharyngitis and the mechanism(s) responsible for failure of antimicrobial therapy to eradicate GABHS from the pharynx.

Study Design: A prospective, randomized clinical trial was conducted in four pediatric offices in which 462 patients with acute pharyngitis and positive culture for GABHS were randomly assigned to receive cefadroxil (n = 232) or penicillin V (n = 230).

Results: Bacteriologic treatment success rates for patients in cefadroxil and penicillin groups were 94% and 86%, respectively.

Triterpenoids of the fruit coats of azadirachta indica.

Three new triterpenoids, azadironolide [24,25,26, 27-tetranorapoeupha-7alpha-acetoxy-23xi-hydroxy-21,23-epoxy-1,14, 20(22)-trien-3,21-dione] (1), isoazadironolide [24,25,26, 27-tetranorapoeupha-7alpha-acetoxy-21xi-hydroxy-21,23-epoxy-1,14, 20(22)-trien-3,23-dione] (2), and azadiradionolide [24,25,26, 27-tetranorapoeupha-7alpha-acetoxy-21,23-epoxy-1,14,20(22)-trien-3, 16,21-trione] (3), were isolated from the fresh fruit coats of Azadirachta indica. Their structures have been elucidated through spectral analysis.

Bio-active cardenolides from the leaves of Nerium oleander.

A bioactivity directed isolation of the methanolic extract of the fresh, uncrushed leaves of Nerium oleander showing a central nervous system (CNS) depressant effect in mice has been undertaken. As a result, four CNS depressant cardenolides including a new cardenolide, neridiginoside and three known constituents, nerizoside, neritaloside and odoroside-H, have been isolated which exhibited CNS depressant activity in mice at a dose of 25 mg/kg. The structure of neridiginoside was elucidated as 3 beta-O-(D-diginosyl)-5 beta, 14 beta-dihydroxy-card-20(22)-enolide, using spectroscopic methods including one-dimensional and two-dimensional NMR (COSY-45, NOESY, J-resolved, HMQC and HMBC).

Hypotensive constituents from the pods of Moringa oleifera.

Hypotensive activity of the ethanolic and aqueous extracts of Moringa oleifera whole pods and their parts, namely, coat, pulp, and seed was investigated. The activity of the ethanolic extract of both the pods and the seeds was equivalent at the dose of 30 mg/kg. The ethyl acetate phase of the ethanolic extract of pods was found to be the most potent fraction at the same dose.

Acetates and benzoates of alkyl catechols and evaluation of their antibacterial activity.

Potential biologically active alkyl catechol esters were prepared and their antibacterial activity was determined against 12 Gram-positive and 16 Gram-negative bacteria. Esterification (acetylation and benzoylation) of mono-, di- and tetra- substituted alkyl catechols afforded the di-acetyl and di-benzoyl derivatives in each case. In the primary screening it was observed that the substitution of hydroxyl group in alkyl catechol with an acyl group generally resulted in a decrease of antibacterial activity.

Cardenolides from the methanolic extract of Nerium oleander leaves possessing central nervous system depressant activity in mice.

Two new cardenolides, 3 beta-O-(D-2-O-methyldigitalosyl)-14 beta-hydroxy-5 beta-carda-16,20(22)-dienolide (1) and 3 beta-hydroxy-8,14-epoxy-5 beta-carda-16,20(22)-dienolide (2), and two known cardenolides, 3 beta-O-(D-digitalosyl)-14 beta-hydroxy-16 beta-acetoxy-5 beta-card-20(22)-enolide (3) and 3 beta-O-(D-digitalosyl)-14 beta-hydroxy-5 beta-card-20(22)-enolide (4), have been isolated from the leaves of Nerium oleander following a bioactivity-directed isolation of the MeOH extract, which showed central nervous system (CNS) depressant activity in mice at a dosage of 50 mg/kg i.p. Their structures were established on the basis of chemical and spectral data.

Chemistry and biological activity of a tryptamine and beta-carboline series of bases.

Twenty-six derivatives of harmaline and tetrahydroharmine were prepared and characterized by UV, IR, MS, and NMR spectroscopy. They were tested for their antimicrobial, antiplatelet aggregation and cytotoxic activity. Their effect on central nervous system was also studied.

Studies on the constituents of the leaves of Nerium oleander on behavior pattern in mice.

Fresh, undried and uncrushed leaves of Nerium oleander were subjected to methanol extraction and bioassay directed fractionation. This led to the isolation of two purified fractions namely, B-1 and B-3. Fractions B-1 and B-3 were studied with respect to their actions on the central nervous system and behavior pattern in mice.

Adsorption studies and the removal of dissolved metals using pyrolusite as adsorbent.

The adsorption of metals from aqueous solutions of Pb(2+), Zn(2+) and Mg(2+) on naturally occurring pyrolusite have been studied. The chemical stability of the pyrolusite has been determined in NaOH, H2SO4, HNO3, HCl, NaCl and NK4Cl solutions of various concentrations. Adsorption of the metal ions followed the order Pb(2+)>Zn(2+)>Cd(2+).

Fully acetylated carbamate and hypotensive thiocarbamate glycosides from Moringa oleifera.

Six new and three synthetically known glycosides have been isolated from the leaves of Moringa oleifera, employing a bioassay-directed isolation method on the ethanolic extract. Most of these compounds, bearing thiocarbamate, carbamate or nitrile groups, are fully acetylated glycosides, which are very rare in nature. Elucidation of the structures was made using chemical and spectroscopic methods, including 2D NMR techniques.

Isolation and structure elucidation of new nitrile and mustard oil glycosides from Moringa oleifera and their effect on blood pressure.

Bioassay-guided analysis of an EtOH extract of Moringa oleifera leaves showing hypotensive activity led to the isolation of two nitrile glycosides, niazirin [1] and niazirinin [2], and three mustard oil glycosides, 4-[(4'-O-acetyl-alpha-L-rhamnosyloxy)benzyl]isothiocyanate [4], niaziminin A, and niaziminin B. Glycoside 2 is a new compound. Niaziminins A and B have previously been obtained from the left extract as a mixture, while compound 4 is new from this source.

In vitro studies of the antibacterial and antifungal activity of oxine and its derivatives.

Twenty-one derivatives of 8-hydroxyquinoline (oxine, 8H, CAS 148-24-3) were prepared and characterized by UV, IR, MS and NMR spectroscopy. Four of these derivatives, N-butyl, 8-butyloxyquinolinium bromide (HBD), 8-pentyloxyquinoline (HPEM), N-pentyl, 8-pentyloxyquinolinium bromide (HPED) and N-benzyl, 8-benzyloxy quinolinium chloride (HBED) are new and reported for the first time. The antimicrobial activity of these compounds was carried out in vitro against 11 Gram positive and 18 Gram negative bacteria, and 18 fungi including 9 dermatophytes, 7 other filamentous fungi and 2 Candida species.

Synthesis of alkyl catechols and evaluation of their antibacterial and cyfotoxic activity.

A series of potential biologically active mono-, di- and tetra- alkyl catechols were prepared through Friedel- Crafts alkylation of catechol, and evaluated for their antibacterial and cytotoxic activity. The mono-substituted alkyl derivatives showed maximum antibacterial activity in vitro which increased with the increasing length of the alkyl chains. Primary screening results indicated that all the monoalkyl derivatives except 4- (2-octyl) catechol inhibited the growth of B.

Constituents of Azadirachta indica: isolation and structure elucidation of a new antibacterial tetranortriterpenoid, mahmoodin, and a new protolimonoid, naheedin.

Mahmoodin [1], a new limonoid, has been isolated from Azadirachta indica (neem) oil, along with seven known tetranortriterpenoids, azadirone, epoxyazadiradione, nimbin, gedunin, azadiradione, deacetylnimbin, and 17-hydroxyazadiradione. A new protolimonoid, naheedin [3], has been obtained from the neem fruits along with azadirachtol. Their structures have been elucidated through chemical and spectral analyses including 2D nmr studies.

Expression of native and deglycosylated colon cancer mucin antigens in normal and malignant epithelial tissues.

Immunohistochemical techniques were used to determine the distribution and cellular location of the mature and precursor forms of a colonic-type mucin in normal and malignant epithelial tissues. The antisera used in this study were prepared against native human colon cancer mucin (LS), partially deglycosylated mucin (HFA or GalNAc-apomucin), and fully deglycosylated mucin (HFB or apomucin). These antisera reacted with most mucin-producing cells of the normal gastrointestinal tract, salivary ductular cells, bronchial epithelial cells, some bronchial mucous glands, and squamous epithelial cells of the esophagus.

Tricyclic Diterpenes from the Stem Bark of Azadirachta indica.

Two new diterpenoids, margosone and margosolone, have been isolated from the stem bark of AZADIRACHTA INDICA A. Juss (neem) and their structures established as 12,13-dihydroxy-14-isoporpylpodocarpa-8,11,13-trien-7-one and 13-hydroxy-12-methoxypodocarpa-8,11,13-trien-7-one, respectively, through chemical and spectroscopic studies.

Deglycosylation of mucin from LS174T colon cancer cells by hydrogen fluoride treatment.

Mucin from xenografts of LS174T human colon cancer cells was treated with anhydrous HF for 1 h at 0 degree C to give a product (HFA) with over 80% of the glucosamine and hexose removed, but retaining some galactosamine, and for 3 h at room temperature to give a product (HFB) devoid of carbohydrate. Rabbit antibodies against HFA bound to HFA much more than to HFB, and bound to native mucin to an intermediate extent. Antibodies to HFB bound to HFB more than to HFA, and did not bind to native mucin.

Kanerocin: A New Triterpene from the Leaves of Nerium oleander.

From the fresh, undried, and uncrushed leaves of NERIUM OLEANDER a new triterpenoid, kanerocin, has been isolated along with known ursolic and oleanolic acids and its structure established through chemical and spectroscopic methods as 3alpha-hydroxy-urs-18,20-dien-28-oic acid.