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PubMed2005

Antileishmanial and trypanocidal activity of Brazilian Cerrado plants.

The side effects and the emerging resistance to the available drugs against leishmaniasis and trypanosomiasis led to the urgent need for new therapeutic agents against these diseases. Thirty one extracts of thirteen medicinal plants from the Brazilian Cerrado were therefore evaluated in vitro for their antiprotozoal activity against promastigotes of Leishmania donovani, and amastigotes of Trypanosoma cruzi. Among the selected plants, Casearia sylvestris var. lingua was the most active against both L. donovani and T. cruzi. Fifteen extracts were active against promastigotes of L. donovani with concentrations inhibiting 50% of parasite growth (IC50) between 0.1-10 microg/ml, particularly those of Annona crassiflora (Annonaceae), Himatanthus obovatus (Apocynaceae), Guarea kunthiana (Meliaceae), Cupania vernalis (Sapindaceae), and Serjania lethalis (Sapindaceae). With regard to amastigotes of T. cruzi, extracts of A. crassiflora, Duguetia furfuracea (Annonaceae), and C. sylvestris var. lingua were active with IC50 values between 0.3-10 microg/ml. Bioassay fractionations of the more active extracts are under progress to identify the active antiparasite compounds.

Animals↗
PubMed2006

Micropropagation: a tool for the production of high quality plant-based medicines.

Medicinal plants are the most important source of life saving drugs for the majority of the world's population. The biotechnological tools are important to select, multiply and conserve the critical genotypes of medicinal plants. Plant tissue culture techniques offer an integrated approach for the production of standardized quality phytopharmaceutical through mass-production of consistent plant material for physiological characterization and analysis of active ingredients. Micropropagation protocols for cloning of some medicinal plants such as Catharanthus roseus (Apocynaceae), Chlorophytum borivilianum (Liliaceae), Datura metel (Solanaceae), and Bacopa monnieri (Scrophulariaceae) have been developed. Regeneration occurred via organogenesis and embryogenesis in response to auxins and cytokinins. The integrated approaches of our culture systems will provide the basis for the future development of novel, safe, effective, and high-quality products for consumers.

Biotechnology↗
PubMed1998

Evaluation of the antioxidant potential of natural products.

Since reactive oxygen radicals play an important role in carcinogenesis and other human disease states, antioxidants present in consumable fruits, vegetables, and beverages have received considerable attention as cancer chemopreventive agents. Thus, in order to identify antioxidants in plant extracts, test materials were assessed for potential to scavenge stable 1,2-diphenyl-2-picrylhydrazyl (DPPH) free radicals, reduce TPA-induced free radical formation in cultured HL-60 human leukemia cells, and inhibit responses observed with a xanthine/xanthine oxidase assay system. Approximately 700 plant extracts were evaluated, and 28 were found to be active in the DPPH free radical scavenging assay. Based on secondary analyses performed to assess inhibition of 7,12-dimethylbenz(a)anthracene-induced preneoplastic lesion formation with a mouse mammary organ culture model, Chorizanthe diffusa Benth. (Polygonaceae), Mezoneuron cucullatum Roxb. (Leguminosae), Cerbera manghas L. (Apocynaceae) and Daphniphyllum calycinum Benth. (Daphniphyllaceae) were selected and subjected to bioassay-guided fractionation. 5,7,3',5'-Tetrahydroxy-8,4'-dimethoxyflavonol, 5,8,4'-trihydroxy-7,3'-dimethoxyflavonol, 5,3',4'-trihydroxy-7-methoxyflavonol, and 6,3',4'-trihydroxy-7-methoxyflavonol were identified as active principles from C. diffusa. Piceatannol, trans-resveratrol, apigenin and scirpusin A were found as the active principles of M. cucullatum, olivil, (-)-carinol, and (+)-cycloolivil were active principles from C. manghas, and 5,6,7,4'-tetrahydroxyflavone 3-O-rutinoside and kaempferol 3-O-neohesperidoside were active principles from D. calycinum. Of these substances, the hydroxystilbenes piceatannol and transresveratrol have thus far been shown to inhibit carcinogen-induced preneoplastic lesion formation in the mouse mammary gland organ culture model.

Animals↗
PubMedDate not supplied

Cardenolides of Trachomitum sarmatiense Woodson.

From the roots of Trachomitum sarmatiense Woodson (Apocynaceae) 5 cardial glycosides were isolated. Among them 4 substances were identified: cymarin and k-strophanthin-beta, and two derivatives of cannogen: apocannosid and apobiosid. In the overground part of the plant, the cardenolides were not found.

Cardanolides↗
PubMed2001

[Diversity and selectivity in biomolecules].

Nature provides molecular constructions in inexhaustible richness. She combines small building blocksacks, and from the great variety of the possible structures, the really existing molecules are selected by kinetic (actually enzymic) and thermodynamic control. The operation of this fundamental principle is demonstrated by means of the graph analysis, in the large community of the monoterpenoid indole alkaloids isolated from the species of the Apocynaceae, Loganiaceae and Rubiaceae plant families. Strictosidine, an alkaloid glucoside, is formed from a single enantiomer of secologanin and tryptamine by enzymic catalysis and with complete diastereoselectivity. It is the exclusive precursor of more than 2200 alkaloids. The configuration of one or more analogous centers of chirality of them is identical, i.e. homochiral, insofar it will be lost or changed in subsequent reactions. Strictosidine exists in a single, most stable conformer of the possible 324 ones. On simple secologanin derivatives it was proved, that the removal of the glucosyl unit by enzyme results, under kinetic control, in the formation of the epimer pair of the primary aglucone. However, proton catalysed hydrolysis gives, under thermodynamic control, the most stable epimer pair of the possible 48 aglucones formed in 368 elementary steps. In the deglucosylation of the strictosidine type compounds, in 2 series, 1 tricyclic, 8 tetracyclic and 16 pentacyclic aglucone types are formed by further oxa-, carba- and/or azacyclizations. The alkaloids derived from strictosidine can be grouped into one unrearranged (I) and two rearranged (II and III) skeletons, in normal and iso series as well as along a and b lines. The processes are directed partially by proton migrations. The really existing alkaloids are formed in subsequent chemical reactions. The rich molecular library obtained by that way reveals the fundamental unity of Nature in the material multiplicity, i.e. it lets shine up the beauty in the world of the biomolecules, too.

Alkaloids↗
PubMed1993

Biosynthesis of car1ssol and carissic Acid.

Carissa carandas belongs to family apocynaceae which consists of 300 genera and 1000 species. It is a large shrub with simple thorn and commonly cultivated throughout Pakistan for hedges and is called "Kakronda". The different parts of this plant have been used for various systems of medicine (Kirtikar et al., 1993). Cardiotonic activity was found in root of this plant (Rastogi et al., 1966; Rastogi et al., 1967; Vohra et al., 1963). This plant has been mentioned in the old chemical literature as purgative, stomachic, antihelmintics and antidote for snake-bite (Kirtikar., 1933). The physical characteristics of oil from the fruits of Carissa carandas were determined by using standard methods. In addition to this a study of sugars and amino acids from the fruits of this plant was also undertaken by the present authors (Naim et al., 1986). Our studies in the chemical investigation on this plant had led to the isolation of two new triterpene carissol Ia (Naim et al., 1985) and carissic acid lb (Naim et al., 1988).

Journal Article↗
PubMed2006

In vitro prostate cancer cell growth inhibition by Brazilian plant extracts.

In the present study, 1220 plant extracts obtained from 352 plants belonging to 73 families that grow in the Amazon and Atlantic rain forests were screened for cytotoxicity against PC-3 prostate cancer cell lines. Extracts were tested in the single dose of 100 microg/mL. Activity was observed in 17 aqueous or organic extracts belonging to Annonaceae, Apocynaceae, Araceae, Capparaceae, Commelinaceae, Flacourtiaceae, Lecythidaceae, Leguminosae, Passifloraceae, Rutaceae, and Violaceae.

Antineoplastic Agents, Phytogenic↗
PubMed1991

[Study on glycosidal constituents from Epigynum auritum].

A known compound and a new glycoside, epigeoside, were isolated from the rhizomes of Epigynum auritum (Schneid.) Tsiang et P. T. Li (Apocynaceae). The structure of known compound was identified as daucosterol (beta-sitosterol-beta-D-glucopyranoside). The structure of epigeoside has been deduced on the basis of spectral analysis and chemical reactions as catechin-3-O-alpha-L-rhamnopyranosyl-(1----4)-beta-D-glucopyranosyl-(1-- --6) -beta-D-glucopyranoside. Partial hydrolysis of II with 0.2 mol/L HCl afforded compound IIa and rhamnose. Acid hydrolysis of IIa with 2 mol/L HCl afforded an aglycone which was identified by comparison with catechin, and glucose.

Antineoplastic Agents, Phytogenic↗
PubMedDate not supplied

Inotropic effects of tanghinin and acetyl-tanghinin on guinea-pig isolated papillary muscle.

Tanghinin and its acetylated derivative acetyl-tanghinin are two cardiotonic glycosides isolated from the seed of Tanghinia venenifera Poir. (Apocynaceae). In vitro, these two heterosides increase the contractile force of the guinea-pig papillary muscle. At an extracellular concentration of 1.2 mM of CaCl2, a concentration of 2.8 x 10(-6) M of tanghinin or acetyl-tanghinin increased muscle tension with 1.3 g and 1.5 g, respectively. In presence of an extracellular concentration of 2.4 mM of CaCl2, maximal effects--1.8 g for tanghinin and 2.2 g for acetyl-tanghinin--were obtained with a glycoside concentration of 2.4 x 10(-6) M. These maximal effects are sustained up to a concentration of 2.8 x 10(-6) M. At higher concentrations, the positive inotropic effect drops rapidly, followed by a rise in diastolic tension.

Animals↗
PubMedDate not supplied

[Preparation and evaluation of antibacterial activity of partial fractions of Vallesia antillana Wood].

A study on the antibacterial properties of alkaloidal fractions of Vallesia antillana Wood, a Cuban plant belonging to the Apocynaceae family, is performed for the first time. Four partial fractions from bark of stems were prepared according to a classical extraction of total alkaloids and a partial fractionation of these, with the use of tartaric acid and ethyl ether and by a pH gradient with values of 2.5, 5.0, 7.0 and alkaline one. Data from thin layer chromatography on the alkaloidal content of different fractions are added and an assessment of antibacterial activity was made; for this, a method of sections in agar medium with bacterial species of human clinical interest was used; inhibitory halos found within 24 hours of incubation at 37 degrees C are reported in millimeters.

Alkaloids↗
PubMedDate not supplied

[Evaluation of antimicrobial activity of indol alkaloids].

In pursuing the study of the antimicrobial properties of alkaloids prepared from Cuban plants the activity of 10 indol alkaloids and 4 semisynthetic variables obtained from three plants--Catharanthus roseus G. Don., Vallesia antillana Wood and Ervatamia coronaria Staph, of the family Apocynaceae--growing in Cuba was assessed in vitro. The alkaloids and the variables used were catharantine, vindoline, vindolinine, perivine, reserpine, tabernaemontanine, tetrahydroalstonine, aparicine, vindolinic acid, reserpic acid and vindolininol. These were faced to 40 bacterial strains from the genera Salmonella, Shigella, Proteus, Escherichia, Pseudomonas, Staphylococcus and Corynebacterium as well as to fungi and yeasts from the genera Aspergillus, kCunnighamella, kCandida and Saccharomyces. The method involving cylindric sections in a double agar layer was applied and lectures were obtained at 24-48 hours of incubation at 25 degrees C for fungi and yeasts and 37 degrees C for bacteria. Inhibition zones are reported in millimeters.

Alkaloids↗
PubMed1997

[Host plants of Cerambycidae (Coleoptera) in the northeast of Argentina].

New host plants and localities are recorded for 84 species of Cerambycidae of Chaco Province (Chaquenian Dominion) and Paranaense Province (Amazonian Dominion) in northeastern Argentina and Brazil. Host plants belong to Anacardiaceae, Asclepiadaceae, Apocynaceae, Bignoniaceae, Bombacaceae, Cactaceae, Caesalpinaceae, Capparidaceae, Casuarinaceae, Fabaceae, Mimosaceae, Moraceae, Nyctaginaceae, Polygonaceae, Rhamnaceae, Rutaceae, Sapindaceae, Sapotaceae and Ulmaceae. First records for Argentina and host plants: Compsocerus barbicornis Serville 1834, Desmiphora lenkoi (Lane 1959), Neocompsa serrana (Martins 1962) and Trachysomus dromedarius (Voet 1778). First host plants records of rare or uncommon Argentine species of Cerambycidae are Methia tubuliventris Gounelle 1913, Paraleptidea femorata Gounelle 1913 and Oncideres pepotinga Martins 1981.

Animals↗
PubMed1998

Medication development of ibogaine as a pharmacotherapy for drug dependence.

The potential for deriving new psychotherapeutic medications from natural sources has led to renewal interest in rain forest plants as a source of lead compounds for the development of antiaddiction medications. Ibogaine is an indole alkaloid found in the roots of Tabernanthe iboga (Apocynaceae family), a rain forest shrub that is native to equatorial Africa. Ibogaine is used by indigenous peoples in low doses to combat fatigue, hunger and in higher doses as a sacrament in religious rituals. Members of American and European addict self-help groups have claimed that ibogaine promotes long-term drug abstinence from addictive substances, including psychostimulants and cocaine. Anecdotal reports attest that a single dose of ibogaine eliminates withdrawal symptoms and reduces drug cravings for extended periods of time. The purported antiaddictive properties of ibogaine require rigorous validation in humans. We have initiated a rising tolerance study using single administration to assess the safety of ibogaine for treatment of cocaine dependency. The primary objectives of the study are to determine safety, pharmacokinetics and dose effects, and to identify relevant parameters of efficacy in cocaine-dependent patients. Pharmacokinetic and pharmacodynamic characteristics of ibogaine in humans are assessed by analyzing the concentration-time data of ibogaine and its desmethyl metabolite (noribogaine) from the Phase I trial, and by conducting in vitro experiments to elucidate the specific disposition processes involved in the metabolism of both parent drug and metabolite. The development of clinical safety studies of ibogaine in humans will help to determine whether there is a rationale for conducting efficacy trials in the future.

Animals↗
PubMed2005

Revision of the absolute configuration of plumericin and isoplumericin from Plumeria rubra.

The absolute configurations of plumericin (1) and isoplumericin (2), isolated from Plumeria rubra, were re-assigned based on a combination of X-ray crystal-structure determination and quantum-mechanical calculations of their circular dichroism (CD) spectra. The experimental CD spectra showed an excellent match with those calculated for the (1S,5R,8R,9R,10R) absolute configuration (corresponding to ent-1 and ent-2, resp.), opposite to that generally accepted and published in the literature. Since the (false) plumericin configuration has been often used to derive the absolute configuration of related iridoids by chemical correlation, their absolute configurations also have to be reconsidered.

Apocynaceae↗