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In vitro screening of leishmanicidal activity in myanmar timber extracts.

Seventy-five Myanmar timber extracts belonging to 27 families were examined for their leishmanicidal activities. Some timber extracts had significant leishmanicidal activity, especially extracts of Millettia pendula, which exhibited the most potent activity (MLC 3.1 microg/ml, MIC 1.6 microg/ml). Other timber extracts showing potent activity included those from Cedrela serrata, Cedrela toona, Cordia fragrantissima, Calophyllum kunstleri, Dalbergia cultrate, Grevillea robusta, Haplophragma adenophyllum, Michelia champaca, and Tectona grandis. From a literature search for reports on the chemical constituents of these plants, most constituents were found to be quinone derivatives or other compounds with unsaturated carbonyl groups.

Animals↗

Antioxidant and insect growth regulatory activities of stilbenes and extracts from Yucca periculosa.

The methanol extract from the bark of Yucca periculosa F. Baker afforded 4,4'-dihydroxstilbene, resveratrol and 3,3',5,5'-tetrahydroxy-4-methoxystilbene and had growth regulatory activity against the Fall Army worm (Spodoptera frugiperda J.E. Smith, Lepidoptera:Noctuidae) an insect pest of corn. The most active compound was 3,3',5,5'-tetrahydroxy-4-methoxystilbene which had significant effects at 3 microg/g in diets. In addition to the inhibitory activity on bleaching of crocin induced by alkoxyl radicals, these compounds also demonstrated scavenging properties toward 2,2-diphenyl-1-picrylhydrazyl in TLC autographic and spectrophotometric assays. Our results indicate that these compounds could be involved in interference of sclerotization and moulting. These compounds appear to have selective effects on the pre-emergence metabolism of the insect. The results were fully comparable to known natural insect growth inhibitors such as gedunin and Cedrela extracts and have had a possible role as natural insecticidal agents.

Animals↗

Species and rotation frequency influence soil nitrogen in simplified tropical plant communities.

Among the many factors that potentially influence the rate at which nitrogen (N) becomes available to plants in terrestrial ecosystems are the identity and diversity of species composition, frequency of disturbance or stand turnover, and time. Replicated suites of investigator-designed communities afforded an opportunity to examine the effects of those factors on net N mineralization over a 12-year period. The communities consisted of large-stature perennial plants, comprising three tree species (Hyeronima alchorneoides, Cedrela odorata, and Cordia alliodora), a palm (Euterpe oleracea), and a large, perennial herb (Heliconia imbricata). Trees were grown in monoculture and in combination with the other two life-forms; tree monocultures were subjected to rotations of one or four years, or like the three-life-form systems, left uncut. The work was conducted on fertile soil in the humid lowlands of Costa Rica, a site with few abiotic constraints to plant growth. Rates of net N mineralization and nitrification were high, typically in the range of 0.2-0.8 microg x g(1) x d(-1), with net nitrification slightly higher than net mineralization, indicating preferential uptake of ammonium (NH4+) by plants and microbes. Net rates of N mineralization were about 30% lower in stands of one of the three tree species, Hyeronima, than in stands of the other two. Contrary to expectations, short-rotation management (one or four years) resulted in higher net rates of N mineralization than in uncut stands, whether the latter were composed of a single tree species or a combination of life-forms. Neither additional species richness nor replenishment of leached N augmented mineralization rates. The net rate at which N was supplied tended to be lowest in stands where demand for N was highest. Careful choice of species, coupled with low frequency of disturbance, can lead to maintenance of N within biomass and steady rates of within-system circulation, whereas pulses, whether caused by cutting and replanting or by the phenological traits of the species selected or combined, subject N supplies to leaching loss.

Biodiversity↗

Interpopulation differences in exudate feeding of pygmy marmosets in Ecuadorian Amazonia.

Local variations in fruit- and leaf-eating have been reported for some primate species; however, similar variations in exudate-feeding of pygmy marmosets, one of the most specialized neotropical primate species, have not been studied. In our 3-year study of four populations of pygmy marmosets in northeastern Ecuador, we characterized their exudate-feeding behavior by describing the use of exudate sources. We tested whether the use of exudate species was related to ecological factors such as the availability of exudate species in an area. We estimated the daily activity budgets of the groups with 1-hr scan samples and found significant interpopulation differences in the time spent on exudate feeding. We recorded a total of 18 exudate species used in the four populations; however, the populations differed in the total number of species used and in the preferred species. The most commonly used plant species were Sterculia apetala at San Pablo, Cedrela odorata at Sacha, Inga marginata at Amazoonico, and Parkia balslevii at Zancudo. We recorded the presence and abundance of the 18 exudate species in 90-m transects in the home range of each group and in one additional control area that contained no marmosets, for each population. Differences in the most-used exudate species among populations did not appear to be related to the availability of these species in each population, i.e., the marmosets did not use at random the exudate species available within their range, nor did they use more often the exudate species that were more abundant in their home ranges. One implication of our results for conservation is that protecting exudate resources based on data from only one area will not be sufficient to preserve pygmy marmosets in all populations.

Animals↗

Insect growth inhibition by tocotrienols and hydroquinones from Roldana barba-johannis.

The methanol extract from the aerial parts of Roldana barba-johannis (Asteraceae) afforded sargachromenol, sargahydroquinoic acid, and sargaquinoic acid. These natural products and their corresponding acetylated and methylated derivatives showed insecticidal and insect growth regulatory activities against the Fall Armyworm [Spodoptera frugiperda J.E. Smith, (Lepidoptera: Noctuidae)], an important insect pest of corn. The most active compounds were sargachromenol and its acetylated derivative; sargahydroquinoic acid and its acetylated derivative; and a mixture of sargachromenol, sargahydroquinoic acid, and sargaquinoic acid (6:3:1) and the acetylated form of this mixture. All these compounds and mixtures had significant inhibitory effects between 5.0 and 20.0 ppm in diets. Most compounds were insecticidal to larvae, with lethal doses between 20 and 35 ppm. In addition, these substances also demonstrated scavenging properties toward 2,2-diphenyl-1-picrylhydrazyl radical in TLC autographic and spectrophotometric assays. These compounds appear to have selective effects on the pre-emergence metabolism of the insect. The results from these compounds were fully comparable in activity to those known natural insect growth inhibitors such as gedunin and methanol extracts of Cedrela salvadorensis and Yucca periculosa. These substances may be useful as natural insecticidal agents.

Animals↗

Insect growth regulatory effects of some extracts and sterols from Myrtillocactus geometrizans (Cactaceae) against Spodoptera frugiperda and Tenebrio molitor.

A methanol extract from the roots and aerial parts of Myrtillocactus geometrizans (Cactaceae) yielded peniocerol 1, macdougallin 2, and chichipegenin 3. The natural products 1, 2 their mixtures, MeOH and CH(2)Cl(2) extracts showed insecticidal and insect growth regulatory activity against fall armyworm [Spodoptera frugiperda J. E. Smith (Lepidoptera: Noctuidae)], an important insect pest of corn, and [Tenebrio molitor (Coleoptera)], a pest of stored grains in Mexico. The most active compounds were 1, 2, and a mixture (M(2)) of 1 and 2 (6:4). All these extracts, compounds and the mixture had insect growth regulating (IGR) activity between 5.0 and 50.0 ppm and insecticidal effects between 50 and 300 ppm in diets. The extracts were insecticidal to larvae, with lethal doses between 100 and 200 ppm. These compounds appear to have selective effects on the pre-emergence metabolism of Coleoptera, because in all treatments of the larvae of T. molitor, pupation were shortened and this process show precociousness in relation to controls. In contrast to S. frugiperda larvae, onset of pupation was noticeably delayed. Emergence in both cases was drastically diminished. In both pupae and in the few adults that were able to emerge, many deformations were observed. The results of these assays indicated that the compounds were more active than other known natural insect growth inhibitors such as gedunin and methanol extracts of Cedrela salvadorensis and Yucca periculosa. Peniocerol, macdougallin and chichipegenin, as well as mixtures of these substances, may be useful as natural insecticidal agents.

Animals↗

Antimalarial activity of tropical Meliaceae extracts and gedunin derivatives.

Extracts of 22 species of Meliaceae were examined for antimalarial activity using in vitro tests with two clones of Plasmodium falciparum, one sensitive to chloroquine (W2) and one chloroquine-resistant (D6). Twelve extracts were found to have activity, including extracts of Cedrela odorata wood and Azadirachta indica leaves, which contained the limonoid gedunin. These extracts were more effective against the W2 clone than the D6 clone, suggesting there is no cross-resistance to chloroquine. Gedunin was extracted in quantity, and nine derivatives prepared for a structure-activity study, which revealed essential functionalities for activity. The study also included four other limonoids derived from related Meliaceae. Only gedunin had better activity than chloroquine against the W2 clone. This active principle could be used to standardize a popular crude drug based on traditional use of A. indica in West Africa.

Animals↗

Electrophysiological responses of female and male Hypsipyla grandella (Zeller) to Swietenia macrophylla essential oils.

The mahogany shoot borer, Hypsipyla grandella, is one of the most economically important Neotropical forest pest insects because it attacks valuable timber of the Meliaceae. Despite detailed information on the life cycle of H. grandella, factors influencing attack by the shoot borer are not well known. Electroantennogram studies of borer antennae indicate that both female and male moths elicited significant antennal responses to essential oil of the terminal shoots, mature and senescent leaves, in three concentrations. Gamma-himachalene, germacrene D, germacrene A, cadina-1,4-diene, hexadecanoic acid, and ethyl hexadecanoate appeared in all essential oils from Swietenia macrophylla. Germacrene-D and gamma-himachalene were also present in the active essential oil of Cedrela odorata and Toona ciliata. These findings suggest that these compounds play a role in attracting H. grandella to oviposit on the leaves of these plants. The GC-EAD of essential oil from S. macrophylla mature leaves to female H. grandella antennae led to the identification of beta-caryophyllene as the main constituent responsible for the antennae response.

Animals↗

Study on the inhibitory effects of Korean medicinal plants and their main compounds on the 1,1-diphenyl-2-picrylhydrazyl radical.

A 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical-generating system was used to evaluate the antioxidant properties of Korean medicinal plants that have been used widely as folk medicines for several disorders, as well as compounds isolated from them. Among the Rosaceae, Rosa rugosa and Rosa davurica showed strong DPPH radical-scavenging activity. The most effective medicinal plant from families other than Rosaceae was Cedrela sinensis, followed in order by Nelumbo nucifera, Eucommia ulmoides, Zanthoxylum piperitum, Cudrania tricuspidata and Houttuynia cordata. These results serve as a good index of the free radical-scavenging activities of Korean medicinal plants. Furthermore, the polyphenols isolated from these plants, procyanidin B-3, (+)-catechin, gallic acid, methyl gallate, quercetin, quercetin-3-O-beta-D-glucoside, quercetin-3-O-beta-galactoside, quercetin-3-O-rutinose and kaempferol, exerted strong DPPH radical-scavenging activity. These results suggest that the Korean medicinal plants and the polyphenols isolated from them that exhibited effective radical-scavenging activity may be promising agents for scavenging free radicals and treating diseases associated with excess free radicals.

Biflavonoids↗

The inhibitory effects of 12 medicinal plants and their component compounds on lipid peroxidation.

The antioxidative activities of 12 medicinal plants and the compounds isolated from them were investigated using the thiocyanate method to evaluate inhibitory effects on lipid peroxidation in the linoleic acid system. The peroxide levels gradually increased during incubation in the presence of linoleic acid over 3 days, and most of the plants inhibited lipid peroxidation. In particular, of the plants tested, Cudrania tricuspidata, Zanthoxylum piperitum, Houttuynia cordata and Ulmus parvifolia reduced lipid peroxidation more effectively as lipid peroxidation progressed, resulting in inhibition of about 80% relative to the control value by the 3rd day of incubation. In addition, the polyphenols isolated from the plants also showed marked and dose-dependent inhibitory effects on lipid peroxidation. The compounds with the strongest activities were 3,4-dihydroxylbenzoic acid, quercetin, the quercetin glycosides quercetin-3-O-beta-D-galactoside, quercetin-3-O-alpha-L-rhamnoside, quercetin-3-O-beta-D-glucoside and quercetin-3-O-rutinose, catechin, gallic acid, methyl gallate and rosamultin isolated from Zanthoxylum piperitum, Houttuynia cordata, Rosa rugosa and Cedrela sinensis. Moreover, quercetin glycosides showed stronger activity than quercetin, suggesting that glycosylation increases the antioxidative activity of quercetin. Our results indicate that the medicinal plants and their polyphenols show promise as therapeutic agents for various disorders involving free radical reactions.

Drugs, Chinese Herbal↗

Acetylcholinesterase and insect growth inhibitory activities of Gutierrezia microcephala on fall armyworm Spodoptera frugiperda J.E. Smith.

From the aerial parts of Gutierrezia microcephala (Asteraceae), four oxyflavones were isolated, namely 5,7,2'-trihydroxy-3,6,8,4',5'-pentamethoxyflavone (1); 5,7,4'-trihydroxy-3,6,8-trimethoxyflavone (2); 5,7,2',4'-tetrahydroxy-3,6,8,5'-tetramethoxyflavone (3); 5,2'-dihydroxy-3,6,7,8,4',5'-hexamethoxyflavone (4), and an ent-clerodane, bacchabolivic acid (5). Compounds 1-5, the synthetic methyl ester (6), n-hexane and MeOH extracts were evaluated against the fall armyworm (Spodoptera frugiperda). Gedunin, a known insect growth regulator isolated from Cedrela spp. was used as a positive control. When tested for activity on neonate larvae into the no-choice artificial diet bioassay, flavone (1), clerodane (5), its methyl ester (6), MeOH and n-hexane extracts caused significant larval mortality with MC50 of 3.9, 10.7, 3.46, 7.95 and 7.5 ppm at 7 days, respectively, as well as growth reduction. They also increased the development time of surviving larvae and a significant delay in time to pupation and adult emergence. Acute toxicity against adults of S. frugiperda was also found, 5, 6, gedunin and n-hexane extract had the most potent activity with LD50 value of 6.59, 15.05, 10.78, and 12.79 ppm, respectively. In addition, MeOH, n-hexane extracts, 5, 6 and gedunin caused acetylcholinesterase inhibition with 93.7, 100, 90.2, 62.0 and 100% at 50.0 ppm, respectively; whereas 1-4 exhibited only moderate inhibitory activity. Compounds 1, 5 and 6 showed inhibitory activities comparable with gedunin. These compounds could be responsible of the insect growth inhibitory activity of this plant.

Acetylcholinesterase↗

Traditionally-used antimalarials from the Meliaceae.

A quantitative ethnobotanical approach to antimalarial drug discovery led to the identification of Lansium domesticum Corr. Ser. (Meliaceae) as an important antimalarial used by Kenyah Dyak healers in Indonesian Borneo. Triterpenoid lansiolides with antimalarial activity were isolated from the bark and shown to have activity in both in vitro bioassays with Plasmodium falciparum, and in mice infected with P. berghei. A survey of African and tropical American Meliaceae led to further development of the limonoid gedunin from the traditionally used medicinal plants, tropical cedar, Cedrela odorata L., and neem, Azadirachta indica A. Juss. Gedunin has significant in vitro activity but initially showed poor in vivo activity. In vivo activity was improved by (1) incorporation into an easy to absorb suspension, (2) preparation of a more stable compound, 7-methoxygedunin; and (3) synergism with dillapiol, a cytochrome P450 3A4 inhibitor. The results show the potential for both antimalarial drug and phytomedicine development from traditionally used plants.

Antimalarials↗

Biological activity of Ruta chalepensis (Rutaceae) and Sechium pittieri (Cucurbitaceae) extracts on Hypsipyla grandella (Lepidoptera: Pyralidae) larvae.

Biological activity of a plant extract (common rue, Ruta chalepensis) and a semi purified fraction (from "tacaco cimarrón", Sechium pittieri) on mahogany shootborer larvae (Hypsipyla grandella) was studied. A randomized complete block design, with four replications, was used. H. grandella third instar larvae were exposed for 24 h to Cedrela odorata leaf discs dipped in several treatment dissolutions of each extract (0.1, 0.32, 1.0, 3.20, and 10%); afterwards, each larva was transferred to a flask containing an artificial diet and was allowed to complete its development. Variables measured included food consumption (foliar area eaten in 24 h), mortality, and developmental effects (developmental time for each larval instar and the pupa, and pupal weight). The common rue extract showed a clear antifeedant activity at a concentration as low as 0.32%, whereas the "tacaco cimarrón" fraction caused toxicity, especially at the two highest concentrations (3.20 and 10%).

Analysis of Variance↗

Screening of Leishmania APRT enzyme inhibitors.

Adenine phosphoribosyltransferase (APRT) enzyme from Leishmania tarentolae has been proposed as a target for the rational search of new leishmanicidal drugs. In this paper, we describe the evaluation of the inhibitory activity on L. tarentolae APRT enzyme of 46 crude extracts of Meliaceae and Rutaceae plants, besides three furoquinolone alkaloids. The results showed that 21 extracts were able to decrease the APRT enzymatic activity (IA% > or = 50). The methanolic extracts from roots and leaves of Cedrela fissilis and from fruits, branches and leaves of Cipadessa fruticosa have showed strong activities. Therefore, these species could be a promising source of lead compounds for the rational design of new leishmanicidal drugs. The phytochemical investigation of an active fraction from Almeidea rubra afforded the alkaloids isodutaduprine, isoskimmianine and isokokusagine, which showed low to moderate activity on APRT.

Adenine Phosphoribosyltransferase↗

[Chemical and biological evaluation of the effect of plant extracts against Plasmodium berghei].

Extracts from thirteen species of plants were evaluated by "in vivo" antimalarial test against plasmodium berghei effects. Significant activities were observed in the ethyl acetate and aqueous extracts, elaborated of Cedrela tonduzii leaves, Trichilia havanensis and Trichilia americana barks, Neurolaena lobata and Gliricidia sepium leaves and Duranta repens fruits. Compounds identified include flavanoids, coumarins, mellilotic acid and iridoids which some kind of biodynamic activity has previously been reported. The flavone quercetin 1 purified from C. tonduzii gave strong antimalarial activity, however, its respective glucosides (quercetin 3-glucoside 2 y robinine 7) showed little significant activity.

Animals↗

12alpha-hydroxystigmast-4-en-3-one: a new bioactive steroid from Toona ciliata (Meliaceae).

In a bioassay guided phytochemical investigation of Toona ciliata (Fam. Meliaceae), a new hydroxy steroidal ketone, 12alpha-hydroxystigmast-4-en-3-one (1) was isolated from the petroleum ether extract of the plant together with two known steroids and three C-methyl coumarins. The structure of 1 was established by means of spectroscopic analyses. Compound 1 was found cytotoxic in a brine shrimp lethality bioassay with LC50 of 9.9 microg/ml and it also showed significant antitumor activity with Ti50 value of 14.1 microg/ml in a potato disc bioassay.

Animals↗

The fractionated Toona sinensis leaf extract induces apoptosis of human ovarian cancer cells and inhibits tumor growth in a murine xenograft model.

OBJECTIVE: Aqueous extract from the leaves of Toona sinensis Roem. has been shown to have an anti-proliferative effect on human lung cancer cells. In this study, we analyzed the anti-cancer activity/effect of different extraction fractions of the extract from T. sinensis leaves on ovarian cancer cells. METHODS: Cell viability was determined by XTT cell proliferation assay and cell survival assay. Apoptotic effect was detected by morphological analysis and immunoblotting. Cell cycle effect was evaluated by flow cytometry analysis and immunoblotting. In vivo therapeutic effect was evaluated by the subcutaneous inoculation of SKOV3 cells in nude mice (Foxnlnu/Foxnlnu) model. RESULTS: TSL2 of T. sinensis was more cytotoxic than other fractions and exhibited selectivity for ovarian cancer cell lines. TSL2 arrested SKOV3 ovarian cancer cells at the G2/M phase and induced cancer cells go through apoptotic pathway. Ex vivo xenograft study of nude mice showed that intraperitoneal injection of TSL2 was able to suppress the proliferation of ovarian cancer cells without significant nephrotoxicity, liver toxicity, or bone marrow suppression.

Animals↗

Morphological and secretory characterization of extrafloral nectaries in plants of coastal Veracruz, Mexico.

BACKGROUND AND AIMS: Morphological descriptions of the extrafloral nectaries (EFNs) of certain plant species are common in the literature, but they rarely relate morphology with histology, gland distribution and secretory attributes. In this study a morphological/secretory characterization of EFNs occurring on several plant species in a tropical coastal community is made and the implications of gland attributes discussed from a functional perspective. METHODS: The morphology and nectar secretion of the EFNs of 20 plant species are characterized through scanning electron microscopy, histochemical detection of reducing sugars (Fehling's reagent) and nectar volume/concentration estimates. KEY RESULTS: Sixty-five per cent of plant species in coastal communities had EFNs on vegetative structures and 35 % of species had glands on reproductive and vegetative organs. The Fabaceae is the plant family with the most species with EFNs and most diversity of gland morphologies. Four types of vascularized nectaries and four of glandular trichomes are described; sugar-secreting trichomes are characterized using Fehling's technique, and the first descriptions of unicellular and peltate trichomes functioning as EFNs are provided. Glands of ten plant species and six genera are described for the first time. Four plant species possess more than one morphological type of EFN. Eleven species have EFNs in more than one location or organ. More complex glands secrete more nectar, but are functionally homologous to the aggregations of numerous secretory trichomes on specific and valuable plant organs. CONCLUSION: Important diversity of EFN morphology was foundin the coastal plant community studied. Both vascularized and non-vascularized EFNs are observed in plants and, for the latter, previously non-existent morpho-secretory characterizations are provided with a methodological approach to study them. It is recommended that studies relating EFN attributes (i.e. morphology, distribution) with their differential visitation by insects (i.e. ants) and the cost of maintenance to the plants are carried out to understand the evolution of these glands.

Acacia↗