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Enhancing of radioresponsiveness of tumors by using radiosensitizers is a promising approach to increase the efficacy of radiation therapy. Recently, the ethanolic extract of the medicinal plant, Derris scandens Benth has been identified as a potent radiosensitizer of human colon cancer HT29 cells. However, cell death mechanisms underlying radiosensitization activity of D scandens extract have not been identified. Here, we show that treatment of HT-29 cells with D scandens extract in combination with gamma irradiation synergistically sensitizes HT-29 cells to cell lethality by apoptosis and mitotic catastrophe. Furthermore, the extract was found to decrease Erk1/2 activation. These findings suggest that D scandens extract mediates radiosensitization via at least two distinct modes of cell death and silences pro-survival signaling in HT-29 cells.

Aim The historical biogeography of three Palaeotropical legume genera, Aganope, Brachypterum and Derris, was investigated with the aim of (1) evaluating competing hypotheses on the origins of Palaeotropical intercontinental disjunctions (PIDs), and (2) inferring spatio-temporal diversification patterns in tropical Southeast Asia. Location Palaeotropics. Methods Plastid (trnL–F IGS, psbA–trnH IGS and trnK–matK ORF) and nuclear ribosomal (ITS/5.8S) DNA sequence data, covering the geographical distribution of all three genera, were analysed using an uncorrelated-rates relaxed molecular clock model. Ancestral areas were reconstructed using a likelihood approach implementing the dispersal–extinction–cladogenesis model (Lagrange) and a Bayesian approach to dispersal–vicariance analysis (S-DIVA). Results A wide ancestral distribution in Africa and Asia was inferred for the Aganope stem and crown groups, with a vicariance event between Africa and Asia in the early Miocene. The Southeast Asian mainland was inferred as the ancestral area for both the Brachypterum and the Derris crown groups. The reconstructions indicated numerous dispersal events westwards to India, and eastwards across Wallace's Line to New Guinea from the middle Miocene onwards. Two dispersal events from Asia to Africa, in the Miocene–Pliocene in Brachypterum and in the Pliocene–Pleistocene in Derris, were deduced. Main conclusions The PID in Aganope is likely to be the result of vicariance, caused by climatic deterioration subsequent to the Middle Miocene Climatic Optimum. The inferred PIDs in Brachypterum and Derris in the middle Miocene to Pliocene–Pleistocene are consistent with long-distance dispersal. The biogeographical patterns of Brachypterum and Derris are similar to patterns identified in other Southeast Asian plant taxa, and highly congruent with geological events in Southeast Asia facilitating dispersal from the early Miocene onwards. Preadaptation to several environmental conditions and habitats including mangrove swamps, and high dispersal capabilities by hydrochory may explain the wide distributions of some species and frequent dispersal across oceanic water bodies separating western and eastern Malesia.

Derris solorioides is described as a new species and illustrated. This species is only the second calciphilous and true-paniculate species of Derris ever recorded. The species was found in isolated and protected limestone areas surrounded by agricultural areas in Nakhon Sawan province, North-Central Thailand. It is characterized by its rather smaller flowers but with more ovules than other species of Derris, and 1-winged pods showing a dark-coloured pericarp around the seeds without thickening of the pericarp. The characters of the pods are similar to those found in Solori, a genus once synonymized with Derris and, therefore, the epithet ‘solorioides’ was assigned. This species appeared to be a distinct taxon in the molecular phylogeny, separate from its morphologically highly similar species, D. marginata. It is also a member of a lineage of Derris consisting of species with a deviating type of inflorescence: intermediate forms and true panicles, which is quite uncommon in this genus. The relationship with its closely related species is discussed, and a key to the species of Derris in the ‘deviating type of inflorescence’ clade is presented.

Oryctes rhinoceros Linnaeus is one of the main pests of oil palm plants. The Oryctes rhinoceros control of being commonly used is synthetic insecticides. However, it is unwise useable to cause negative impacts on humans and the agricultural environment. Therefore, an alternative insecticide that is safer and environmentally friendly is needed, such as tuba root (Derris elliptica Benth.). The research was conducted in a Plant Pest laboratory, Faculty of Agriculture, University of Riau, Pekanbaru, from July to August 2018. This study aims to obtain an effective concentration of tuba root extract to control Oryctes rhinoceros larvae. The research was conducted experimentally using a Completely Randomized Design (CRD), which consists of five treatments and four replications. The treatment used is the concentration of tuba root extracts 0 g.l-1 of water, 25 g.l-1 of water, 50 g.l-1 of water, 75 g.l-1 of water and 100 g.l-1 of water. The result in them showing that the application of tuba root extract at a concentration of 75 g.l-1 was able to decrease O. rhinoceros larvae population with a total mortality of 82.5%. The lethal concentration to kill 50% of O. rhinoceros larvae population was 1.0% or equal to 10 g.l-1 of tuba root extract, while the lethal concentration to kill 95% of O. rhinoceros larvae population was 30.6% or equal to 306 g.l-1 tuba root extract.

This study was performed to evaluate the acute contact and oral toxicity of plant extracts (neem, sophora and derris) against Honeybee (Apis mellifera L.). As a result of acute contact toxicity test, LD of neem and derris extracts were more than 100 µg/bee while LD of sophora extracts were 1.7 µg/bee. In case of acute oral toxicity test, LD of neem and derris extracts were more than 100 µg/bee while LD of sophora extracts were 1.7 and 0.3 µg/bee. In conclusion, it is evaluated that neem and derris extracts are practically nontoxic while sophora extracts are highly toxic.

In some previous studies, we described the isolation of nine compounds from leaves of Derris urucu, a species found widely in the Amazon rainforest, identified as five stilbenes and four dihydroflavonols. In this work, three of these dihydroflavonols [urucuol A (1), urucuol B (2) and isotirumalin (3)] were evaluated to identify their potential as allelochemicals, and we are also reporting the isolation and structural determination of a new flavonoid [5,3′-dihydroxy-4′-methoxy-(7,6:5″,6″)-2″,2″-dimethylpyranoflavanone (4)]. We investigated the effects of the dihydroflavonols 1-3 on seed germination and radicle and hypocotyl growth of the weed Mimosa pudica, using solutions at 150 mg.L–1. Urucuol B, alone, was the substance with the greatest potential to inhibit seed germination (26%), while isotirumalin showed greater ability to reduce the development of the hypocotyl (25%), but none of the three substances showed the potential to inhibit radicle. When combined in pairs, the substances showed synergism for the development of root and hypocotyl and effects on seed germination that could be attributed to antagonism. When tested separately, the trend has become more intense effects on seed germination, while for the substances tested in pairs, the intensity of the effect was greater on development of weed. Em estudos anteriores descrevemos o isolamento de nove substâncias, a partir das folhas de Derris urucu, uma espécie encontrada amplamente na floresta Amazônica, as quais foram identificadas como cinco estilbenos e quatro diidroflavonóis. Neste trabalho, três desses diidroflavonóis [urucuol A (1), urucuol B (2) e isotirumalina (3)] foram avaliados para identificar seus potenciais como aleloquímicos. Estamos relatando também, o isolamento e a determinação estrutural de um novo flavonóide [5,3′-diidroxi-4′-metoxi-(7,6:5″,6″)-2″,2″-dimetilpiranoflavanona (4)]. Investigamos os efeitos dos diidroflavonóis 1-3 sobre a germinação de sementes e desenvolvimento da radícula e do hipocótilo da planta daninha Mimosa pudica, usando soluções a 150 mg.L–1. Urucuol B, isoladamente, foi quem apresentou o maior potencial para inibir a germinação de sementes (26%), por sua vez, isotirulamina exibiu maior capacidade para reduzir o desenvolvimento do hipocótilo (25%), porém nenhuma das três substâncias mostrou potencial para inibir o desenvolvimento da radícula. Quando combinadas aos pares, as substâncias mostraram sinergismo ao desenvolvimento da radícula e do hipocótilo e efeitos, na germinação de sementes, que poderiam ser atribuídos a antagonismo. Quando testadas separadamente, as substâncias apresentaram maior tendência para inibir a germinação de sementes, enquanto que, quando testadas aos pares, observou-se aumento no efeito de inibição do desenvolvimento da planta daninha.

Chloroform extracts of the fruit shell, leaves, root bark, root wood, seeds, stem bark and stem wood of Derris indica Bennet. were tested against the brine shrimp, Artemia salina nauplii. All the test extracts of D. indica were found to be effective. The LC50 values of the extracts were 15312.37, 92.074 and 29.661 ppm for the fruit shell; 60922.83, 61.522 and 23.777 ppm for the leaf; 15312.37, 51.477 and 19.169 ppm for the root bark; 2598.584, 30.480 and 8.260 ppm for the root wood; 545.025,26.730 and 7.719 ppm for the seed; 60922.83, 114.549 and 29.572 ppm for the stem bark and 7734.618, 58.501 and 23.694 ppm for the stem wood at 30 minute, 24 hours and 48 hours post exposures respectively at doses 200, 100, 50, 25, 12.5, 6.25, 3.125 and 1.563 ppm against A. salina . The toxicity of the extracts could be arranged in the order: seed > root wood > root bark> stem wood > leaf > fruit shell > stem bark extract. However, the extracts did not significantly inhibit the germination of mustard oil seeds, and thus its application to crops or to the crop field may not cause any harm to crop plants.DOI: http://dx.doi.org/10.3329/ujzru.v31i0.15402Univ. j. zool. Rajshahi Univ. Vol. 31, 2012 pp. 59-64

This study presents a consumer and farmer safety evaluation on the use of four botanical pesticides in pepper berry crop protection. The pesticides evaluated include preparations from clove, tuba root, sweet flag and pyrethrum. Their safety evaluation was based on their active ingredients being eugenol, rotenone, β-asarone and pyrethrins, respectively. Botanical pesticides from Acorus calamus are of possible concern because of the genotoxic and carcinogenic ingredient β-asarone although estimated margins of exposure (MOE) for consumers indicate a low priority for risk management. For the other three botanical pesticides the margin of safety (MOS) between established acute reference doses and/or acceptable daily intake values and intake estimates for the consumer, resulting from their use as a botanical pesticide are not of safety concern, with the exception for levels of rotenone upon use of tuba root extracts on stored berries. Used levels of clove and pyrethrum as botanical pesticides in pepper berry crop production is not of safety concern for consumers or farmers, whereas for use of tuba root and sweet flag some risk factors were defined requiring further evaluation and/or risk management. It seems prudent to look for alternatives for use of sweet flag extracts containing β-asarone.

Derris elliptica (Fabaceae) is one of the most important sources of the insecticide rotenone. The present study was aimed at developing microsatellite markers and evaluating their potential for use in germplasm genetics. There were 37 microsatellite markers specific for D. elliptica developed from an AC-enriched genomic library using the Fast Isolation by AFLP of Sequences Containing repeats (FIASCO) method. All markers were polymorphic amongst 16 accessions of the cultivated D. elliptica and four accessions of wild relatives, providing evidence for cross-species transferability within the genus Derris. These markers amplified a total of 159 alleles with a range of 2–8 and an average of 4.3 per locus. The polymorphic information content (PIC) value across all loci was 0.53 with a range of 0.05–0.75. There was similar genetic variability within cultivated and wild accessions (both with average expected heterozygosity of 0.54). Cluster analysis clearly distinguished all wild relatives from each other and from the cultivated genotypes. These markers should be used for genetic diversity studies and breeding programs in D. elliptica.

(Right) C N Sundaresan is currently an Associate Professor in the Department of Chemistry at the Sri Sathya Sai Institute of Higher Learning, Bangalore. His research interests are in synthesis of biologically active compounds, and pharmacuetical co-crystals. Among the several ways of exploiting locally available plants in their day-to-day activities by primitive communities all over the world, catching fish for food was a major one. The plants used for this purpose included species of Derris and Lonchocarpus of the family Leguminosae (Fabaceae). The active principle, rotenone, is a pentacyclic isoflavanoid derivative. Several other closely related compounds are also known and these are together classified as rotenoids.

Antiglycating potentials of Derris indica L., derived constituents were evaluated against advanced glycation end product formation using in vitro bioassays and compared with those of commonly used standards. The structures of 12 constituents of Derris indica were characterized by spectroscopic analyses (NMR and Mass). Further, these constituents were simultaneously determined using high performance liquid chromatography (HPLC) using a Waters XTerra RP18 column (250 × 4.6 mm, 5 µ) with a gradient elution system comprising of acetonitrile, water and 0.1% (v/v) acetic acid, flow rate 0.8 mL/min and column temperature 25°C, respectively. The limits of detection (LODs) were below 0.10 µg/mL, whereas the limits of quantification (LOQs) were below 0.30 µg/mL. It is concluded that the method has merits such as high sensitivity, specificity, and simplicity versus those of the other methods reported in the literature.

The total syntheses of (-)-rotenone and (-)-dalpanol have been achieved by a group-selective, stereospecific 1,2-shift of an epoxy alcohol and S

In this study, lupinifolin, a prenylated flavonoid, was isolated from Derris reticulata stem, identified by NMR spectra and confirmed with mass spectrometry. Lupinifolin was freshly prepared by solubilizing in 0.1 N NaOH and immediately diluted in Muller–Hinton broth for antibacterial testing. The data showed that Gram-positive bacteria were more susceptible to lupinifolin than Gram-negative bacteria. Of four strains of Gram-positive bacteria tested, Staphylococcus aureus was the most susceptible. Using the two-fold microdilution method, it was found that lupinifolin possessed antimicrobial activity against S. aureus with minimum inhibitory concentration and minimum bactericidal concentration of 8 and 16 µg/ml, respectively, which is less potent than ampicillin. However, from the time–effect relationship, it was shown that lupinifolin had faster onset than ampicillin. The faster onset of lupinifolin was confirmed by scanning electron microscopy. To investigate the mechanism of action of lupinifolin, transmission electron microscopy (TEM) was performed to observe the ultrastructure of S. aureus. The TEM images showed that lupinifolin ruptured the bacterial cell membrane and cell wall. Due to its fast onset, it is suggested that the action of lupinifolin is likely to be the direct disruption of the cell membrane. This hypothesis was substantiated by the data from flow cytometry using DiOC2 as an indicator. The result showed that the red/green ratio which indicated bacterial membrane integrity was significantly decreased, similar to the known protonophore carbonyl cyanide 3-chlorophenylhydrazone. It is concluded that lupinifolin inhibits the growth of S. aureus by damaging the bacterial cytoplasmic membrane.

Bio-pesticides are natural occurring substances that control pest and derived either from plants or microorganism. It play a vital role in coping with adverse effect arise due to massive used of synthetic pesticides and development of insecticide resistance of some insect groups in crop productions. Thus, Derris species from Leguminosae (Fabacea) family is a climbing plant of Southeast Asia that was well known for its environmental friendly bioactive compound is used as one of the effective insecticides. Rotenone was one of the bioactive constituents extracted from Derris plant that was used as agricultural pest control due to its strong paralysis action (knock-down effect) on cold blooded animals. Moreover, it has a lethal mechanism in inhibiting respiratory enzyme of insects and easily degrades which makes it environmental friendly. Extraction of rotenone commonly uses organic solvents as extractant either in non-conventional extraction methods or conventional method. Application of green solvents, ionic liquids as extractant is new approach for rotenone extraction. Indeed environmental friendly bio-pesticides have not been studied thoroughly and several approach and further study are required to produce high quality and environmental friendly bio-pesticides. In addition, biological assay such as “Brine Shrimp (Artemia salina) Lethality” study is also vital in order to determine a preliminary safe exposure limit of extracted rotenone prior to be used as pesticides. For that reason, a review of the environmental friendly bio-pesticide rotenone extracted from Derris sp. is presented herewith. This article reviews the up scaling extraction methods, toxicity and its effectiveness against several moth species such as Spodoptera litura and Plutella xylostella.

Four different data representations were evaluated for the determination of the total antioxidant activities of four different Prunella L. species, which are Prunella vulgaris, Prunella grandiflora, Prunella laciniata, and Prunella orientalis Bornm. Three different antioxidant assays, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABST), 2,2-diphenyl-1-picrylhydrazyl (DPPH), and Folin-Ciocalteu (FC) reagent measured the total antioxidant activity and phenolic content of the four Prunella L species that were extracted with 12 different solvent systems. The data set of 48 Prunella L extracts was collected by high-performance liquid chromatography (HPLC) with ultraviolet diode array detection. The prediction of total antioxidant activity of Prunelia L species by super partial least square (sPLS) regression was obtained using four different representations of the data; the entire two-way chromatographic-spectral images, the average UV spectra, the total absorbance chromatogram, the lambda max (lambda(max)) chromatogram. The coefficients of determination (R-2) for the entire two-way chromatographic-spectral images (the ABST (0.943 +/- 0.008), the DPPH (0.91 +/- 0.01), and the FC (0.963 +/- 0.006)) indicated good accuracy for predicting antioxidant activities. The three different wet chemical assays are known to yield different values so it is advantageous to estimate the three separate values with a single LC measurement. The entire two-way chromatographic-spectral images have been used to the first time for calibration. Acidic hexane, as an extraction solvent, gave the least root mean square error of prediction (RMSEP) for the two-way chromatographic-spectral images, so it would be the best solvent for modeling antioxidant activities. United States Department of Agriculture (USDA) USDA Agricultural Research Service Canna Print, LLC

Six compounds were isolated from Derris laxiflora Benth., including two new pterocarpans, 7,6'-dihydroxy-3'-methoxypterocarpan (1) and derrispisatin (2), as well as four known ones, lespedezol D, (3), secundiflorol 1 (4), 6a-hydroxymaackiain (5) and pisatin (6). The structures of these compounds were determined by analysis of their spectroscopic data.

Due to the increased development of resistance of vectors against synthetic insecticides and chemical drugs, plant based insecticides serve as promising biocontrol agents for effective vector control. Green approach for the synthesis of nanoparticles has been attained using environmentally safe, non-toxic plant extracts. The present study was aimed to investigate the potent larvicidal activity of silver nanoparticles (AgNPs) produced by Derris trifoliata leaf extract in relation to the various concentrations of methanol and chloroform extracts for 24h against 3rd and 4th instar larvae of Aedes aegypti. AgNPs were synthesized using D. trifoliata leaf extract as reducing and stabilizing agent. Synthesized AgNPs were characterized by UV-Vis spectroscopy, FTIR spectroscopy, SEM, EDX, XRD and HRTEM. The size of AgNPs as estimated from the full width at half-maximum of (200) peak of silver was 16.13nm, the average crystalline size of the synthesized AgNPs was approximately 20nm, which was correlated with the HRTEM results (20nm). SEM and TEM images have shown the formation of polydispersed nanoparticles with an average size of 20nm. The FTIR spectra of AgNPs exhibited prominent peaks at 2360.7, 1606.2, 1095.6 and 785.9cm-1. The spectral peak observed at 1606.2, assigned to stretching vibration (C=O) in carbonyl compounds characterized by the presence of major constituents of flavonoids and terpenoids. The results obtained in FTIR spectroscopy correlated with the GC-MS analysis of methanol and chloroform extracts and indicates the presence of phytosteroids, flavonoids and terpenoids. The highest larvicidal activity was observed for the synthesized AgNPs against the 3rd instar larvae with LC50 values of 5.87mg/l and LC90 of 12.11mg/l, while against 4th instar larvae these values were7.00 and17.76mg/l respectively. The chloroform extracts also showed increased larvicidal activity than methanol extracts against 3rd instar larvae (LC50=54.42mg/l, LC90=140.83mg/l) and 4th instar larvae (LC50=62.47mg/l, LC90=145.06mg/l) of A. aegypti. Besides, the synthesized AgNPs also exhibited potent antibacterial activity against certain food borne pathogens. These results infer that the biologically synthesized AgNPs and organic solvent extracts have the potential to be used as an excellent eco-friendly approach for vector control against A. aegypti.

Derris scandens (ROXB.) BENTH. (Fabaceae) is used as an alternative treatment for cancer in Thai traditional medicine. Investigation of the topoisomerase II (Top2) poison of compounds isolated from this plant may reveal new drug leads for the treatment of cancer. Bioassay-guided isolation was performed on an extract of D. scandens stems using a yeast cell-based assay. A yeast strain expressing the top2-1 temperature-sensitive mutant was used to assay Top2 activity. At the permissive temperature of 25°C, yeast cells were highly sensitive to Top2 poison agents. At the semi-permissive temperature of 30°C, where enzyme activity was present but greatly diminished, cells displayed only marginal sensitivity. The bioassay-guided fractionation of the extract led to the isolation of two known isoflavones: 5,7,4'-trihydroxy-6,8-diprenylisoflavone (1) and lupalbigenin (2). These two compounds also displayed cytotoxicity against three different cancer cell lines, KB, MCF-7 and NCI-H187. In conclusion, Top2 poison agents from D. scandens are reported for the first time, substantiating the use of D. scandens in Thai traditional medicine for cancer treatment.

Background & Objectives: Vector control is facing a threat due to the emergence of resistance to synthetic insecticides. Insecticides of botanical origin may serve as suitable alternative in near future. In the present study, crude plant extracts of 32 commonly available plants were evaluated at different concentrations against third instars larvae of Culex quinquefasciatus to establish their mosquito larvicidal activity. Methods : Three different Concentrations (0.1, 0.5 and 1.0%) of crude extracts were prepared from selected plants and observed larval mortality after 24h, 48h & 72h of post exposure against third instars larvae of Cx. quinquefasciatus . LC 50 and LC 90 were determined by using log-probit analyses. Effects on non target organisms were also tested. Result : Among the tested concentrations, highest mortality was recorded at 1% concentration of crude extract within 72 hours of exposure in all plant extracts. In laboratory based larvicidal bioassay, lowest LC 50 and LC 90 values were recorded in fruit extracts of Solanum nigrum and Solanum sisymbrifolium respectively. Mosquito larvicidal property of Clerodendrum viscosum , Cleome viscosa, Alangium salvifolium, Murraya k oenigii, Polyalthia longifolia and Derris indica were also satisfactory. Tested non-target organisms were entirely safe against the tested concentrations during study. Interpretation & Conclusion : Among tested 32 plants, the crude extracts ofeight plantshave the potent larvicidal activity against filarial vector Cx. quinquefasciatus without harmful effect on non target organisms.

PREMISE OF THE STUDY Palaeotropic Derris-like taxa (family Fabaceae, tribe Millettieae) comprise 6-9 genera. They are well known as important sources of rotenone toxin, which are used as organic insecticide and fish poison. However, their phylogenetic relationships and classification are still problematic due to insufficient sampling and high morphological variability. METHODS Fifty species of palaeotropic Derris-like taxa were sampled, which is more than in former studies. Three chloroplast genes (trnK-matK, trnL-F IGS, and psbA-trnH IGS) and nuclear ribosomal ITS /5.8S were analyzed using parsimony and Bayesian methods. KEY RESULTS Parsimony and Bayesian analyses of individual and combined markers show more or less similar tree topologies (only varying in terminal branches). The old-world monophyletic genera Aganope, Brachypterum, and Leptoderris are distinct from Derris s.s., and their generic status is here confirmed. Aganope may be classified into two or three subgeneric taxa. Paraderris has to be included in Derris s.s. to form a monophyletic group. The genera Philenoptera, Deguelia, and Lonchocarpus are monophyletic and distinct from each other and clearly separate from Derris s.s. Morphologically highly similar species of Derris s.s. are shown to be unrelated. Our study shows that previous infrageneric classifications of Derris are incorrect. Paraderris elliptica may contain several cryptic lineages that need further investigation. CONCLUSIONS The concept of the genus Derris s.s. should be reorganized with a new generic circumscription by including Paraderris but excluding Brachypterum. Synapomorphic morphological features will be examined in future studies, and the status of the newly defined Derris and its closely related taxa will be formalized.

Ethnopharmacological relevance The plants used in this study had previously been identified and used by Thai folk practitioners, who had knowledge of Thai traditional medicine, as alternative treatments for cancer. Investigation into the mechanism of the Topoisomerase II (Top2) poison of these plants may give rise to new drug leads for cancer treatment. Aim of the study This study aimed to screen ethnomedicinal plants used in Thai traditional medicine for Top2 poison activity using a yeast cell-based assay and also to validate the traditional uses of these plants by examining the Top2 poison activity. Materials and methods Thirty Thai medicinal plants were harvested and identified. Plant methanol extracts were prepared and screened in vitro using a yeast cell-based assay. Mutant yeast strains carrying the top2-1 allele, which encodes a temperature-sensitive topoisomerase, were used to establish the yeast spot test. Strains carrying this mutation grow normally at 25 °C and generally have a wild-type drug sensitivity. These yeast strains are able to grow at 30 °C, but the Top2 activity is greatly reduced at this temperature, which causes the strains to be highly drug resistant to anti-Top2 agents. Cell growth was measured by colony survival after exposure to various concentrations of extracts at different temperatures. Results The extracts of six out of thirty ethnomedicinal plants, Curcuma longa , C. zedoaria , Derris scandens , Grangea maderaspatana , Stephania pierrei and S. suberosa , were found to have Top2 poison activity against the yeast cells. Conclusions The yeast screening system confirmed the proposed anti-cancer mechanisms of plants used in Thai traditional medicine by traditional doctors.

A new coumaronochromone, 6,4'-dihydroxy-7,5' -dimethoxy-coumaronochromone (1), together with eleven known flavonoids (2-12) were isolated from the ethanol extract of the aerial part of Derris elliptica. Their structures were elucidated on the basis of spectroscopic analysis. Compounds 2, 4, 7, 8 and 9 exhibited moderate insecticidal activities against larvae of Aedes albopictus. All compounds showed strong cytotoxic activities against Spodoptera litura (SL) and Trichoplusia ni BTI-Tn-5B1-4 (Hi-5) cells comparison to positive control of rotenone.

Chloroform extracts of fruit shell, leaf, root-bark, root-wood, seeds, stem-bark and stem-wood of Derris indica Bennet. were tested on the mosquito Culex quinquefasciatus Say larvae. The LC50 values of fruit shell, leaf, root-bark, root-wood, seed, stem-bark and stem-wood were 30762.54, 60922.83, 70070.31, 3867.32, 361.89, 453810.10 and 225860.20 ppm, respectively for 30 minutes of exposure; 220.60, 141.56, 59.54, 36.95, 21.52, 229.92 and 82.84 ppm, respectively for 24 hours of exposure, and 49.97, 34.00, 26.26, 18.33, 8.64 , 68.88 and 30.15 ppm, respectively for 48 hours of exposure. The dose-mortality effects were in the order: seed > root-wood > root-bark > stem-wood > leaf > fruit shell > stem-bark. DOI: http://dx.doi.org/10.3329/bjz.v39i2.10568 Bangladesh J. Zool. 39(2): 137-145, 2011

A new flavanone, 4',5,7-trihydroxy-6,8-di-(2-hydroxy-3-methylbut-3-enyl)-flavanone, was isolated from the aerial parts of Derris trifoliate, together with eleven known compounds: rotenone, tephrosin, 12a-hydroxyrotenone, deguelin, 6a,12a-dehydro-rotenone, dehydrodeguelin, 7a-O-methyldeguelol, 7a-O-methylelliptonol, 5,7,3',4'-tetra-hydroxy- 6,8-diprenylisoflavone, daidzein and 4'-hydroxy-7-methoxyflavanone. 7a-O-Methylelliptonol was isolated for the first time from the genus Derris. Their structures were characterized on the basis of spectral data. Eight of the isolated compounds were found to be significantly toxic to brine shrimp (LC50 range 0.06-9.95 mu g/mL). The new compound showed weak toxicity (LC50 = 211.31 mu g/mL).

Application test of crude extracts of pinang fruit, tuba root, patah tulang, and neem leaf on golden apple snail (Pomacea sp.) in green house. This research was conducted to evaluate the effect of four botanical crude extracts namely Areca catechu, Derris eliptica, Euphorbia tirucalli and Azadirachta indica on golden apple snails under green house condition. All experiment units were arranged in randomized completely design consisting of some levels of concentration (titer). The result showed that low concentration of the crude extract of A. catechu fruit (0,5 g/l) and crude extracts of D. elliptica root (1 g/l) were very toxic, indicated by all snails tested were died. Mortality of snails tested caused by crude extract of A. indica was 100% at the concentration of 4 g/l, meanwhile crude extract of E. tirucalli was only 84% at a higher concentration of crude extract (8 g/l) occurring 96 hours after application.

The South American fruit fly, Anastrepha fraterculus (Wied.), is one of the principal pests of fruit crops in Brazil. While organic farms use several compounds to control fruit flies, such as oils, plant extracts and soaps, there is little scientific evidence of their effectiveness. Our main goal was to evaluate the phytosanitary products used in organic orchards on A. fraterculus under laboratory conditions. Four multiples (0.25×, 0.5×, 1× and 2×) of the manufacturer-recommended concentrations of Rotenat CE ® (extract of Derris spp. with rotenone 5%) (600 ml 100 l −1 ), Pironat ® (pyroligneous extract) (250 ml 100 l −1 ), Biopirol 7M ® (pyroligneous extract) (200 ml 100 l −1 ), Organic neem ® (neem oil 80%) (500 ml 100 l −1 ), Natuneem ® (neem oil – 1500 ppm of azadirachtin) (500 ml 100 l −1 ) and lime sulfur (20% S + 9% Ca) (5000 ml 100 l −1 ) were tested on A. fraterculus via ingestion and direct contact, topical application and residual application. We subsequently tested deterrence effects of the same products on oviposition. Organic Neem ® , Natuneem ® , lime sulfur, Pironat ® , and Biopirol 7M ® showed no insecticidal effect on the South American fruit fly. Only Rotenat CE ® (1200 ml 100 l −1 ) showed an effect (71.6% mortality) following ingestion/contact. Lime sulfur, Pironat ® and Biopirol 7M ® did not prevent oviposition of A. fraterculus on artificial fruits.

Introduction The Derris genus is known to contain flavonoid derivatives, including prenylated flavanones and isoflavonoids such as rotenoids, which are generally associated with significant biological activity. Objective To develop an efficient preparative isolation procedure for bioactive cajaflavanone. Methodology Fast centrifugal partition chromatography (FCPC) was optimised to purify cajaflavanone from Derris ferruginea stems in a single step as compared to fractionation from the cyclohexane extract by successive conventional solid–liquid chromatography procedures. The purification yield, purity, time and solvent consumption per procedure are described. The anti-fungal, anti-bacterial, anti-leishmanial, anti-plasmodial, anti-oxidant activities and the inhibition of advanced glycation end-products (AGEs) by cajaflavanone accumulation are described. Results FCPC enabled cajaflavanone purification in a single separation step, yielding sufficient quantities to perform in vitro biological screening. Interestingly, cajaflavanone had an inhibitory effect on the formation of AGEs, without displaying any in vitro anti-oxidant activity. Conclusion A simple and efficient procedure, in comparison with other preparative methods, for bioactive cajaflavone purification has been developed using FCPC. Copyright © 2011 John Wiley & Sons, Ltd.

The vapor-phase toxicity of Derris scandens Benth.-derived constituents was evaluated against four stored-product pests ( Callosobruchus chinensis L., Sitophilus oryzae L., Rhyzopertha dominica L., and Tribolium castaneum H.) using fumigation bioassays and compared to those of commonly used insecticides. The structures of all constituents of were characterized by spectroscopic analyses [nuclear magnetic resonance (NMR) and mass spectrometry]. The sensitivity of the test insect to compounds varied with exposure time, concentration, and insect species. Over 100% mortality after 24 h was achieved with the compounds osajin (2), scandinone (5), sphaerobioside (8), and genistein (9) against all of the test insects, while laxifolin (3) and lupalbigenin (4) showed 100% mortality after 72 h against T. csataneum and R. dominica . Scandenone (1), scandenin A (6), and scandenin (7) were less effective. Among the insects, C. chinensis , S. oryzae , and R. dominica were more susceptible to the treatments, whereas T. castaneum was less susceptible. The results of fumigation tests indicated that compounds from D. scandens whole plant extract are potential candidates to control stored-product pests.

Two rotenoids (rotenone and deguelin) were successfully isolated and purified from the roots of Derris by high-speed counter-current chromatography (HSCCC) with a two-phase solvent system composed of n-hexane-ethylacetate-methanol-water (7: 0. 25:5:3, v/v/v/v) on a preparative scale. The lower phase was used as the mobile phase and the upper phase was used as the stationary phase. The revolution speed was 850 r/min, the detection wavelength was set at 254 nm and the flow rate was 2.0 mL/min. Under the optimized conditions, within 2.5 h, 6.4 mg of rotenone with the purity of 96.60% and 23.4 mg of deguelin with the purity of 97.87% were obtained from 50 mg of the crude extract of the roots of Derris in a one-step elution. The results indicate that the rotenone and deguelin with high purities can be obtained by HSCCC, and the established method can provide the basic experimental material for the intensive study of rotenoids.

A more precise procedure for the colorimetric evaluation of Derris root is described, making use of the colour which rotenone and the matter which may be extracted from Derris root by ether produce with concentrated sulphuric acid containing a trace of sodium nitrite. Rotenone is used as a standard. A number of samples of Derris powder with varying contents of rotenone and ether extract were analyzed. It was found that the amount of “rotenoid” substances present in the different samples corresponded fairly well to the ether extract.

Purpose : To investigate the antitumor effect of candidone extracted from Derris indica , against human cholangiocarcinoma (CCA) cells. Methods : Candidone was purified from the hexane extract of Derris indica fruit. CCA cell lines, KKUM156 and KKU-M213, were treated with candidone. Sulforhodamine B (SRB) assay and acridine orange/ethidium bromide (AO/EB) staining were used to investigate the effects of candidone on cell proliferation and induction of apoptosis, respectively. The effect on cell migration was assessed by wound healing assay. Reverse transcription-quantitative polymerase chain reaction (RT-qPCR) was employed to assess the effects of candidone on the expression of genes that regulate proliferation and apoptosis. Results : Candidone exerted strong anticancer effects on CCA cells. The agent suppressed CCA cell proliferation and induced apoptotic cell death. RT-qPCR assay revealed that candidone significantly increased the expression of anti-proliferative and pro-apoptotic genes, including p21 and Bax, and decreased the expression of anti-apoptotic genes, including Bcl-2 and survivin. Moreover, candidone inhibited the migration of CCA cells induced by IGF-1. Conclusion : Candidone exhibits potent antitumor effect on CCA cells. These findings suggest that candidone is potentially suitable for the management of CCA and, therefore, warrants further investigation. Keywords : Candidone, Derris indica, Cholangiocarcinoma, Cytotoxicity, Apoptosis

The phytochemical study of the whole plant of Derris scandens (Leguminosae) has resulted in the isolation of a new isoflavone derivative, scandinone A (11), together with 11 known compounds (1-10, 12). Structural elucidations of these compounds were performed using spectroscopic methods especially 1D, 2D NMR, and mass spectral analyses. The alpha-glucosidase-inhibitory activity of the isolates was also evaluated.

Until the end of the past century, Deguelia species had been described or combined under the taxa Lonchocarpus and Derris . Although most of the species have recently been combined in some regional studies, four endemic species from the Guiana Shield (one of which also occurs in adjacent areas of Venezuela and Colombia) remain to be combined under Deguelia . Here, we propose new combinations for Lonchocarpus chrysophyllus , Lonchocarpus martynii , Lonchocarpus pictus and Lonchocarpus rufescens , with comments on their taxonomy, distribution, ecology and vernacular names. Furthermore, two new synonyms and five lectotypes are proposed here.

Two natural insecticides, rotenone and limonine caused antifeedant and growth inhibition of the red palm weevil Rhynchophorus ferrugineus larvae and adults. Rotenone was extracted from the root of Lanchocarpus sp. or Derris sp. and limonene extracted from citrus fruit oil. The concentrations of 1.5, 3, 6, 9, 12 and 15% of both insecticides were used for treatment of the sugar cane pieces. Adult stage was more tolerant than the larvae. Also, the rotenone insecticide was more effective than limonene insecticide. Moreover increasing of rotenone and limonene concentrations were reduced the food consumption and increased the larval and adult mortality. The chemical analysis was suggested the structure of rotenone is flavonoid compound and its chemical formula is C23H22O6. While the chemical nature of limonene is alkaloid with the chemical formula of C10H13O4.

Three new species of eriophyid mites from Longlin and Heng Counties, Guangxi Zhuang Autonomous Region, South China are described and illustrated: Calacarus cinerascens sp. nov. infesting Cipadessa cinerascens (Pellegr.) Hand.Mazz. (Meliaceae); Calacarus smilax sp. nov. infesting Smilax sp. (Liliaceae) and Tetra guangxiensis sp. nov. infesting Derris sp. (Leguminosae).

A molecular docking investigation has been carried out on cytotoxic prenylated flavonoids from Lonchocarpus haberi with cancer-relevant chemotherapeutic targets known to be inhibited by flavonoids. Two molecular docking programs, Molegro and ArgusDock, were used to compare the binding energies of Lonchocarpus flavonoids with other flavonoids, inhibitors, or known ligands, to aromatase (CYP 19), fatty acid synthase (FAS), xanthine oxidase (XO), cyclooxygenases (COX-1 and COX-2), lipoxygenase (LOX-3), ornithine decarboxylase (ODC), protein tyrosine kinase (PTK), phosphoinositide 3-kinase (PI3K), protein kinase C (PKC), topoisomerase II (ATP binding site), ATP binding cassette (ABC) transporter, and phospholipase A(2) (PLA). The Lonchocarpus flavonoids examined in this study exhibited docking energies comparable to or stronger than other flavonoids that had been previously shown to be effective inhibitors of these enzymes. Furthermore, prenylated flavonoids, such as the Lonchocarpus flavonoids and xanthohumol, generally showed greater binding energies than the non-prenylated flavonoids. We conclude, therefore, that the Lonchocarpus flavonoids possibly owe their cytotoxic activity by inhibition of one or more of these enzymes.

A bioassay-guided fractionation and chemical examination of antihyperglycemic root extract of Derris indica resulted in isolation and characterization of two new furanoflavanoids (1, 2) along with thirteen known compounds (3-15). Their structures were determined on the basis of extensive spectroscopic (IR, MS, 1D and 2D NMR) data analysis and by comparison with the literature data. All the compounds were tested in vitro for intestinal alpha-glucosidase inhibitory and DPPH radical activity. New compounds (1, 2) displayed moderate intestinal alpha-glucosidase inhibitory as well as free radical scavenging activity. Other compounds also displayed varying degrees of moderate intestinal alpha-glucosidase inhibitory activity. Pongamol (6) displayed potent intestinal alpha-glucosidase inhibition.

A combination of column chromatography (CC), gas chromatography (GC), thin layer chromatography (TLC) and liquid chromatography (LC) techniques were performed to analyze lipid classes, fatty acids and fat-soluble bioactives of Derris indica crude seed oil. Hexane extract of Derris indica oilseeds was found to be 56%. Level of neutral lipids in the crude seed oil was the highest, followed by glycolipids and phospholipids, respectively. Linoleic followed by α-linolenic, palmitic and oleic were the major fatty acids in the crude seed oil. The ratio of unsaturated fatty acids to saturated fatty acids was higher in neutral lipid classes than in the polar lipid fractions. The oil was characterized by a relatively high amount of phytosterols, wherein the sterol markers were β-sitosterol, campesterol and stigmasterol. γ-Tocopherol was the major tocopherol while the rest being α-tocopherol. In consideration of potential utilization, detailed knowledge on the composition of Derris indica oil is of major importance.

The gastroprotective effect of DDF (3,6-dimethoxy-6“, 6”-dimethyl-[2“, 3”: 7,8]-chromeneflavone) from Lonchocarpus araripensis Benth. (Leguminosae) on gastric damage induced by absolute ethanol (96%, 0.2 mL/mouse) and indometacin (30 mg kg−1, p.o.) in mice was investigated. Intraperitoneally administered DDF at dose levels of 50, 100 and 200 mg kg−1 markedly reduced the gastric lesions in the ethanol model by 62, 72 and 96%, and in the indometacin model by 34, 70 and 75%, respectively, as compared with misoprostol (50 μg kg−1, p.o.), the reference compound that caused lesion suppression by 67% in ethanol model and by 72% against indometacin-induced ulceration. The ED50 of DDF in reducing gastric lesions induced by ethanol and indometacin (dose of the DDF that reduced the gastric lesion area by 50% in relation to the control value) was 50.87 and 61.56 mg kg−1, respectively. Mechanistic studies were carried out at 100 mg kg−1 DDF using the ethanol model. Compared with N-acetylcysteine (750 mg kg−1, p.o.), a donor of sulfhydryls, DDF only partially replenished the ethanol-induced depletion of gastric mucosal NP-SH. Pretreatment with TRPV1 antagonist capsazepine (5 mg kg−1, i.p.) or the non-selective cyclooxygenase inhibitor indometacin (10 mg kg−1, p.o.) effectively blocked the gastroprotective effect of DDF (100 mg kg−1) against ethanol damage. Furthermore, the effect of DDF was significantly reduced in mice pretreated with L-NAME, or glibenclamide, the respective inhibitors of nitric oxide synthase and K+ATP channel activation. These data provide evidence to show that DDF affords gastroprotection against gastric damage induced by ethanol and indometacin by different and complementary mechanisms, which include involvement of endogenous prostaglandins, nitric oxide release, the activation of TRPV1 receptor or K+ATP channels, besides a sparing effect on NP-SH reserve.

Recently, we reported that the natural product derrubone exhibits Hsp90 inhibitory activity. Due to its unique architectural scaffold and proposed rapid assembly, the synthesis of this natural product was pursued with the aim of identifying structure--activity relationships. Synthesis of the natural product was accomplished in eight highly convergent steps, which led to a facile method for the construction of related compounds. Biological evaluation of derrubone and its analogues identified several compounds that exhibit low micromolar inhibitory activity against breast and colon cancer cell lines.

A stereoselective approach for synthesizing (2R,5S)-dihydroxymethyl-(3R,4R)-dihydroxypyrrolidine 1 (2,5-dideoxy-2,5-imino- d -glucitol, DGDP) was achieved using a seven-step approach starting from 2,3,4,6-tetra-O-benzyl- d -mannose (7). Key steps for the preparation of the title compound 1 involved the regioselective and diastereoselective amination of the cinnamyl anti-1,2-polybenzyl ethers 5 and 6 using chlorosulfonyl isocyanate (CSI) and ring cyclization to form the pyrrolidine ring. The reaction between anti-1,2-polybenzyl ether 5 and CSI in toluene at 0 °C afforded the corresponding anti-1,2-amino alcohol 4 as a major product with a diastereoselectivity of 16:1 in 76% yield. The mechanism underlying these reactions may be explained by the neighboring-group effect leading to the retention of stereochemistry.