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Derris eriocarpa, a traditional Chinese medicine belonging to the family of Leguminosae, is widely distributed mainly over Yunnan, Guangxi and Guizhou of China. Modern pharmacological researches on this herb showed that it had extensive bioactivities, such as promoting urination, removing dampness and cough and reducing inspissated mucus and other biological activities. The extensive studies on the chemical constituents of this plant have resulted in the isolation of triterpenoids, steroids, fatty acid and others, but the flavone compounds haven't reported before. In our further research on the ethyl acetate of this plant, nine flavone compounds were obtained by column chromatography on silica gel, Sephadex LH-20, semi-prep HPLC, polyamide column chromatography and recrystallization for separation and purification. The structures were determined on the basis of extensive spectroscopic analysis, including MS, NMR experiments and comparison with spectroscopic data in the literature, respectively, as diosmetin (1), 3, 3'-di-O-methylquercetin (2), afromosin (3), 6, 3'-dihydroxy-7, 4'-dimethoxyisoflavone (4), odoratin (5), 7, 3'-dihydroxy-8, 4'-dimethoxyisoflavone (6), 6, 4'-dihydroxy-7, 3'-dimethoxyisoflavone (7), 5, 7, 4'-trihydroxy-3, 3', 5'-trimethoxyflavone (8), and alpinumisoflavone (9). All these compounds were isolated from Derris eriocarpa How for the first time. And the in vitro assays showed that compound 2 possessed moderate inhibitory activity against human cancer cells K562 and HEL.

The high rotenone content and the rotenone crude extract of Tephrosia vogelii and Derris trifoliata were evaluated for its efficacy in the control of red imported fire (RIFA), Solenopsis invicta under both laboratory and field conditions. The acetone extracts of D. trifoliata roots and T. vogelii leaves exhibited strong toxicity to macroergate and micrergate of RIFA. When active ingredients of the crude extracts were convert to rotenone, the activity of the acetone extracts were higher than that of rotenone technical material. At the same time, the extracts showed significant inhibitory effect on walking ability and grasping ability of worker ants and stronger than the effect of 98.6% rotenone technical material. Under field conditions, the 0.01% rotenone-bait, formulated with the acetone extract of D. trifoliata roots and T. vogelii leaves, had the same control effect on RIFA as that of 0.01% fipronil-bait when treated after 30 d. The bait formulated with the extract of D. trifoliata exhibited quicker and higher effect on RIFA than that of rotenone technical material. It was showed that the acetone extracts of D. trifoliata roots and T. vogelii leaves are able to control S. invicta under both laboratory and field conditions and can be used as an effective agent against RIFA.

Rotenone is a bio-active compound extracted from Derris elliptica (locally known as ‘Tuba’ plant). It has long been used as bio-pesticide, which is more environmental friendly than the commercially available pesticides and has the potential to be used in eliminating mosquito larvae. Therefore, the objective of this study is to determine the mosquito larvicidal activity (LC50) through the usage of liquid crude extract of Derris plant root. The rotenone liquid crude extract was extracted using normal soaking extraction (NSE) method. Two different solvent ratios were used to extract rotenone namely: (A) methyl chloride: methanol (1:1) and (B) methyl chloride: methanol (1:9). The extracts were concentrated using rotary evaporator at 40 oC with vacuum pressure of 800 mbar prior to the reverse-phase high performance liquid chromatography analysis (RP-HPLC) and biological activity (LC50) study. Next, the diluted extracts were subjected to the biological activity treatment for 6 hrs. The results showed that the concentrated liquid crude extracts of methyl chloride: methanol (1:1) which contained the highest rotenone content produced the lowest treatment concentration of 0.024 mg/ml to achieve 50% mortality within 3 hrs of treatment (p

Derris eriocarpa How is an important medicinal plant, which is used as Zhuang ethnomedicine and Dai ethnomedicine to treat various diseases. One new compound, 3',4'-di-O-methylene-5-hydroxy-7-methoxy-6-isopentenyl isoflavone (1) and a known synthetic but new naturally occurring compound trans-3,4,5-trimethoxy-4'-isopentenyloxyl-stilbene (2), together with five known compounds, 5,7-dimethoxy-6-(3-methyl-2-butenyl)-4'-hydroxyl isoflavones (3), robustone (4), trans-3,4,5,4'-tetramethoxy-stilbene (5), robustic acid (6), and robustin (7) were isolated from the stem of D. eriocarpa. Spectroscopic analysis revealed the chemical structures of compounds 1-7.. Compounds 1 and 3 exhibited significant scavenging activities against 1,1-diphenyl-2-picrylhydrazyl radical and superoxide anions. Compounds 1-3 exhibited potent antiproliferative activity on Hela cells.

To investigate allelopathic activity of a leguminous mangrove plant, Derris indica, the 'Protoplasts Co-culture Method' for bioassay of allelopathy was developed using suspension culture. A suspension culture was induced from immature seed and sub-cultured in Murashige and Skoog's (MS) basal medium containing 10 μM each of 2,4-dichlorophenoxyacetic acid (2,4-D) and 6-benzyladenine (BA). The protoplasts were isolated using the separate wells method with 2% each of Cellulase RS, Driselase 20 and Macerozyme R10 in 0.4 M mannitol solution. Protoplast cultures of D. indica revealed that high concentrations of cytokinins, BA and thidiazuron, were effective for cell divisions. The co-cultures of D. indica protoplasts with recipient lettuce protoplasts using 96 multi-well culture plates were performed in MS basal medium containing 0.4 M mannitol solution and 1 μM 2,4-D and 0.1 μM BA. The protoplast density of D. indica used in co-culturing varied from 6 x 10(3) - 10(5) / mL. Very strong inhibitory allelopathic effects of D. indica protoplasts on lettuce protoplast growth were found. A similar strong inhibitory allelopathic activity of dried young leaves on lettuce seedling growth was also observed by using the sandwich method. Rotenone, which is a component of Derris root, dissolved in DMSO, was highly inhibitory on the growth of lettuce protoplasts in culture and this could be one of the causes of the strong allelopathic activity of D. indica.

The ability of cancer cells to resist to anoikis has been shown to augment cancer cell metastasis in many cancers. In search for potential substances for anti-metastatic approaches, this study aimed to investigate anoikis-sensitizing activity of lupalbigenin, extracted from Derris scandens.Human lung cancer cells were treated with non-cytotoxic concentrations of lupalbigenin in a detachment condition. Anoikis was evaluated at various time points using MTT viability assays. The effect of lupalbigenin on anchorage-independent growth was performed by soft-agar assay. The survival signaling proteins, as well as regulatory proteins of apoptosis and metastasis, were examined by western blot analysis.Lupalbigenin treatment significantly down-regulated survival proteins, including protein kinase B (pAKT/AKT) and extracellular signal-regulated kinase (pERK/ERK), as well as anti-apoptotic protein B-cell lymphoma 2 (BCL-2), resulting in the enhancement of the cellular response to anoikis and the decrease of growth and survival in an anchorage-independent condition.Lupalbigenin sensitizes detachment-induced cell death in human lung cancer cell through down-regulation of pro-survival proteins.

Rotenone is one of the prominent insecticidal isoflavonoid compounds which can be isolated from the extract ofDerrissp. plant. Despite being an effective compound in exterminating pests in a minute concentration, procuring a significant amount of rotenone in the extracts for commercialized biopesticides purposes is a challenge to be attained. Therefore, the objective of this study was to determine the best ionic liquid (IL) which gives the highest yield of rotenone. The normal soaking extraction (NSE) method was carried out for 24 hrs using five different types of binary solvent systems comprising a combination of acetone and five respective ionic liquids (ILs) of (1) [BMIM] Cl; (2) [BMIM] OAc; (3) [BMIM] NTf2; (4) [BMIM] OTf; and (5) [BMPy] Cl. Next, the yield of rotenone, % (w/w), and its concentration (mg/mL) in dried roots were quantitatively determined by means of RP-HPLC and TLC. The results showed that a binary solvent system of [BMIM] OTf + acetone was the best solvent system combination as compared to other solvent systems (P<0.05). It contributed to the highest rotenone content of 2.69 ± 0.21% (w/w) (4.04 ± 0.34 mg/mL) at 14 hrs of exhaustive extraction time. In conclusion, a combination of the ILs with a selective organic solvent has been proven to increase a significant amount of bioactive constituents in the phytochemical extraction process.

Background: The anti-malarials quinine and artemisinin were isolated from traditionally used plants (Cinchona spp. and Artemisia annua, respectively). The synthetic quinoline anti-malarials (e.g. chloroquine) and semi-synthetic artemisinin derivatives (e.g. artesunate) were developed based on these natural products. Malaria is endemic to the Amazon region where Plasmodium falciparum and Plasmodium vivax drug-resistance is of concern. There is an urgent need for new anti-malarials. Traditionally used Amazonian plants may provide new treatments for drug-resistant P. vivax and P. falciparum. Herein, the in vitro and in vivo antiplasmodial activity and cytotoxicity of medicinal plant extracts were investigated. Methods: Sixty-nine extracts from 11 plant species were prepared and screened for in vitro activity against P. falciparum K1 strain and for cytotoxicity against human fibroblasts and two melanoma cell lines. Median inhibitory concentrations (IC50) were established against chloroquine-resistant P. falciparum W2 clone using monoclonal anti-HRPII (histidine-rich protein II) antibodies in an enzyme-linked immunosorbent assay. Extracts were evaluated for toxicity against murine macrophages (IC50) and selectivity indices (SI) were determined. Three extracts were also evaluated orally in Plasmodium berghei-infected mice. Results: High in vitro antiplasmodial activity (IC50 = 6.4-9.9 μg/mL) was observed for Andropogon leucostachyus aerial part methanol extracts, Croton cajucara red variety leaf chloroform extracts, Miconia nervosa leaf methanol extracts, and Xylopia amazonica leaf chloroform and branch ethanol extracts. Paullinia cupana branch chloroform extracts and Croton cajucara red variety leaf ethanol extracts were toxic to fibroblasts and or melanoma cells. Xylopia amazonica branch ethanol extracts and Zanthoxylum djalma-batistae branch chloroform extracts were toxic to macrophages (IC50 = 6.9 and 24.7 μg/mL, respectively). Andropogon leucostachyus extracts were the most selective (SI >28.2) and the most active in vivo (at doses of 250 mg/kg, 71 % suppression of P. berghei parasitaemia versus untreated controls). Conclusions: Ethnobotanical or ethnopharmacological reports describe the anti-malarial use of these plants or the antiplasmodial activity of congeneric species. No antiplasmodial activity has been demonstrated previously for the extracts of these plants. Seven plants exhibit in vivo and or in vitro anti-malarial potential. Future work should aim to discover the anti-malarial substances present. © 2015 Lima et al.

The extraction of active compounds from plants is one of the most critical steps in the commercial development of natural products for medicinal, herbicidal or pesticidal use. The focus of this study was to compare conventional maceration and pressurized liquid extraction (PLE) techniques for the efficient extraction of rotenone from the stem and root of Derris elliptica Benth and Derris malaccensis Prain. The effects of experimental variables, such as solvent, temperature and pressure, on PLE efficiency have been studied. Chloroform was determined to be a good extraction solvent (rotenone content 40.6%, w/w) compared to commonly used solvent, 95% ethanol (rotenone content 15.0%, w/w). The optimal conditions for PLE were 50 degrees C and 2000 psi. PLE showed higher extraction efficiency (rotenone content 46.1%, w/w) as compared with conventional maceration method (rotenone content 40.6%, w/w). The order of rotenone content found in crude extract obtained by optimized method from the highest to the lowest was root (46.1%, w/w) and stem (9.4%, w/w) of D. elliptica and stem of D. malaccensis (5.2%, w/w), respectively. Moreover, the results from this study indicated that PLE was considerably less time and solvent consuming (30 min, 3 ml/g of dried sample) than the conventional maceration techniques (72 h, 10 ml/g of dried sample).

Flavonoids (1-4), together with ten known compounds (5-14) were isolated from the stems and roots of the mangrove plant Derris indica. Their chemical structures were elucidated by analysis of their spectroscopic data. All compounds except compounds 2 and 6 exhibited antimycobacterial activity with minimum inhibitory concentrations (MIC) between 6.25 and 200 microg/mL.

The crude alcoholic extracts of various parts of five different Bangladeshi mangrove plants (Amoora cucullata, Caesalpinia bonducella, Cerbera odollam, Derris uliginosa and Sonneratia caseolaris) were screened in-vitro for anti-oxidant activity using the 1,1-diphenyl-2-picryldydrazyl-hydrate (DPPH) free radical scavenging assay. Of all of them, the ethanolic extracts of the leaves of Derris uliginosa and Sonneratia caseolaris showed potential antioxidant activity (: 94.406 and 26.30 mg/ml respectively) whereas the ethanolic extracts of aerial parts of Derris uliginosa, barks of Cerbera odollam and leaves and stems of Caesalpinia bonducella showed moderate activity (: 125.89, 211.35 and 301.99 mg/ml respectively). Mild anti-oxidant activity was observed with the methanolic extract of leaves of Amoora cucullata and ethanolic extracts of fruits of Cerbera odollam.

We have investigated the anti-inflammatory and antimicrobial effect of the lectin from Lonchocarpus sericeus seeds (LSL) in a model of infectious peritonitis in adult Wistar rats. Animals were treated with saline or LSL (10mg kg−1, i.v) immediately and 6h after the induction of peritonitis via cecal ligation and single puncture. Twelve hours after surgery, animals were killed and the infectious process was monitored by total and differential count of cells from blood and peritoneal washing liquid, adenosine deaminase activity, antibiogram and the number of viable bacteria of the peritoneal cavity. LSL treatment decreased the inflammatory response evoked by the induction of peritonitis, as seen by the inhibition of neutrophil migration into peritoneal cavities, leucocytosis and reduction of adenosine deaminase activity in the peritoneal fluid. All these effects were reversed by the lectin association to N-acetyl-glucosamine. LSL in-vitro did not show any antimicrobial action, but promoted a marked decrease of the viable bacterial population in peritoneal cavities. In conclusion, LSL inhibited the inflammatory response and the bacterial colonization of infectious peritonitis in rats.

From the acetone extract of the roots of Derris trifoliata an isoflavonoid derivative, named 7a-O-methyldeguelol, a modified rotenoid with an open ring-C, representing a new sub-class of isoflavonoids (the sub-class is here named as rotenoloid), was isolated and characterised. In addition, the known rotenoids, rotenone, deguelin and alpha-toxicarol, were identified. The structures were determined on the basis of spectroscopic evidence. Rotenone and deguelin were identified as the larvicidal principles of the acetone extract of the roots of Derris trifoliata.

Fractionation of the aqueous extract of Derris scandens stems extract using tests for eicosanoid inhibition resulted in the isolation of three isoflavonoids, genistein, its 7- O-alpha-rhamno(1-->6)-beta-glucosyl glycoside, a new compound, and two known isoprenyl derivatives 3'-gamma,gamma-dimethylallylweighteone and scandenin. The isoprenylated compounds showed a high inhibitory effect on eicosanoid production in vitro but HPLC analysis showed that the genistein accounted for most of the activity of the total extract. Antioxidant studies showed that genistein and the isoprenylated compounds showed activity comparable to standard antioxidants. Genistein and its glycoside demonstrated no cytotoxicity in the MTT test but the prenylated compounds showed some toxicity and also increased LDH release from polymorphonucleocytes, at concentrations much greater than would be encountered in an aqueous extract of D. scandens.

A study of the chemical constituents of the stems of Derris trifoliata Lour. (Leguminosae) led to the isolation and identification of one new rotenoid, 6aalpha,12aalpha-12a-hydroxyelliptone ( 3), together with five other known rotenoids. In a search for novel cancer chemopreventive agents (anti-tumor promoters), we carried out a primary screening of five of the rotenoids isolated from the plant for their inhibitory effects on Epstein-Barr virus early antigen (EBV-EA) activation induced by 12- O-tetradecanoylphorbol 13-acetate (TPA) in Raji cells. The inhibitory activity of 3 was found to be equivalent to that of beta-carotene without any cytotoxicity. Deguelin ( 4) and alpha-toxicarol ( 5) exhibited a marked inhibitory effect on mouse skin tumor promotion in an in vivo two-stage carcinogenesis test. This investigation indicated that rotenoids might be valuable anti-tumor promoters.

Rotenone and rotenoids (deguelin, beta-rotenolone (12a beta-hydroxyrotenone), tephrosin (12a beta-hydroxydeguelin), 12a alpha-hydroxyrotenone, and dehydrorotenone) were determined in cubè resins and formulations. Cubè resins from Lonchocarpus contain large quantities of deguelin (ca. 21.2%) and smaller quantities of tephrosin (ca. 3.5%) and beta-rotenolone (ca. 3.0%). The composition of commercial formulations may present very different rotenoid contents depending on the extracts used to prepare them. Because these rotenoids also present insecticide activity, the efficacy of these formulations may be very different. The storage stability and photodegradation of some rotenone formulations were studied. Rotenone and rotenoids are very sensitive to solar radiation, which degrades them rapidly, with half-lives in the order of a few tens of minutes. Some formulations show greater disappearance rates than that of cubè resin, indicating that not much attention has been paid to protecting the active ingredients from photodegradation in the formulation. A study on the residues on olives was also carried out to assess not only the rotenone content, but also that of the main rotenoids. At harvest, the residues of deguelin, tephrosin, and beta-rotenolone were 0.10, 0.06, and 0.10 mg/kg, respectively, very similar to rotenone (0.08 mg/kg), and though a few data indicate similar acute toxicity values for deguelin, only rotenone is taken into consideration in the legal determination of the residue.

The leaves of Acanthus ebracteatus, stembark of Oroxylum indicum and the stems of Cryptolepis buchanani and Derris scandens are used as traditional remedies in Thailand for arthritis. Aqueous and alcoholic extracts were tested using three different in vitro systems for effects relevant to anti-inflammatory activity. The aqueous extracts of O. indicum and D. scandens significantly reduced myeloperoxide release. Eicosanoid production was reduced only by the aqueous extracts of A. ebracteatus and D. scandens. D. scandens extract showed potent inhibitory activity against generation of leukotriene B(4) and also displayed antioxidant activity. In the rat hind paw edema test, D. scandens extract showed significant activity when given intraperitoneally but did not produce a significant reduction when given orally. The results therefore supported to some extent the traditional use of D. scandens for arthritic conditions and provided slight indication of activity which could explain the use of O. indicum and A. ebracteatus. No relevant activity was demonstrated in any of the tests for C. buchanani extracts.

Traditional physicians in and around Kotagiri village near Ootacamund, use a mixture of powdered roots of Cassia occidentalis, Derris brevipes variety coriacea and Justicia simplex to control female fertility. A mixture of powdered roots of these three plants, powdered root of Derris brevipes variety coriacea and its ethanolic extract were screened for antifertility activity in proven fertile female rats at 200 and 600 mg/kg body weight, respectively and given orally on D1–7 of pregnancy. Both doses of the root powder of Derris brevipes variety coriacea showed 50% anti-implantation activity and also a significant reduction in the number of litters born. The ethanolic extract exhibited 40% anti-implantation activity when given orally at 600 mg/kg body weight. The rats, which continued their pregnancy, did not deliver any litters after their full term. Hence, the combined antifertility (anti-implantation and abortifacient) activity of the ethanolic extract was 100%. The results suggest that the ethanolic extract possesses more abortifacient type effect than the anti-implantation activity. The ethanolic extract also exhibited weak estrogenic activity when given alone and tested in immature ovariectomised female albino rats. But, when given along with ethinyl estradiol, it exhibited slight antiestrogenic activity. Histological and biochemical estimations were carried out to confirm this.

Derris Lour. is revised for the Flora Malesiana region. In the introduction comments are given on some characters and the seedlings of D. trifoliata Lour. are described. The introduction is followed by a section ‘Notes on species’ in which the varieties of D. elegans Graham ex Benth. are described, including a new one from Celebes (var. celebica Adema) and a new one from Malaysia, Java, Borneo, the Philippines and the Moluccas (var. korthalsiana (Blume ex Miq.) Adema). Several other species are discussed at some length. A key to the species of Derris in Malesia is presented. The paper concludes with notes on aberrant specimens and excluded species.

Aqueous suspension of ethanol extracts of Derris (Lonchocarpus) urucu (Leguminosae), collected in the state of Amazonas, Brazil, were tested for larvicidal activity against the mosquito Aedes aegypti (Diptera:Culicidae). The aim of this study was to observe the alterations of peritrophic matrix in Ae. aegypti larvae treated with an aqueous suspension of D. urucu extract. Different concentrations of D. urucu root extract were tested against fourth instar larvae. One hundred percent mortality was observed at 150 microg/ml (LC(50) 17.6 microg/ml) 24 h following treatment. In response to D. urucu feeding, larvae excreted a large amount of amorphous feces, while control larvae did not produce feces during the assay period. Ultrastructural studies showed tha larvae fed with 150 microg/ml of D. urucu extract for 4 h have an imperfect peritrophic matrix and extensive damage of the midgut epithelium. Data indicate a protective role for the peritrophic matrix. The structural modification of the peritrophic matrix is intrinsically associated with larval mortality.

Rotenone, a natural compound derived from plants of the genera Derris and Lonchocarpus, is used worldwide as a pesticide and piscicide. This study aims to assess short-term toxicity of rotenone to early-life stages of the fish Danio rerio and Poecilia reticulata using a wide and integrative range of biomarkers (developmental, biochemical, behavioral, and histopathological). Moreover, the species sensitivity distribution (SSD) approach was used to compare rotenone acute toxicity to fish species. Toxicity tests were based on the OECD protocols, fish embryo toxicity test (for D. rerio embryos), and fish acute toxicity test (for P. reticulata juveniles). D. rerio embryos were used to estimate lethal concentrations and analyze embryonic and enzymatic alterations (activity of catalase, glutathione-S-transferase, and cholinesterase), while P. reticulata juveniles were used for the assessment of histological damage in the gills and liver. Rotenone induced significant mortality in zebrafish embryos with a 96-h lethal concentration 50% (LC50) = 12.2 μg/L. Rotenone was embryotoxic, affecting the development of D. rerio embryos, which showed cardiac edema; tail deformities; loss of equilibrium; and a general delay characterized by lack of tail detachment, delayed somite formation, yolk sac absorption, and lack of pigmentation. Biochemical biomarker inhibition was observed for concentrations ≥1 μg/L for CAT and glutathione-S-transferase (GST) and for cholinesterase (ChE) in concentration from 10 μg/L. Behavioral changes were observed for P. reticulata juveniles exposed to concentrations equal to or above 25 μg/L of rotenone; moreover, histological damage in the liver and gills of fish exposed to concentrations equal to or above 2.5 μg/L could be observed. A hazard concentration 5% (HC5) of 3.2 μg/L was estimated considering the acute toxicity data for different fish species (n = 49). Lethal and sublethal effects of rotenone raise a concern about its effects on nontarget fish species, especially because rotenone and its metabolite rotenolone are frequently reported in the microgram range in natural environments for several days after field applications. Rotenone should be used with caution. Given the high toxicity and wide range of sublethal effects here reported, further studies in a chronic exposure scenario are recommended.

Background Antidiabetic activity of Derris reticulata extract on alloxan-induced diabetic rats has been reported. The extract was found to lower blood glucose and inhibit intestinal glucose absorption. The aim of this study was to further investigate mechanisms underlying the antihyperglycemic activity of D. reticulata extract in vitro. Methods The aqueous extract was obtained from D. reticulata stem. Phytochemical screening, total phenolic, and flavanoid contents were examined. ABTS and DPPH scavenging assays, and FRAP method were used to determine in vitro antioxidant activities. Measurement of cell viability on alloxan-induced cellular damage was performed in the insulin-secreting RINm5F cells by MTT assay. The effects of the extract on α-glucosidase activity and insulin release were studied. In addition, sub-chronic toxicity test in rats was also conducted. Results The results revealed that the extract, which consisted of terpenoids, saponins, tannins and flavonoids, possessed moderate radical scavenging activities. Pre-treatment of RINm5F cells with the extract was also found to exert moderate, but significant, in vitro protection against alloxan, an oxidative stress producing agent. Unlike glibenclamide, the extract did not stimulate insulin secretion. However, the extract was found to inhibit α-glucosidase activity similar to acarbose. It was found that in sub-chronic toxicity studies D. reticulata extract did not cause mortality or produce any remarkable haematological, biochemical and histopathological adverse effects in rats. Conclusions The data suggest that the possible mechanisms underlying antihyperglycemic activity of D. reticulata extract are cytoprotective effect on pancreatic cells, presumably by its antioxidant activity, and inhibition of α-glucosidase. Sub-chronic toxicity study also provides scientific evidence to corroborate the safety of this plant as an alternative antidiabetic agent.

Trypanosoma evansi, the causative agent of "surra", infects many species of wild and domestic animals worldwide. In the current study, the aqueous and ethanolic extracts of six medicinal plants, namely, Aquilaria malaccensis, Derris elliptica, Garcinia hombroniana, Goniothalamus umbrosus, Nigella sativa, and Strobilanthes crispus were screened in vitro for activity against T. evansi. The cytotoxic activity of the extracts was evaluated on green monkey kidney (Vero) cells using MTT-cell proliferation assay. The median inhibitory concentrations (IC50) of the extracts ranged between 2.30 and 800.97 μg/ml and the median cytotoxic concentrations (CC50) ranged between 29.10 μg/ml and 14.53 mg/ml. The aqueous extract of G. hombroniana exhibited the highest selectivity index (SI) value of 616.36, followed by A. malaccensis aqueous extract (47.38). Phytochemical screening of the G. hombroniana aqueous extract revealed the presence of flavonoids, phenols, tannins, and saponins. It is demonstrated here that the aqueous extract of G. hombroniana has potential antitrypanosomal activity with a high SI, and may be considered as a potential source for the development of new antitrypanosomal compounds.

Two new compounds, derrivanone (1) and derrischalcone (2), were isolated from the crude hexane extract of the fruits of Derris indica. In addition, 14 known compounds were isolated from the fruits of this plant. Chalcones 2–4 showed strong cytotoxicity against cholangiocarcinoma cell line (M156) and human hepatoma HepG2 cells. In addition, flavanones 15 and 16 exhibited potent and high cytotoxic efficacy.

An extract of a rotenone-containing plant yam bean, Pachyrhizus erosus (L.) Urban, seeds was tested against the diamondback moth, Plutella xylostella (L.) in a greenhouse to determine its potential as an oviposition deterrent and compared with coumarin and rutin, known as diamondback moth oviposition deterrent compounds, rotenone, and an extract of Peruvian cube root, at a concentration of 0.5% (w/v). Oviposition deterrent index (ODI) was used to determine effects of extracts or compounds in inhibiting oviposition of diamondback moth. Coumarin showed a stronger deterrent effect than the yam bean seed extract with a higher ODI value. On the contrary, rotenone, rutin, and the cube root extract, containing 6.7% (w/w) of rotenone, showed no significant deterrent effects having low or negative ODI values, suggesting that the deterrent effect of the yam bean seed extract is not due to rotenone content of the yam bean seeds. The extract of yam bean seed and coumarin partially deterred the moth from laying eggs on treated leaves in a concentration-dependent manner. The effective concentration for 50% deterrency of coumarin and the yam bean seed extract were 0.11 and 0.83% (w/v), respectively. However, the yam bean seed extract showed a residual deterrent effect on the moth even at 3 d after the treatment and is probably because of its low volatile nature. A long-term deterrency of the yam bean seed extract is an advantage over coumarins. Both the yam bean seed extract and coumarin deterred diamondback moth from laying eggs in total darkness, indicating their nonvisual deterrent effect. This made the extract an effective deterrence to diamondback moth in light and in darkness. To conclude, this study revealed the potential of the crude extract of the yam bean seed to prevent diamondback moth from ovipositing on its plant host.

Sixty five methanolic extracts of Sumatran rainforest plants representing 63 species of 21 families were assayed in vivo for antinematodal activity against Bursaphelenchus xylophilus using our cotton ball-fungal mat method. Extracts of 27 plants species from 14 families exhibited antinematodal activity, while 37 species were inactive. Among them, three extracts of Bischofia javanica, Knema hookeriana and Areca catechu exhibited very strong activity at minimum effective dose (MED ) of 0.7 mg/cotton ball (mg/bl.). Eight extracts from Allamanda cathartica, Ervatamia corymbosa, Hoya diversifolia, Bischofia javanica, Derris malacensis, Melastoma melabathricum, Ophiorriza konsteleary and Brucea sumatrana also showed strong activity (MED, 5 mg/bl.).

The inhibitory effects of essential oils extracted from 10 Indian plants were evaluated against five fungi. The plants used for extraction of essential oils were six species of the genus Eucalyptus and Ocimum basilicum, Prosopis cineraria and Derris indica. The fungi used in the experiments were Fusarium solani, F. oxysporum, F. pallidoroseum, F. acuminatum and F. chlamydosporum. The susceptibility of the Fusarium species was tested by the paper disc method and the serial dilution technique. The results were compared with the inhibitory effects of miconazole on the fungi. The essential oils extracted from the Eucalyptus species markedly inhibited fungal growth. Prosopis cineraria did not show inhibiting properties. Among the fungi, F. oxysporum proved to be the most resistant species.

From the leaves of Derris trifoliata, collected in Okinawa, 15 glycosidic compounds were isolated and identified.

Two new pyranoflavanones, 2‴,3‴-epoxylupinifolin and dereticulatin, together with the known flavonoid lupinifolin, were identified from the stems of Derris reticulata . The structures and NMR spectral data were assigned by the use of 2D NMR technology and chemical transformations. All of the isolates showed cytotoxic activity in the P-388 cell line.

Derris Lour. (family Fabaceae/tribe Millettieae) is a quite well-known legume genus as many species are a source of Rotenone toxin, a commercial organic insecticide and fish poison used in many countries. The genus is characterized mainly by its indehiscent, flat, thin but leathery pods with usually wing(s) along the suture(s). In the tribe Millettieae, however, there are several plants in the tropical areas of the old and new world which have similar pods and other morphological characters comparable to Derris. They all are called Derris-like taxa (or Derris-like plants) in this thesis. In the course of time, different generic circumscriptions of these plants were proposed by various taxonomists. The main objectives of this thesis are to clarify the relationships between species and genera within this complex group of Derris-like taxa [mainly focused on the old-world Asian genera: Aganope, Brachypterum and Derris (+Paraderris)] and to provide a new classification which reflects the evolutionary and biogeographic relationships of these plants.

Study of the chemical constituents of the stems of Derris trifoliata Lour. (Leguminosae) collected in Singapore led to the isolation and identification of three known and two new rotenoid derivatives. The new derivatives, named derrisfolin A (1) and B (2), inhibited nitric oxide production in murine macrophage-like RAW 264.7 cells stimulated with interferon-gamma and lipopolysaccharide.

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 D1 (3), secundiflorol I (4), 6a-hydroxymaackiain (5) and pisatin (6). The structures of these compounds were determined by analysis of their spectroscopic data.

In the present study, the antioxidant and analgesic potential of the ethanolic extract of the leaves of Derris trifoliata was evaluated. The free radical scavenging activity of the crude extract on the stable radical 1, 1-diphenyl-2-picrylhydrazyl (DPPH) was determined by comparing the DPPH inhibitory capacity of the extract. In the quantitative assay, Derris trifoliata extract displayed a free radical scavenging activity in the DPPH assay (IC50 = 19 ?g/ml) which is comparable to that of ascorbic acid (IC50 = 7.80 ?g/ml), a well-known standard antioxidant. The analgesic responses of the given samples of extracts were evaluated using the Tail immersion method. In the analgesic activity test, extract at dose of 200 mg/kg and 400 mg/kg exhibited significant (P

To study the brine shrimp lethal activities of the roots and stems from Derris trifoliata.The biological activity of the athyl acetate extract was tested by the 2nd-instar of Artemia franciscana by the method of Silica gel column chromatography, Sephadex LH-20 column chromatography, Semipreparative HPLC, and their structures were elucidated by spectral analysis.Eleven compounds were isolated from the athyl acetate extract, and LD50 s of 12a-hydroxyrotenone, tephrosin, rotenone and deguelin were 0.365, 0.236, 0.060 and 0.734 microg/mL, respectively.The results of bioassay show that 12a-hydroxyrotenone, tephrosin,rotenone and deguelin have strong brine shrimp lethal activity.

Two new flavonoids, (2 S)-3′,4′,5′-trimethoxyflavanone (1) and 2′-hydroxy-2,4-dimethoxy-4′- O-[( E)-3,7-dimethyl-2,6-octadienyl]chalcone (2), together with a known pterocarpene, flemichapparin B (3), and a known rotenoid, dehydrodeguelin (4), were isolated from the seeds of Derris scandens. Their structures were determined by means of extensive 1D and 2D NMR spectral studies.

A new acetophenone, 1-[2,4-dihydroxy-5-(3-methylbut-2-enyl)phenyl]ethanone (1) was isolated from the root bark of Derris indica, along with 3,7,-dimethoxy-3',4'-methylenedioxyflavone (desmethoxykanugin) (2), 5-methoxyfurano[4",5":6,7]flavone (pinnatin) (3), and 3'-hydroxyfurano[4",5":7,8]flavone (pongol) (4). The structures of these compounds were established by means of chemical and spectral studies. The occurrence of this prenylated acetophenone in D. indica is of biogenetic and chemotaxonomic significance.

The use of herbal products as radiosensitizers is a promising approach to increase the efficacy of radiotherapy. However, adverse effects related to the use of herbal medicine on radiotherapy are not well characterized. The present study concerns the impact of Derris scandens Benth extract on the radiosensitivity of Hep-2 laryngeal cancer cells. Pretreatment with D. scandens extract prior to gamma irradiation significantly increased clonogenic survival and decreased the proportion of radiation-induced abnormal nuclei of Hep-2 cells. Furthermore, the extract was found to enhance radiation-induced G2/M phase arrest, induce Akt activation, and increase motility of Hep-2 cells. The study thus indicated that D. scandens extract potentiates radioresistance of Hep-2 cells, further demonstrating the importance of cellular background for the adverse effect of D. scandens extract on radiation response in a laryngeal cancer cell line.

International audience; 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.

The aim of this study was to reveal the pyridine metabolism in leaves of two mangrove legumes, Derris indica (= Millettia pinnata or Pongamia pinnata) and Caesalpinia crista. Radioactivity from [carbonyl-14C]nicotinamide supplied exogenously to young leaf disks was recovered in nicotinic acid, nicotinic acid mononucleotide, NAD, NADP, nicotinamide mononucleotide and trigonelline. These mangrove species, especially D. indica, have strong ability to convert nicotinamide to trigonelline, but not to nicotinic acid glucoside. The endogenous trigonelline content in leaves of D. indica was more than 830 microg/g dry weight. This value is 5-12 times greater than that in leaves of Glycine max. There was little short-term effect of 250 and 500 mM NaCl (equivalent to ca. 50% and 100% sea water) on nicotinamide metabolism.

In this revision of the Thai species of the genus Derris and the morphologically similar genera, Aganope and Paraderris, all currently recognized species are enumerated. Two new species, Derris glabra Sirichamorn and Derris pseudomarginata Sirichamorn, are described and illustrated. Keys to the genera and species are provided, together with descriptions and notes for all taxa.

Tandonella dolichoides sp. nov. on Dolichos biflorus and Sclerographium indicum sp. nov. on Derris scandens are described, illustrated and compared with known species.

A new rotenoid, derrisin (1), together with 10 known rotenoids (2-11) were isolated from the roots of Derris malaccensis Plain. The structure of 1 was elucidated by spectroscopic analysis. Nine of the isolated rotenoids (3-11) showed antibacterial activity against Helicobacter pylori.

Estudos com inseticidas botânicos vêm ganhando espaço como alternativa no Manejo Integrado de Pragas. Conduziu-se este trabalho com o objetivo de avaliar o efeito de extratos aquosos de folhas e frutos da espécie Clibadium sylvestre, e folhas e raízes da espécie Derris amazonica nas concentrações 0, 1, 2, 4 e 8%, no controle do pulgão Myzus persicae (Hemiptera: Aphididae). Foram conduzidos quatro ensaios, dois testes de preferência sem chance de escolha e dois testes de preferência com chance de escolha, totalizando nove tratamentos com cinco repetições. Foi realizada a triagem fitoquímica das folhas e dos frutos da espécie C. sylvestre e das folhas e das raízes de D. amazonica. As avaliações de mortalidade, número de ninfas e índice de deterrência dos insetos, foram realizadas 24, 48 e 72 horas após a aplicação dos extratos. Os extratos aquosos do fruto do C. sylvestre nas concentrações testadas apresentaram maior mortalidade frente à testemunha, na análise do número de ninfas, o extrato aquoso do fruto do C. sylvestre a 8% apresentou maior eficiência que os demais tratamentos. O extrato da folha de D. amazonica na concentração 1% apresentou maior mortalidade e menor número de ninfas que os demais tratamentos. Os extratos da raiz de D. amazonica aumentaram a mortalidade em todas as concentrações testadas e a concentração 8% da raiz de D. amazonica, apresentou menor número de ninfas. Todos os tratamentos testados apresentaram efeito deterrente. O período de 72 horas foi o que apresentou maior efeito dos extratos, das duas espécies estudadas sobre os insetos. Studies with botanical insecticides have become more popular as an alternative to Integrated Pest Management. The purpose of this study was to evaluate the effect of leaf and fruit aqueous extracts, from the species Clibadium sylvestre, and leaves and root of Derris amazonica species at concentrations of 0, 1, 2, 4 and 8%, in the control of the aphid Myzus persicae (Hemiptera: Aphididae). Four experiments were conducted; two tests with choice preference and two tests with no choice preference, giving nine treatments and five repetitions. Phytochemical screening was carried out from the leaves and fruit of the species C. sylvestre and leaves and root of D. amazonica. Evaluations of mortality, number of nymphs, and deterrence index of the insects were conducted 24, 48 and 72 h after the application of the extracts. The aqueous extracts tested from C. sylvestre fruit concentrations had the highest mortality compared to the control; in the analysis of the number of the nymphs, the aqueous extract from fruit at 8% concentration had a higher efficiency than the other treatments. The D. amazonica leaves extract at 1% concentration showed the highest mortality and the lowest number of nymphs. The D. amazonica root extracts increased mortality at all concentrations tested, and the 8% concentration had the fewest nymphs. All treatments showed a deterrent effect. The 72 h period showed the greatest effect of the extracts, on two species of insects.

Some concerns, especially environmental ones, lead the researchers to find new avenues of insect control in agriculture. Considering negative effects of synthetic pesticides especially on non-target organisms caused a general perception that natural compounds are better products or Generally Regarded As Safe (GRAS) (Scott et al., 2003). So, researches has been concentrated on the plant kingdom for solutions leading to the production of a myriad of secondary compounds that can have toxic, growth reducing, and antifeedant properties against insects (Berenbaum & Zangerl, 1996). The use of plant extracts (botanical insecticides) to protect crops and stored products is as old as crop protection. Indeed, prior to the development and commercial success of synthetic insecticides beginning in the 1940s, botanical insecticides were major weapons in the farmer’s arsenal against crop pests (Isman, 2008). Four major types of botanical insecticides are being used for insect control including pyrethrum, rotenone, neem, and essential oils along with three others in limited use (Isman, 2006). Pyrethrum is an oleoresin extracted from the dried flowers of the pyrethrum daisy, Tanacetum cinerariaefolium (Asteraceae) that its active ingredients are three esters of chrysanthemic acid and three esters of pyrethric acid (Isman, 2006). The insecticidal action of the pyrethrins is characterized by a rapid knockdown effect, particularly in flying insects, and hyperactivity and convulsions in most insects. These symptoms are the result of the neurotoxic action of the pyrethrins, which block voltage-gated sodium channels in nerve axons. Azadirachtin is an extraction from Indian neem tree, Azadirachta indicahas that has two profound effects on insects (Schmutter, 2002). Azadirachtin, apart from its antifeedant effects on insects, inhibited the synthesis and release of ecdysteroids from the prothoracic gland resulting incomplete ecdysis in immature insects and sterility in adult females (Isman, 2006). Rotenone is a type of isoflavonoids extracted from the roots or rhizomes of the tropical legumes like Derris, Lonchocarpus, and Tephrosia (Isman, 2006). Rotenone is a mitochondrial poison by blocking the electron transport chain leading to inhibition of energy production (Hollingworth et al., 1994). Acetogenin extracts from seeds of Annona squamosa known as annonin I, or squamocin, and a similar compound, asimicin were isolated from the bark of the American pawpaw tree, Asimina triloba (Johnson et al., 2000). Although, there are many plant extracts widely use against insects but here one of them, Artemisia, is discussed. The genus Artemisia is a member of a large plant family Asteracea

A new prenylated isoflavone, pomiferin-4'-O-methyl ether, and a new prenylated chalcone, 2',4'-dihydroxy-4-methoxy-3'-(2-hydroxy-3-methylbut-3-enyl)chalcone, together with four known flavonoids, were isolated from the leaves of Derris malaccensis. All isolated compounds were evaluated for their cytotoxicity.

Four species of Prunella L. (Prunella vulgaris L., Prunella laciniata L., Prunella grandiflora L. and Prunella orientalis Bornm.) belong to the family of Lamiaceae and representing popular Western and Chinese herbal medicine were examined for the content of phenolic compounds. Phenolic acids (rosmarinic acid, caffeic acid, ferulic acid, chlorogenic acid, protocatechuic acid), flavonoids (rutin, quercetin) in different quantitative proportions depending on extracts were determined by the rapid, selective and accurate method combining solvent/acid hydrolysis extraction and high performance liquid chromatography-diode array detection (HPLC-DAD). Water, methanol, butanol, acetonitrile, ethyl acetate, hexane and their acidic solutions were used to examine the efficiency of different solvent systems for the extraction of phenolic compounds. Acid hydrolysis extraction was established as the most suitable extraction method for phenolic compounds.

The molluscicidal activity of crude extracts from five highly potential plants, Annona squamosa seed, Nerium indicum Leaves, Stemona tuberose root, Cyperus rotundus corm and Derris elliptica root was assessed to Pomacea canaliculata. D. elliptica root and C. rotundus corm extracts showed the highest toxicity against 3-month old snails which have LC50 as 23.68 +/- 2.96 mg/l and 133.20 +/- 7.94 mg/l, respectively. The C. rotundus corm extracts were chosen for detoxification enzyme in vivo assay which shows esterase and glutathione S-transferase activity in stomach, intestinal tracts and digestive glands of survival treated P. canaliculata were inhibited.

A new method for determination of total phenolic content of four Prunella L. species was developed by immobilizing horseradish peroxidase (HRP) on styrene-divinylbenzene-polygluteraldehyde (STY-DVB- PGA) polymer. The method is based on the spectrophotometric measurement of the final quinone-imine colored product, absorbing at 510 nm, by horseradish peroxidase oxidation in presence of hydrogen peroxide. The effects of solvents were investigated for the extraction of phenolic compounds in Prunella L. plants. HRP was covalently attached on the STY-DVB-PGA with 90% efficiency at optimum immobilization conditions. The total phenol contents ranged from 4 to 152 mg GAE per g of dried sample for pure solvents and ranged from 19 to 763 mg GAE per g of dried sample for acidic extracts using the immobilized enzymatic method. STY-DVB-PGA beads are a good potential support for the immobilization of HRP enzyme and can be used for determination of the total phenolic content of plants. In the analysis of four Prunella L. species, high correlations were obtained between enzymatic and Folin methods, supporting the validity of the enzymatic method proposed. The enzymatic (free/immobilized) methods are more specific and rapid than the Folin method. Acidic solvents are more effective than pure solvents for extraction of phenolic compounds in Prunella L. species.