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The activity of β-caryophyllene oxide as either a contact or noncontact repellent was evaluated against two laboratory strains (Aedes albopictus and Anopheles dirus) using an excito-repellency test system. N, N-Diethyl-3-methylbenzamide (DEET) was used as a standard reference baseline for comparative purposes. β-Caryophyllene oxide and DEET were tested at concentrations of 0.1, 0.25, 0.5 and 1.0% (v/v). In addition, the phototoxic and genotoxic effects of β-caryophyllene oxide were investigated on Balb/c 3T3 mouse fibroblasts (3T3-L1) and Chinese hamster ovary cell line (CHO-K1). The results demonstrated that the higher concentrations of test compounds (0.5 and 1.0%) produced greater behavioral responses. Aedes albopictus was more sensitive to β-caryophyllene oxide than An. dirus. Moderate avoidance response rates (25-56% escape) of Ae. albopictus at 0.5% and 1.0% β-caryophyllene oxide were observed in contact and noncontact trials compared with low response rates from An. dirus (26-31% escape). DEET at ≤1% displayed lower irritancy and repellency (1-38%) than β-caryophyllene oxide when tested against the two mosquito species. Knockdown responses (37%) were only observed in An. dirus exposed to 1% β-caryophyllene oxide in the contact trial. β-Caryophyllene oxide did not show any phototoxic potential (PIF= 0.38) nor was there any significant genotoxic response as indicated by no increase in micro-nucleated cells with or without metabolic activation. β-Caryophyllene oxide could be considered as a safe repellent, effective against mosquitoes.

Six limonoids [kotschyienone A and B (1, 2), 7-deacetylgedunin (3), 7-deacetyl-7-oxogedunin (4), andirobin (5) and methyl angolensate (6)] were investigated for their trypanocidal and leishmanicidal activities using bloodstream forms of Trypanosoma brucei and promastigotes of Leishmania major. Whereas all compounds showed anti-trypanosomal activity, only compounds 1–4 displayed anti-leishmanial activity. The 50% growth inhibition (GI50) values for the trypanocidal and leishmanicidal activity of the compounds ranged between 2.5 and 14.9 μM. Kotschyienone A (1) was found to be the most active compound with a minimal inhibition concentration (MIC) value of 10 μM and GI50 values between 2.5 and 2.9 μM. Only compounds 1 and 3 showed moderate cytotoxicity against HL-60 cells with MIC and GI50 values of 100 μM and 31.5–46.2 μM, respectively. Compound 1 was also found to show activity against intracellular amastigotes of L. major with a GI50 value of 1.5 μM. The results suggest that limonoids have potential as drug candidates for the development of new treatments against trypanosomiasis and leishmaniasis.

Background Many medicinal plants have been used in Vietnam but most of them have not been studied and documented. In this study, the traditional plants used by K’Ho-Cil people living in BiDoup-Nui Ba National Park, Vietnam for treatment of diarrhea and identified potential medicinal plants were documented. Methods Information of the medicinal plants used was collected through field surveys and semi-structured interviews with key informants. Plants used for anti-diarrhea were selected for further analysis in structured questionnaires. The potential medicinal plants were identified through quantitative tools: fidelity level (FL) and choice value (CV). The relationship between traditional knowledge and gender, age and geological site was also evaluated using statistical analysis. Results Of the 133 taxa reported by 12 key informants, 34 anti-diarrheal plants were confirmed by 127 non-specialist informants. Interestingly, these plants were also used for 35 other health problems. Among the medicinal plants, Asteraceae was the most predominant family. Elephantopus mollis and Chromolaena odorata belonging to this family with the highest CV were the most preferred ones in diarrheal treatment (1.23 and 1.04, respectively). Moreover, in regard to FL and literature review, several potential plants for further studies were identified, for example Hedyotis capitellata var pubescens and Syzygium ripicola (FL = 100%), or Clitoria mariana and Dacrycarpus imbricatus (FL = 80 %). Conclusion In Vietnam, folk medicine has been widely used by many people without documentation for preservation and scientific study. This study contributes a database of anti-diarrhea plants used by K’Ho-Cil people living in BiDoup-Nui Ba National Park, Vietnam.

A structure-activity relationship study of active molecules against chloroquine-resistant Plasmodium falciparum K1 strain is reported. Structurally simplified analogues of antiplasmodial active alkaloids presented similar levels of activity as their corresponding natural products extracted from Guiera senegalensis and Mitragyna inermis with IC50 values on chloroquine-resistant P. falciparum K1 strain of up to 10.6 μM for spirooxindoles and 13.8 μM for β-carbolines. The identification of such simpler and cheaper structural analogues is crucial to efficiently study these natural products' action mode as well as developing new cures against malaria.

The new acylated flavonoid bioside 4′-O-methylisoscutellarein-7-O-[4′′′-O-acetyl]allopyranosyl-(1→2)-glucopyranoside (1) was isolated from the aerial parts of Stachys annua L. (Lamiaceae). Subterranean organs yielded for the first time 4′-O-methylisoscutellarein (2) and 4′-O-methylisoscutellarein-7-O-[6′′-Oacetyl] allopyranosyl-(1→2)-glucopyranoside (3). Chemical structures of the isolated compounds were elucidated using NMR spectroscopy.

International audience; Inula montana is a member of the family Asteraceae and is present in substantial numbers in Garrigue country (calcareous Mediterranean ecoregion). This species has traditionally been used for its anti-inflammatory properties as well as Arnica montana. In this study, three habitats within Luberon Park (southern France) were compared regarding their pedoclimatic parameters and the resulting morpho-physiological response of the plants. The data showed that I. montana grows in south-facing poor soils and tolerates large altitudinal and temperature gradients. The habitat conditions at high elevation appear to affect mostly the morphology of the plant (organ shortening). Although the leaf contents of total polyphenols and flavonoids subclass essentially followed a seasonal pattern, many sesquiterpene lactones were shown to accumulate first at the low-elevation growing sites that suffered drought stress (draining topsoil, higher temperatures and presence of a drought period during the summer). This work highlights the biological variability of I. montana related to the variation of its natural habitats which is promising for the future domestication of this plant. The manipulation of environmental factors during cultivation is of great interest due to its innovative perspective for modulating and exploiting the phytochemical production of I. montana.

International audience; Introduction: Drugs resistant Plasmodium falciparum is a recurring issue that threatens public health. New anti-plasmodial drugs are needed to overcome this problem. The aim of this study was to characterize in vitro an-tiplasmodial activity of Withania frutescens (Solanaceae) against chloroquine-resistant Plasmodium falciparum strain. Methods: The in vitro antiplasmodial activity of leaves and roots extracts from Withania frutescens was performed in 96 well plates and preliminary phytochemical analysis was performed for the active fractions. The toxicity of the plant extract against CHO (Chinese Hamster Ovary) cells was assessed using the tetrazolium salt MTT col-orimetric assay. The selectivity index (SI) was calculated as the ratio between the cytotoxic and antiparasitic activities. Results: The methanol extract of W. frutescens leaves showed a good antiplasmodial activity (CC 50 18.1 μg/ml). Furthermore, ethyl acetate and butanol fractions showed promising in vitro antiplasmodial activity with a se-lectivity index of 3.1 and 2.4, respectively. The roots of W. frutescens were found to be inactive with a CC 50 value > 80 μg/ml. Conclusion: The antiplasmodial activity of W. frutescens may in part be attributed to the presence of polyphenolic and flavonoid compounds. Based on our results, ethyl acetate and butanol leaves fractions could be considered as a promising source for the development of putative antiplasmodial drugs.

We provide in this article the catalogue of the species names currently accepted in the genus Stephania (Menispermaceae), together with information relative to their types. Sixty-nine species of Stephania are recognized and 36 lectotypes are designated here. This checklist constitutes the basis for a future taxonomical revision of the genus Stephania.

International audience; Fractionation of the ethyl acetate-soluble extract of the roots of Leplaea mayombensis afforded two new 3,4-seco-lanostane-type triterpenoids, leplaeric acids A and B (1, 2), the new lanostane-type triterpenoid leplaeric acid C (3), and six known natural products (5–10). Derivatization of the main constituent, 1, afforded the dimethyl ester 4, the monoamide 11, and diamide 12 for SAR studies. The structures of these compounds were established through spectroscopic methods, and a single-crystal X-ray diffraction analysis was used to confirm the relative configuration of compound 1. These lanostane derivatives are unique since they are the first C-21-oxygenated lanostanes isolated from plant sources. Preliminary biological assays against the MDA MB 231 breast cancer cell line showed that compounds 1, 2, 4, and 11 have modest cytotoxic activity. Compound 2 was the most active, with an IC50 of 55 ± 7 μM. From these results, the amides (11, 12) derived from triterpenoid 1 were found to be less active than the derived esters (2, 4).

International audience; A phytochemical investigation of the ethanol extract of leaves and flowers of Inula montana L. led to the isolation of one new sesquiterpene acid called Eldarin (1) and four new inositol derivatives, Myoinositol,1,5-diangelate-4,6-diacetate (2), Myoinositol,1,6-diangelate-4,5-diacetate (3), Myoinositol-1-angelate-4,5-diacetate-6-(2-methylbutirate) (4), Myoinositol-1-angelate-4,5-diacetate-6-isovalerate (5) isolated for the first time, along with eleven known compounds described for the first time in Inula montana, 1β-Hydroxyarbusculin A (6), Artemorin (7), Santamarin (8), Chrysosplenol C (9), 6-Hydroxykaempferol 3,7-dimethyl ether (10), Reynosin (11), 2 Calenduladiol-3-palmitate (12), Costunolide (13), 4-Hydroxy-3,5-dimethoxybenzenemethanol (14), 9β-Hydroxycostunolide (15) and Hispidulin (16). Structural elucidation has been carried out by spectral methods, such as 1D and 2D NMR, IR, UV and HR-ESI-MS. These compounds have been tested in vitro for anti-inflammatory and cytotoxic activity on macrophages RAW 264.7. As a result, compounds 2, 3, 7, 13, 14, 15 and 16 showed a release of NO with IC 50 value < 30 µM on macrophages.

From the stem barks of Jacaranda mimosifolia benzoic acid (1), 1-naphthaleneacetic acid, 5-carboxy- 1,2,3,4,4a,7,8,8a-octahydro-1,2,4a-trimethyl-[1S-(1α,2β,4aβ,8aα)] ( 2), betulinic acid ( 3), lupeol (4) and ursolic acid (5) were isolated. Similarly, lapachol (6), dehydro-α-lapachone (7), 2- acetylfuro-1, 4-naphthoquinone (8), p-coumaric acid (9), caffeic acid (10), nonacosanoic acid, 2-(4-hydroxyphenyl)ethyl ester (11), β-sitosterol (12), kigelinol (13), oleanolic acid (14), β-friedelinol (15), pomolic acid (16), and kojic acid (17) were isolated from the stem barks of Kigelia africana. All the isolated compounds were characterized by using spectroscopic methods especially 1D and 2D NMR and ESI mass spectrometry and comparison with literature data. To the best of our knowledge, compounds 1, 2, 3 and 5, and compounds 11, 14, 15 and 16 were isolated for the first time from Jacaranda mimosifolia and Kigelia africana, respectively. All these compounds were screened for anticandidal activity by agar diffusion method and microbroth dilution technique on four Candida albicans strains (ATCCL26, ATCC12C, ATCCP37039, and ATCCP37037). Among them, compounds 9, 10, and 17 exhibited the highest anticandidal activity that varied between the microbial species (MIC= 0.01 ± 0.00 − 0.03 ± 0.00 mg/mL) on C. albicans ATCCL26, ATCCP37037, ATCCP37039 and ATCC12C strains. Compound 17 was likely the most active against the four Candida albicans strains (MIC= 0.01 ± 0.00 − 0.02 ± 0.00 mg/mL).

This research paper presents a quick and ecofriendly technique for the extraction of harpagoside (HS), the active marker of Harpagophytum procumbens (HP), along with a comparison with conventional methods so as to propose an efficient HPLC method. HP is widely used as an anti-inflammatory in phytotherapy. The quality control of the herbal drug and extract calls for a time consuming method of conventional extraction, which involves a high consumption of solvents. In this study, HP has been extracted using conventional ultrasound (UAE) and microwave (MAE)-assisted methods. The effects have been examined based on several parameters of HS extraction efficiencies. An HPLC method with a core-shell column was developed in order to calculate the HS in HP. The flow rate was reduced by 4. The method of validation used is specific, linear, precise and accurate. MAE and UAE saved solvent consumption, time and energy. It has, therefore, been found that the combined UAE-HPLC process is convenient and appropriate for the quality control of HP.

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International audience; DIG, a liquid herbal preparation made from a mixture of diluted mother tinctures of Berberis vulgaris, Taraxacum officinale and Arctium lappa, was assessed for its antimutagenic properties against mitomycin C. The micronucleus assay on Chinese hamster ovary (CHO)-K1 cells was used to evaluate the in vitro anticlastogenic activity of DIG compared to those of separately diluted mother tinctures. The micronucleus assay was performed on mouse erythrocytes and the comet assay was performed on mouse liver, kidney, lung, brain and testicles to assess the protective effects of DIG (0.2 and 2 % at libitum) against an intraperitoneal injection of mitomycin C (1 mg Kg(-1)) in mice. DIG exerted a powerful anticlastogenic activity, under both pretreatment and simultaneous treatment conditions as assessed by the micronucleus assay in CHO-K1 cells. Its protective activity was greater than that observed for each mother tincture. DIG reduced micronuclei levels in mouse erythrocytes and suppressed \textgreater 80 % of DNA strand breaks in the liver, kidney, lung, brain and testicles of mice exposed to mitomycin C.

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The spread ofPlasmodium falciparumresistance toward most of the used drugs requires new antimalarial compounds. Taking advantage of the biodiversity, the ethnopharmacological approach opens the way for the discovery and the characterization of potent original molecules. Previous works led to the selection of a bisbenzylisoquinoline, cepharanthine, extracted fromStephania rotunda, which is mainly present in Cambodia. A sensitive and selective liquid chromatography method has been developed for the determination of cepharanthine in mouse plasma. The method involved a semiautomated microextraction by packed sorbent (MEPS) using 4 mg of solid phase silica-C8 sorbent. LC separation was performed on a Kinetex XB-C18 column (2.6 µm) with a mobile phase of acetonitrile containing formic acid and 10 mM ammonium formate buffer pH 3.5. Data were acquired at 282 nm with a diode array detector. The drug/internal standard peak area ratios were linked via linear relationships to plasma concentrations (75–2,000 ng/mL). Precision was below 5% and accuracy was 99.0–102%. Extraction recovery of cepharanthine was 56–58%. The method was successfully used to determine the pharmacokinetic profile of cepharanthine in healthy andPlasmodium bergheiinfected mice. The infection did not impact pharmacokinetic parameters of cepharanthine.

International audience; Aim of the study Antiplasmodial activity, inhibition of nitric oxide (NO) overproduction, and anti-proliferative activity were investigated in vitro to evaluate the bioactive potential of the traditional pharmacopoeia of the Mascarene Archipelago, which is known for its biodiversity and for the richness of its endemic flora. Materials and methods A total of 45 methanol (MeOH) and dichloromethane (DCM) extracts were prepared from 19 plant species collected on Réunion and Mauritius Islands. Ninety-six-well microplate assays were performed on chloroquine sensitive Plasmodium falciparum 3D7 strain, on LPS-stimulated Raw 264.7 murine macrophages and on A-549, DLD-1 and WS1 human cells. Activity was evaluated through spectrophotometric methods. Results Activity was attributed to plant extracts expressing IC50 \textless 50 μg/ml for antiplasmodial response, IC50 \textless 100 μg/ml for cytotoxicity, and IC50 \textless 130 μg/ml for anti-inflammatory reaction. The majority of the extracts tested (69%) exhibited potency in at least one of these three types of activity. This is the first report describing promising antiplasmodial activity (IC50 \textless 15 μg/ml) for Psiadia dentata DCM extract and Terminalia bentzoe MeOH bark extract. NO inhibition assay revealed seven interesting plants, described for the first time as anti-inflammatory: Aphloia theiformis, Buddleja salviifolia, Eupatorium riparium, Hiptage benghalensis, Psiadia arguta, Psiadia dentata, and Scutia commersonii. Finally, anti-proliferative activity was observed for two endemic species, Geniostoma borbonicum and Nuxia verticillata. Conclusion Using the criterion of endemism as part of the criteria for traditional medicinal use raises the chances of finding original active principles. In our case, 86% of the endemic plants tested displayed pharmacological interest.