Microwave and ultrasound extraction of antioxidant phenolic compounds from Lantana camara Linn. leaves: Optimization, comparative study, and FT-Orbitrap MS analysis.

INTRODUCTION: The species Lantana camara is used in folk medicine. The biological activities of this medicinal plant are attributable to the presence of various derivatives of triterpenoids and phenolic compounds present in its preparations, indicating excellent economic potential. OBJECTIVE: In this study, the operational conditions of ultrasound-assisted extraction (UAE) and microwave-assisted extraction (MAE) were optimized using Box-Behnken design to improve the total phenolic content (TPC) recovered in hydroethanolic extracts of L. camara leaves. MATERIAL AND METHODS: The TPC, total flavonoid content (TFC), and antioxidant activities of the hydroalcoholic extracts of L. camara, prepared by UAE and MAE under the optimized extraction conditions, were compared with those of the extracts obtained by conventional extraction methods. RESULTS: Under the optimal conditions, the extracts obtained by UAE (35% ethanol, 25 min, and a solvent-to-solid ratio of 60:1 mL/g) and by MAE (53% ethanol, 15 min, and 300 W) provided high yields of 32.50% and 38.61% and TPC values of 102.89 and 109.83 mg GAE/g DW, respectively. The MAE extract showed the best results with respect to TPC, TFC, and antioxidant activities, followed by extracts obtained by UAE, Soxhlet extraction, decoction, maceration, and infusion, in that order. CONCLUSION: The results obtained indicate that L. camara may be used as an important source of antioxidant phenolic compounds to obtain products with high biological and economic potential, especially when the extraction process is performed under appropriate conditions using MAE and/or UAE, employing environmentally friendly solvents such as water and ethanol.

Dereplication of Lantana trifolia L. leaves and fruits by UFLC-DAD-(+)-ESI-MS/MS and its antifungal and cytotoxic activities.

INTRODUCTION: Lantana trifolia L. (Verbenaceae) is a shrubby plant. In folk medicine, its leaves are used in the form of infusions and syrups to treat angina, coughs, and colds; they are also applied as tranquilizer. Previous studies have reported the antimicrobial potential of the compounds present in L. trifolia leaves. OBJECTIVES: To report the anti-Candida activities of the fractions obtained from the fruits and leaves of two L. trifolia specimens. METHODS: The L. trifolia fractions were submitted to UFLC-DAD-(+)-ESI-MS/MS, and the data were analyzed by using multivariate statistical tools (PCA, PLS-DA) and spectral similarity analyses based on molecular networking, which aided dereplication of the bioactive compounds. Additionally, NMR analyses were performed to confirm the chemical structure of some of the major compounds in the fractions. RESULTS: The ethyl acetate fractions presented MIC values lower than 100 µg mL-1 against the three Candida strains evaluated herein (C. albicans, C. tropicalis, and C. glabrata). Fractions FrPo AcOEt, FrPe AcOEt, and FrPe nBut had MIC values of 1.46, 2.93, and 2.93 µg mL-1 against C. glabrata, respectively. These values resembled the MIC value of amphotericin B, the positive control (0.5-1.0 µg mL-1), against this same strain. Cytotoxicity was measured and used to calculate the selectivity index. CONCLUSION: On the basis of our data, the most active fractions in the antifungal assay were more selective against C. glabrata than against non-infected cells. The analytical approach adopted here allowed us to annotate 29 compounds, nine of which were bioactive (PLS-DA results) and belong to the class of phenolic compounds.

Exploration of anticancer potential of Lantadenes from weed Lantana camara: Synthesis, in silico, in vitro and in vivo studies.

Naturally occurring pentacyclic triterpenoids and their semisynthetic analogues have engrossed increasing attention for their anticancer potential and exhibiting promising role in discovery of new anticancer agents. Present study include the semi synthetic modifications of Lantadenes from the weed Lantana carama and their structures delineation by FT-IR, 1H-NMR, 13C-NMR & mass spectroscopy. All the compounds were scrutinized for in vitro cytotoxicity, ligand receptor interaction and in vivo anticancer studies. Most of the novel analogues displayed potent antiproliferative activity against A375 & A431 cancer cell lines and found superior to parent Lantadenes. In particular, 3ß-(4-Methoxybenzoyloxy)-22ß-senecioyloxy-olean-12-en-28-oic acid was found to be most suitable compound, with IC50 value of 3.027 µM aganist A375 cell line having least docking score (-69.40 kcal/mol). Promising anticancer potential of the lead was further indicated by significant reduction in tumor volume and burden in two stage carcinoma model. These findings suggests that the Lantadene derivatives may hold promising potential for the intervention of skin cancers.

Phytochemical study of Lantana camara flowers, ecotoxicity, antioxidant, in vitro and in silico acetylcholinesterase: molecular docking, MD, and MM/GBSA calculations.

Lantana camara L. (Verbenaceae), commonly called lead cambará, has often been used in folk medicine as antiseptic, antispasmodic, against hemorrhages, flu, colds, and diarrheic. This plant is considered a weed and an ornamental and medicinal plant and is an essential source of natural organic compounds, mainly flavonoids. This work aims to investigate the chemical composition and evaluate the biological properties such as antioxidant and acetylcholinesterase of the constituents from L. camara flowers. In addition, the computational simulation was carried out with the constituents identified. The results showed that methanolic extract of the flowers of L. camara presents toxicity, antioxidant activity with 97.8% inhibition percentage in the concentration of 0.25 mg mL-1 against the DPPH radical, and acetylcholinesterase activity. The phytochemical study of extract from L. camara flowers resulted in LC-MS identification of 18 polyphenolic compounds, such as phenolic acid derivatives, phenylethanoid glycosides, and flavonoids. In the in silico study, flavonoid isoverbascoside showed affinity energy of -9.9 kcal.mol-1 with the AChE enzyme. Their phytochemical content, mainly the presence of flavonoids and phenolic compounds in L. camara extracts, may be related to the antioxidant and anticholinesterase potential observed.

Cytotype Affects the Capability of the Whitefly Bemisia tabaci MED Species To Feed and Oviposit on an Unfavorable Host Plant.

The acquisition of nutritional obligate primary endosymbionts (P-symbionts) allowed phloemo-phageous insects to feed on plant sap and thus colonize novel ecological niches. P-symbionts often coexist with facultative secondary endosymbionts (S-symbionts), which may also influence their hosts' niche utilization ability. The whitefly Bemisia tabaci is a highly diversified species complex harboring, in addition to the P-symbiont "Candidatus Portiera aleyrodidarum," seven S-symbionts whose roles remain poorly understood. Here, we compare the phenotypic and metabolic responses of three B. tabaci lines differing in their S-symbiont community, reared on three different host plants, hibiscus, tobacco, or lantana, and address whether and how S-symbionts influence insect capacity to feed and produce offspring on those plants. We first show that hibiscus, tobacco, and lantana differ in their free amino acid composition. Insects' performance, as well as free amino acid profile and symbiotic load, were shown to be plant dependent, suggesting a critical role for the plant nutritional properties. Insect fecundity was significantly lower on lantana, indicating that it is the least favorable plant. Remarkably, insects reared on this plant show a specific amino acid profile and a higher symbiont density compared to the two other plants. In addition, this plant was the only one for which fecundity differences were observed between lines. Using genetically homogeneous hybrids, we demonstrate that cytotype (mitochondria and symbionts), and not genotype, is a major determinant of females' fecundity and amino acid profile on lantana. As cytotypes differ in their S-symbiont community, we propose that these symbionts may mediate their hosts' suitable plant range. IMPORTANCE Microbial symbionts are universal in eukaryotes, and it is now recognized that symbiotic associations represent major evolutionary driving forces. However, the extent to which symbionts contribute to their hosts' ecological adaptation and subsequent diversification is far from being fully elucidated. The whitefly Bemisia tabaci is a sap feeder associated with multiple coinfecting intracellular facultative symbionts. Here, we show that plant species simultaneously affect whiteflies' performance, amino acid profile, and symbiotic density, which could be partially explained by differences in plant nutritional properties. We also demonstrate that, on lantana, the least favorable plant used in our study, whiteflies' performance is determined by their cytotype. We propose that the host plant utilization in B. tabaci is influenced by its facultative symbiont community composition, possibly through its impact on the host dietary requirements. Altogether, our data provide new insights into the impact of intracellular microorganisms on their animal hosts' ecological niche range and diversification.

Phytochemical Investigation and Biological Activities of Lantana rhodesiensis.

Lantana rhodesiensis Moldenke is a plant widely used to treat diseases, such as rheumatism, diabetes, and malaria in traditional medicine. To better understand the traditional uses of this plant, a phytochemical study was undertaken, revealing a higher proportion of polyphenols, including flavonoids in L. rhodesiensis leaf extract and moderate proportion in stem and root extracts. The antioxidant activity of the extracts was also determined using three different assays: the radical 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging activity, the FRAP method (Ferric-reducing antioxidant power) and the ß-carotene bleaching test. The anti-malarial activity of each extract was also evaluated using asexual erythrocyte stages of Plasmodium falciparum, chloroquine-sensitive strain 3D7. The results showed that the leaf extract exhibited higher antioxidant and anti-malarial activities in comparison with the stem and root extracts, probably due to the presence of higher quantities of polyphenols including flavonoids in the leaves. A positive linear correlation was established between the phenolic compound content (total polyphenols including flavonoids and tannins; and total flavonoids) and the antioxidant activity of all extracts. Furthermore, four flavones were isolated from leaf dichloromethane and ethyl acetate fractions: a new flavone named rhodescine (5,6,3',5'-tetrahydroxy-7,4'-dimethoxyflavone) (1), 5-hydroxy-6,7,3',4',5'-pentamethoxyflavone (2), 5-hydroxy-6,7,3',4'-tetramethoxyflavone (3), and 5,6,3'-trihydroxy-7,4'-dimethoxyflavone (4). Their structures were elucidated by 1H, 13CNMR, COSY, HSQC, HMBC, and MS-EI spectral methods. Aside from compound 2, all other molecules were described for the first time in this plant species.

Isolation optimisation, synthesis, molecular docking and in silico ADMET studies of lantadene a and its derivatives.

A simple and economical method was developed for the extraction and isolation of pentacyclic triterpenoid lantadene A from the leaves of Lantana camara. The lantadene A displays significant anti-inflammatory and anticancer properties via the inhibition of IKK-mediated NF-κB protein. Therefore, the derivatives of lantadene A were synthesised to further optimise the pharmacophore for anti-inflammatory and anticancer activities. The synthesised compounds were docked into the active site of IKK to find the most potent inhibitor of IKK. Molecular docking studies revealed that 3ß,22ß-diisobutyl substituted lantadene derivative (10) binds to the IKK protein with the highest affinity. Furthermore, in the in silico ADMET studies, the lead IKK inhibitor (10) was found to be Ames non-toxic, non-carcinogen, and a weak inhibitor of hERG.[Figure: see text].

A lectin with anti-microbial and anti proliferative activities from Lantana camara, a medicinal plant.

BACKGROUND: Lectins are known to possess interesting biological properties such as anti microbial, nematicidal, anti tumor and anti viral activities. Lantana camara from verbenaceae family is a medicinal plant known for possessing anti oxidant and anticancer activities. Since anticancer activity is reported in plant lectins, leaves of Lantana camara was used to check the presence of lectin. METHODS AND RESULTS: Here we report the purification, characterization and biological properties of a lectin from Lantana camara (LCL) leaves. LCL was purified by ion exchange chromatography on CM-cellulose column followed by affinity chromatography on mucin coupled Sepharose 4B column and gel filtration chromatography on Superdex G75 column. LCL is a glycoprotein with 10% of the carbohydrate and is blood group non specific. SDS-PAGE analysis of affinity purified LCL showed two proteins with apparent molecular weight of 14.49 kDa and 17.4 kDa which were subsequently separated by Gel filtration chromatography on Superdex G75 column. Hapten inhibition studies of LCL revealed its highest affinity for Chitin, Milibiose, α-D-Methyl galactopyranoside and glycoproteins like mucin, asialomucin. LCL showed strong binding to human colon adenocarcinoma HT29 cells with MFI of 242 which was effectively blocked by 68.1 and 62.5% by both mucin and milibiose. LCL showed dose and time dependent growth inhibitory effects on HT29 cells with IC50 of 3.75  µg/ml at 48 h. LCL has potent antibacterial and anti fungal activity. CONCLUSION: LCL can be explored for its clinical potential.

Sedative effects of the essential oil from the leaves of Lantana camara occurring in the Republic of Benin via inhalation in mice.

Lantana camara Linn. (Verbenaceae) is used traditionally for its numerous medicinal properties such as antimalarial, antibacterial, anticancer and anti-inflammatory. In the present study, we investigated the chemical composition of essential oil from the leaves of L. camara (LCEO) occurring in the Republic of Benin (West Africa) in comparison with LCEOs from other regions; evaluated its sedative effects in mice via inhalation administration; and identified the compounds responsible for activity. LCEO was extracted by hydrodistillation and chemical analyses of the oil were performed by GC and GC/MS. The oil was dominated by monoterpene hydrocarbons (60.58%) and oxygenated monoterpenes (33.39%), among which sabinene (38.81%) and 1,8-cineole (28.90%) were the most abundant. LCEO administered via inhalation to mice significantly decreased locomotor activity in a dose-dependent manner, mainly at the doses of 0.0004 and 0.04 mg per 400 µL of triethyl citrate (TEC). The oil was fractionated to give two fractions, which were further investigated, and revealed that both sabinene and 1,8-cineole were the principal active compounds. The results of the present study indicated that via inhalation administration, LCEO and its main constituents could be considered as promising candidates for the management of dementia, insomnia, attention deficit hyperactivity disorder and other central nervous system-associated diseases.

Green synthesis of highly fluorescent nitrogen - Doped carbon dots from Lantana camara berries for effective detection of lead(II) and bioimaging.

Here, we developed a simple green approach for the synthesis of highly fluorescent nitrogen doped carbon dots (NCDs) using Lantana camara berries. Optical and physicochemical properties of as synthesized NCDs were extensively studied by using various analytical techniques. NCDs exhibited bright fluorescence with Quantum yield as high as 33.15%, which is stable to various effects like heat, pH, ionic strength and continuous irradiation. Furthermore, the NCDs presented highly selective and sensitive fluorescence response towards Pb2+ which explored their potential to serve as a label-free fluorescent probe for the effective detection of Pb2+. As developed NCDs based probe exhibited a great linear response (R2=0.998) towards Pb2+ in the concentration range of 0-200nM with a detection limit of 9.64nM. The probe further presented high precision without any interference and was successfully applied for the detection of Pb2+ in the real water and human sera (serum and urine) samples. Cytotoxicity studies on both cancerous (human breast adenocarcinoma MCF-7) and normal (Human embryonic kidney HEK-293) cell lines revealed their excellent biocompatibility. With their low cytotoxicity, strong fluorescence and excitation-dependent emission, NCDs were successfully applied as multi-colour bioimaging agents and Pb2+ detection capabilities were further evaluated in live cells.

Modulation of Fatty Acids and Interleukin-6 in Glioma Cells by South American Tea Extracts and their Phenolic Compounds.

Dietary phenolic compounds are plant metabolites with beneficial effects on the central nervous system. Thus, our aim was to identify anti-inflammatory compounds from South American plants on glia, which regulates neuro-immune response. The compounds were extracted from Lantana grisebachii (LG), Aspidosperma quebracho-blanco (AQB), and Ilex paraguariensis (IP) teas and identified by HPLC-DAD-MS. Extracts (0-200 µg/ml) were tested on human T98-G and rat C6 glioma lines. Cellular viability (by the resazurin assay), fatty acid profile (by gas chromatography) and pro-inflammatory interleukin-6 release (IL-6 by ELISA) were determined. Data were analyzed by partial least-square regression to discriminate bioactive compounds. Twenty-one compounds were determined in LG, mainly iridoids, which were linked to ω-3 and ω-6 polyunsaturated fatty acids, but not to IL-6 release. Thirty-one compounds were found in AQB, mostly hydroxybenzoic derivatives, which were positively related to IL-6 release. Twenty-three compounds were identified in IP, including caffeoylquinic derivatives and mainly chlorogenic acid. They increased the ω-7 palmitoleic fatty acid, which was related to IL-6 decrease. These results enhances phytochemical knowledge of widely available plants, and suggest the lipid-related anti-inflammatory activity of IP phenolic compounds, which give nutritional relevance to the tea.

Evaluation of the anti-diarrheal activity of the aqueous stem extract of Lantana camara Linn (Verbenaceae) in mice.

BACKGROUND: Diarrheal disease remains a public health problem in developing countries, including Ethiopia. In order to alleviate this disease, Ethiopian traditional healers use a wide range of medicinal plants from which Lantana camara is one of them. The stem of this plant is traditionally used for the treatment of diarrhoea. In addition, this plant is scientifically evaluated to have an antispasmodic effect on in vitro study. The aim of this study was to evaluate the antidiarrheal activity of the aqueous stem extract of L. camara Linn in mice. METHODS: The antidiarrheal activity of the extract was investigated using castor oil induced diarrhoea, enteropooling and small intestine transit models. The test groups received various doses (100, 200, and 400 mg/kg) of the extract, whereas positive controls received Loperamide (3 mg/kg) and negative controls received distilled water (10 ml/kg). RESULTS: In castor oil induced diarrhoea model, the extract, at all test doses, significantly (p < 0.001) prolonged diarrhoea onset, decreased the frequency of defecation, and weight of faeces. Similarly, the extract produced a significant (p < 0.001) decline in the weight and volume of intestinal contents at all tested doses. In addition, a significant (P < 0.001) reduction in the gastrointestinal motility in charcoal meal test was also observed in all doses of the extract. Phytochemical screening of the extract revealed the presence of flavonoids, alkaloids, tannins, and phytosterols that may play a key role in its antidiarrheal activity. CONCLUSION: The obtained results of the present study confirm antidiarrheal activity of the stem of L. camara, thus provide the scientific basis for the traditional uses of this plant as a treatment for diarrhoea.

Lantana camara Linn root extract-mediated gold nanoparticles and their in vitro antioxidant and cytotoxic potentials.

The Lantana camara Linn root extract derived gold nanoparticles (Au NPs) were characterized by Ultraviolet-Visible spectroscopy, X-ray diffraction, fourier transform-infrared, high resolution transmission electron microscopy, selected area electron diffraction pattern and energy dispersive X-ray analyses. In DPPH assay, the inhibitory concentration (IC50) of Au NPs and gallic acid was 24.17 and 5.39 µg/ml, whereas, for cytotoxicity assay, the IC50 of Au NPs was 17.72 and 32.98 µg/ml on MBA-MB-231 and Vero cells, respectively. Thus, the Au NPs possess significant in vitro antioxidant and cytotoxic properties which could be considered as potential alternate for the development of anticancer drug in future.

[Regional oxidative stress in encephalon of female mice with polyphenolic exposure from tea extracts in oral overweight plant-based treatment].

Polyphenols provide by diet may act as antioxidant in the Central Nervous System and exert a protective effect on metabolic diseases. The aim of this study was to establish tea extract effects on oxidative status and murine overweight in accordance with polyphenolic availability in different encephalic regions. METHODS: Balb/c mice (female, n>3) with overweight received for 15 days 100 mg/Kg/d of extract from Lantana grisebachii, Aspidosperma quebracho-blanco, or Ilex paraguariensis extracts and control group (received water without extract). Body weight gain was recorded regularly. Polyphenols, hydroperoxides (HP), lipid peroxides (LP), and superoxide anion (SO) were measured in brain (telencephalon and diencephalon), midbrain, brainstem and cerebellum. Results were compared by ANOVA followed by the Tukey test (P<0.05). RESULTS: A. quebracho-blanco-based treatment decreased weight gain and increased polyphenols in brainstem (p<0.02), although it concomitantly increased SO and LP in this region (p=0.0029 and p=0.0280, respectively). L. grisebachii-based treatment reduced oxidative markers differentially in each region (p<0.05). I. paraguariensis-based treatment oxidized midbrain and cerebellum, although it was antioxidant in the brainstem (p<0.05). All treatments were antioxidant in telencephalon (p=0.0029). CONCLUSIONS: The A. quebracho-blanco extract was active on overweight and increased polyphenols in brainstem, with safe functional derivatives being required to avoid oxidative stress. Other extracts affected oxidative status in a region-dependent manner.

[Bioavailability of phenolic compounds and redox state of murine liver and kidney as sex-dependent responses to phytoextracts.]

BACKGROUND: Plant extracts can be obtained to carry bioactive compounds, useful for prevention and treatment of different illnesses. This also supports the intake of teas as functional beverages. Nonetheless, it is incompletely known whether these extracts can act as effective sources and vehicles de phenolic compounds (phenolics/polyphenols) to reach their targets. OBJECTIVE: To establish whether phytoextract ingestion modified in a sex-dependent manner the phenolic bioavailability and redox response in liver and kidney. METHOD: BALB/C mice ingested for a month 100 mg/Kg/d of extracts (tea-like) from Aspidosperma quebracho-blanco (AQB), Lantana grisebachii (LG) or Ilex paraguariensis (IP). Then, phenolics, peroxides and nitrites were analyzed by spectrophotometry. Also, phenolic permeation from digested and undigested extracts was evaluated in vitro with a rat jejunum-based assay. RESULTS: Phenolic permeation depended on extract digestion. In males, IP showed a special time course of hepatic phenolics, whereas all extracts decreased renal phenolics at 15 days. Extracts induced hepatic lipoperoxides at 15 days. LG reduced renal hydroperoxides at 15 days and hepatic nitrites at 30 days, whereas AQB and IP reduced renal lipoperoxides and nitrites at 30 days. In females, extracts reduced hydroperoxides, with LG and AQB also reducing lipoperoxides. IP increased renal lipoperoxides at 30 days. CONCLUSION: IP was a relevant phenolic source. Sex-dependent responses were found in all variables, which should be considered to prevent misleading generalizations in phytodrug bioprospecting.

Transformation of toxic and allelopathic lantana into a benign organic fertilizer through vermicomposting.

In a first study of its kind, the composition of vermicompost derived solely from the toxic and allelopathic weed lantana has been investigated using UV-visible and Fourier transform infrared (FT-IR) spectroscopy, thermogravimetric (TG) and differential scanning calorimetry (DSC), gas chromatography-mass spectometry (GC-MS), and scanning electron microscopy (SEM). The studies reveal that a sharp reduction in humification index, substantial mineralization of organic matter and degradation of complex aromatics such as lignin and polyphenols into simpler carbohydrates and lipids occur in the course of vermicomposting. GC-MS analysis shows significant fragmentation, bio-oxidation and molecular rearrangements of chemical compounds in vermicompost in comparison to those in lantana. SEM micrographs of vermicompost reflect strong disaggregation of material compared to the much better formed lantana matrices. The phenols and sesquiterpene lactones which are specifically responsible for the toxicity and allelopathy of lantana are seen to get significantly degraded in the course of vermicomposting - turning it into a plant-friendly organic fertilizer. The study leads to the possibility that the millions of tons of phytomass that is generated annually by lantana can be gainfully utilized in producing organic fertilizer via vermicomposting.

Chemical Characterization and Trypanocidal, Leishmanicidal and Cytotoxicity Potential of Lantana camara L. (Verbenaceae) Essential Oil.

Drug resistance in the treatment of neglected parasitic diseases, such as leishmaniasis and trypanosomiasis, has led to the search and development of alternative drugs from plant origins. In this context, the essential oil extracted by hydro-distillation from Lantana camara leaves was tested against Leishmania braziliensis and Trypanosoma cruzi. The results demonstrated that L. camara essential oil inhibited T. cruzi and L. braziliensis with IC50 of 201.94 µg/mL and 72.31 µg/mL, respectively. L. camara essential oil was found to be toxic to NCTC929 fibroblasts at 500 µg/mL (IC50 = 301.42 µg/mL). The composition of L. camara essential oil analyzed by gas chromatography-mass spectrometry (GC/MS) revealed large amounts of (E)-caryophyllene (23.75%), biciclogermacrene (15.80%), germacrene D (11.73%), terpinolene (6.1%), and sabinene (5.92%), which might be, at least in part, responsible for its activity. Taken together, our results suggest that L. camara essential oil may be an important source of therapeutic agents for the development of alternative drugs against parasitic diseases.

The Chemical Diversity of Lantana camara: Analyses of Essential Oil Samples from Cuba, Nepal, and Yemen.

The aerial parts of Lantana camara L. were collected from three different geographical locations: Artemisa (Cuba), Biratnagar (Nepal), and Sana'a (Yemen). The essential oils were obtained by hydrodistillation and analyzed by gas chromatography/mass spectrometry. A cluster analysis of 39 L. camara essential oil compositions revealed eight major chemotypes: ß-caryophyllene, germacrene D, ar-curcumene/zingiberene, γ-curcumen-15-al/epi-ß-bisabolol, (E)-nerolidol, davanone, eugenol/alloaromadendrene, and carvone. The sample from Cuba falls into the group dominated by (E)-nerolidol, the sample from Nepal is a davanone chemotype, and the sample from Yemen belongs to the ß-caryophyllene chemotype. The chemical composition of L. camara oil plays a role in the biological activity; the ß-caryophyllene and (E)-nerolidol chemotypes showed antimicrobial and cytotoxic activities.

Lantana montevidensis Essential Oil: Chemical Composition and Mosquito Repellent Activity against Aedes aegypti.

The essential oil (EO) of Lantana montevidensis (Spreng.) Briq. (L. sellowiana Link & Otto) was investigated for its chemical composition and mosquito repellent activity. The essential oil obtained by hydrodistillation of aerial plant parts was analyzed by GC-FID and GC-MS. The major constituents were p-elemene (22.0%), ß-caryophyllene (20.1%), and germacrene D (9.4%). Sesquiterpene hydrocarbons were present.in considerable quantities (78.9%) in the L. montevidensis EO, followed by oxygenated sesquiterpenes (8.9%), monoterpene hydrocarbons (7.7%), oxygenated monoterpenes (1.9%), diterpenes (1.2%) and other compounds (0.2%). The oil of L. montevidensis was repellent with a minimum effective dosage (MED) of 0.021 ± 0.013 mg/cm(2) as compared with that of the positive control N,N-diethyl-3-methylbenzamide (DEET) with a MED of 0.006 : 0.001 mg/cm(2)) against Aedes aegypti L. The major compound ß-elemene was tested individually for its repellency and had a MED value of 0.23 ? 0.14 mg/cm2 (DEET was 0.008 ? 0.001 mg/cm2). This is the first report on the repellent activity of L. montevidensis EO and P-elemene using human-based in vivo assays against Ae. aegypti.

Cytotoxic, Antiproliferative and Pro-Apoptotic Effects of 5-Hydroxyl-6,7,3',4',5'-Pentamethoxyflavone Isolated from Lantana ukambensis.

Lantana ukambensis (Vatke) Verdc. is an African food and medicinal plant. Its red fruits are eaten and highly appreciated by the rural population. This plant was extensively used in African folk medicinal traditions to treat chronic wounds but also as anti-leishmanial or cytotoxic remedies, especially in Burkina Faso, Tanzania, Kenya, or Ethiopia. This study investigates the in vitro bioactivity of polymethoxyflavones extracted from a L. ukambensis as anti-proliferative and pro-apoptotic agents. We isolated two known polymethoxyflavones, 5,6,7,3',4',5'-hexamethoxyflavone (1) and 5-hydroxy-6,7,3',4',5'-pentamethoxyflavone (2) from the whole plant of L. ukambensis. Their chemical structures were determined by spectroscopic analysis and comparison with published data. These molecules were tested for the anti-proliferative, cytotoxic and pro-apoptotic effects on human cancer cells. Among them, 5-hydroxy-6,7,3',4',5'-pentamethoxyflavone (2) was selectively cytotoxic against monocytic lymphoma (U937), acute T cell leukemia (Jurkat), and chronic myelogenous leukemia (K562) cell lines, but not against peripheral blood mononuclear cells (PBMCs) from healthy donors, at all tested concentrations. Moreover, this compound exhibited significant anti-proliferative and pro-apoptotic effects against U937 acute myelogenous leukemia cells. This study highlights the anti-proliferative and pro-apoptotic effects of 5-hydroxy-6,7,3',4',5'-pentamethoxyflavone (2) and provides a scientific basis of traditional use of L. ukambensis.