Evaluation of plant-mediated synthesized silver nanoparticles against vector mosquitoes

Diseases transmitted by blood-feeding mosquitoes, such as dengue fever, dengue hemorrhagic fever, Japanese encephalitis, malaria, and filariasis, are increasing in prevalence, particularly in tropical and subtropical zones. To control mosquitoes and mosquito-borne diseases, which have worldwide health and economic impacts, synthetic insecticide-based interventions are still necessary, particularly in situations of epidemic outbreak and sudden increases of adult mosquitoes. Green nanoparticle synthesis has been achieved using environmentally acceptable plant extract and eco-friendly reducing and capping agents. In view of the recently increased interest in developing plant origin insecticides as an alternative to chemical insecticide, in the present study, the adulticidal activity of silver nanoparticles (AgNPs) synthesized using Heliotropium indicum plant leaf extract against adults of Anopheles stephensi, Aedes aegypti, and Culex quinquefasciatus was determined. Adult mosquitoes were exposed to varying concentrations of aqueous extract of H. indicum and synthesized AgNPs for 24 h. AgNPs were rapidly synthesized using the leaf extract of H. indicum, and the formation of nanoparticles was observed within 6 h. The results recorded from UV–vis spectrum, Fourier transform infrared, X-ray diffraction, scanning electron microscopy, and transmission electron microscopy support the biosynthesis and characterization of AgNPs. The maximum efficacy was observed in synthesized AgNPs against the adult of A. stephensi (lethal dose (LD)₅₀?=?26.712 μg/mL; LD₉₀?=?49.061 μg/mL), A. aegypti (LD₅₀?=?29.626 μg/mL; LD₉₀?=?54.269 μg/mL), and C. quinquefasciatus (LD₅₀?=?32.077 μg/mL; LD₉₀?=?58.426 μg/mL), respectively. No mortality was observed in the control. These results suggest that the leaf aqueous extracts of H.indicum and green synthesis of AgNPs have the potential to be used as an ideal eco-friendly approach for the control of the A. stephensi, A. aegypti, and C. quinquefasciatus. This is the first report on the adulticidal activity of the plant extracts and AgNPs.     

Larvicidal effects of some Euro-Asiatic plants against Culex quinquefasciatus Say larvae (Diptera: Culicidae)

Methanol extracts of the aerial parts from 62 Euro-Asiatic plant species were tested for larvicidal activity against the mosquito Culex quinquefasciatus Say (Diptera: Culicidae) under laboratory conditions. The fourth larval instar was tested. The extracts of the plants Seseli pallasii and Schisandra chinencis displayed the highest larvicidal activities with LD₅₀ 6 and 15 ppm, respectively, followed by Arthemisia campestris, Verbena officinalis, and Imperatoria osthruthium with LD₅₀ 23, 38, and 49 ppm, respectively. The appraised value of LD₅₀ for two species was between 51–100 ppm; eight species had lethal doses from 101 to 500 ppm, 13 species showed lethal doses from 501 to 1,000 ppm, and 34 species did not show lethal doses for low mortality (LD₅₀ > 1,000 ppm).     

Antiprotozoan activity of Brazilian marine cnidarian extracts and of a modified steroid from the octocoral <Emphasis Type="Italic">Carijoa riisei</Emphasis>

In the present investigation, we have evaluated the antileishmanial and antitrypanosomal activity of methanolic crude extracts obtained from eight species of cnidarians and of a modified steroid isolated from the octocoral Carijoa riisei. The antileishmanial activity of cnidarians crude extracts showed 50% inhibitory concentration (IC₅₀) values in the concentration range between 2.8 and 93.3 μg/mL. Trypomastigotes of Trypanosoma cruzi were less susceptible to the crude extracts, with IC₅₀ values in the concentration range between 40.9 and 117.9 μg/mL. The steroid (18-acetoxipregna-1,4,20-trien-3-one) displayed a strong antileishmanial activity, with an IC₅₀ value of 5.5 μg/mL against promastigotes and 16.88 μg/mL against intracellular amastigotes. The steroid also displayed mammalian cytotoxicity (IC₅₀ of 10.6 μg/mL), but no hemolytic activity was observed at the highest concentration of 12.5 μg/mL. The antileishmanial effect of the steroid in macrophages suggested other mechanism than macrophage activation, as no upregulation of nitric oxide was observed. The antitrypanosomal activity of the steroid resulted in an IC₅₀ value of 50.5 μg/mL. These results indicate the potential of cnidarian natural compounds as antileishmanial drug candidates.     

Antiplasmodial activity of botanical extracts against Plasmodium falciparum

The absence of a vaccine and the rampant resistance to almost all antimalarial drugs have accentuated the urgent need for new antimalarial drugs and drug targets for both prophylaxis and chemotherapy. The aim of the study was to discover effective plant extracts against Plasmodium falciparum. In the present study, the hexane, chloroform, ethyl acetate, acetone, and methanol extracts of Citrus sinensis (peel), Leucas aspera, Ocimum sanctum, Phyllanthus acidus (leaf), Terminalia chebula (seed) were tested for their antimalarial activity against chloroquine (CQ)-sensitive (3D7) strain of P. falciparum which was cultured following the candle-jar method. Antimalarial evaluations of daily replacement of culture medium containing CQ and different plant crude extracts were performed on 96-well plates at 37°C for 24 and 48 h. Parasitemia was determined microscopically on thin-film Giemsa-stained preparations. Plant extracts were tested for their cytotoxicity using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay on human laryngeal cancer cell line (HEp-2) and normal cell line (Vero). Out of the 25 extracts tested, six showed good (IC₅₀ 4.76–22.76 μg/mL), 15 exhibited moderate (IC₅₀ 31.42–88.03 μg/mL), while four displayed mild (IC₅₀ > 100 μg/mL) antiplasmodial activity. The leaf ethyl acetate and methanol extracts of L. aspera; ethyl acetate, acetone, and methanol extracts of P. acidus; and seed acetone extract of T. chebula had good antiplasmodial activity (IC₅₀ = 7.81, 22.76, 9.37, 14.65, 12.68, and 4.76 μg/mL) with selectivity indices 5.43, 2.04, 4.88, 3.35, 3.42, and 9.97 for HEp-2 and >5.79, >2.20, >11.75, >3.41, >3.94, and >7.38 for Vero cells, respectively. These analyses have revealed for the first time that the components present in the solvent extracts of L. aspera, P. acidus, and T. chebula have antiplasmodial activity. The high antiplasmodial activity observed make these plants good candidates for isolation of anti-protozoal compounds which could serve as new lead structures for drug development.     

In vitro and in vivo trypanocidal activity of native plants from the Yucatan Peninsula

Ethanol extracts of Senna villosa, Serjania yucatanensis, Byrsonima bucidaefolia, and Bourreria pulchra were evaluated for their in vitro activity against epimastigotes and trypomastigotes of Trypanosoma cruzi. Results showed that the leaf extracts of S. yucatanensis and B. pulchra were the most active against epimastigotes (IC₁₀₀ = 100 μg/mL) and trypomastigotes of T. cruzi (95% or more reduction in the number of parasites at 100 and 50 μg/mL). However, only the leaf extract of S. yucatanensis showed significant trypanocidal activity when tested in vivo, reducing 75% of the parasitemia in infected mice at 100 mg/kg. This same extract inhibited the egress of trypomastigotes from infected cells and proved not to be cytotoxic (IC₅₀ = 318.8 ± 2.3 μg/mL).     

In vitro antiplasmodial activity and cytotoxicity of crude extracts and compounds from the stem bark of <Emphasis Type="Italic">Kigelia africana</Emphasis> (Lam.) Benth (Bignoniaceae)

In order to assess the potential of the stem bark of Kigelia africana (Lam.) Benth as source of new anti-malarial leads, n-hexane and ethyl acetate (EtOAc) extracts and four compounds isolated from the stem bark were screened in vitro against the chloroquine-resistant W-2 and two field isolates of Plasmodium falciparum using lactate dehydrogenase assay. The products were also tested for their cytotoxicity on LLC/MK2 monkey kidney cells. The EtOAc extract exhibited a significant antiplasmodial activity (IC₅₀ = 11.15 μg/mL on W-2; 3.91 and 4.74 μg/mL on field CAM10 and SHF4 isolates, respectively), whereas the n-hexane fraction showed a weak activity (IC₅₀ = 73.78 μg/mL on W-2 and 21.85 μg/mL on SHF4). Three out of the four compounds showed good activity against all the three different parasite strains (IC₅₀ < 5 μM). Specicoside exhibited the highest activity on W-2 (IC₅₀ = 1.54 μM) followed by 2β, 3β, 19α-trihydroxy-urs-12-en-28-oic acid (IC₅₀ = 1.60 μM) and atranorin (IC₅₀ = 4.41 μM), while p-hydroxycinnamic acid was the least active (IC₅₀ = 53.84 μM). The EtOAc extract and its isolated compounds (specicoside and p-hydroxycinnamic acid) were non-cytotoxic (CC₅₀ > 30 μg/mL), whereas the n-hexane extract and two of its products, atranorin and 2β, 3β, 19α-trihydroxy-urs-12-en-28-oic acid showed cytotoxicity at high concentrations, with the last one being the most toxic (CC₅₀ = 9.37 μg/mL). These findings justify the use of K. africana stem bark as antimalaria by traditional healers of Western Cameroon, and could constitute a good basis for further studies towards development of new leads or natural drugs for malaria.     

Molluscicidal activity of some marine substances against the snail <Emphasis Type="Italic">Biomphalaria glabrata</Emphasis> (Mollusca,Planorbidae)

Freshwater snails of the genus Biomphalaria play a major role as intermediate hosts of Schistosoma mansoni, the etiologic agent of schistosomiasis. While Biomphalaria spp. control by molluscicides is one of the main strategies to reduce the snail population in infected areas, there are few effective molluscicides commercially available. Natural products may be considered as potentially useful and safe molluscicides. We have evaluated the molluscicidal activity of 12 extracts from ten marine organisms on adult and embryonic stages of Biomphalaria glabrata. Only extracts of the red algae Liagora farinosa and of the sponge Amphimedon viridis presented molluscicidal activity. Lethal concentration (LC)₅₀ values obtained were 120 μg/mL for L. farinosa CH₂Cl₂ extract (apolar fraction) and 20 μg/mL for A. viridis extract and halitoxin. The polar alga fraction and halitoxin had no effect on B. glabrata embryos. The algae apolar fraction was active on B. glabrata in all embryonic development stages, with LC₅₀ values for blastulae at 42 μg/mL, gastrulae at 124 μg/mL, trochophore at 180 μg/mL, and veliger at 222 μg/mL. This is the first report of extracts from marine organisms which presented molluscicidal activity.     

In vitro activities of plant extracts on human Loa loa isolates and cytotoxicity for eukaryotic cells

Loa loa, a filarial worm, can cause fatal encephalitis in humans. In an attempt to find alternatives to the standard treatments (ivermectin and diethylcarbamazine citrate), we tested 12 methanolic extracts of nine traditional plant remedies. The extracts (100–0.09 μg/ml) were incubated with 20 Loa loa microfilariae isolated from patients at 37°C with 5% CO₂ in modified Eagle’s medium supplemented with 10% fetal serum and antibiotics. Activity was evaluated 120 h later by counting live microfilariae under a microscope. Cytotoxicity for eukaryotic cells was estimated by measuring 3-[4,5-dimethylthiazol-2-yl]-2-5 diphenyl tetrazolium bromide transformation to formazan at 450 nM in a spectrophotometer. The plants tested were Lophira alata, Greenwayodendron suaveolens, Uapaca togoensis, Zanthoxylum heitzii, Peperomia pellucida, Piptadeniastrum africanum, Petersianthus macrocarpus, Vernonia conferta, and Vernonia hymenolepis. Chemical screening showed that most of the extracts contained reducing sugars, tannin or polyphenols, sterols or triterpenes, saponosides, and alkaloids. None contained carotinoids and few contained flavonoids. The 50% lethal concentration ranged from 0.22 to 70.28 μg/ml, while the 50% inhibitory concentration for eukaryotic cells (IC₅₀) ranged from 8.52 to 119.52 μg/ml. Extracts of P. macrocarpus (selectivity index = 72.16), P. africanum (13.69), Z. heitzii (12.11), and L. alata (9.26) were highly selective for L. loa.     

In vitro anthelmintic effects of Bridelia ferruginea,Combretum glutinosum,and Mitragyna inermis leaf extracts on Haemonchus contortus,an abomasal nematode of small ruminants

Gastrointestinal nematodes remain a major constraint on the health, welfare, and production of small ruminants. This study was conducted to evaluate three plant extracts (from Bridelia ferruginea, Combretum glutinosum, and Mitragyna inermis) as effective remedies against gastrointestinal parasites of small ruminants. Phytochemical screening was conducted on the plant leaves, and the potential anthelmintic properties of these plants were tested in vitro on Haemonchus contortus using the egg hatch, larval migration, and adult worm motility assays. The phytochemical screening of the leaves revealed the presence of several bioactive components in all the plants. The number of eggs that hatched was reduced in a concentration-dependent manner (p < 0.01) upon treatment with the methanol extract of B. ferruginea and the acetone extracts of C. glutinosum and M. inermis. The inhibitory effect of the acetone extract of B. ferruginea and the methanol extracts of C. glutinosum and M. inermis was not concentration-dependent (p > 0.05). There was a significant difference (p < 0.05) in the reduction in larval migration between the lowest concentrations (75 to 150 μg/mL) and the highest concentrations (300 to 1200 μg/mL) of plant extracts. The ability of plant extracts to affect the mobility of the adult worms was not concentration-dependent (p > 0.05); however, it was dependent on the time of incubation (p < 0.01). At the highest concentration (2400 μg/mL), all adult worms were motionless after 24 h of exposure, while at the lowest concentration (< 150 μg/mL), this occurred after 48 h of exposure. M. inermis and C. glutinosum extracts were more effective than B. ferruginea extracts (p < 0.05). Overall, these results suggest that these plants used by small-scale farmers possess antiparasitic properties useful for helminthiasis control. However, the effects of the plants remain to be confirmed via in vivo assays and toxicity tests in further studies.

     

Activity of doripenem against extended-spectrum β-lactamase-producing Enterobacteriaceae and Pseudomonas aeruginosa isolates

The in vitro activity of doripenem was evaluated against a recent collection of extended-spectrum β-lactamase (ESBL)-producing Enterobacteriaceae and Pseudomonas aeruginosa isolates (201 ESBL-producing Enterobacteriaceae [153 Escherichia coli and 48 Klebsiella pneumoniae] and 201 P. aeruginosa). Comparator agents included amikacin, tobramycin, ciprofloxacin, cefepime, cefotaxime, ceftazidime piperacillin-tazobactam, imipenem, and meropenem. Both doripenem and meropenem inhibited 100% of the ESBL-producing Enterobacteriaceae at ≤0.5 μg/mL. For these isolates, the MIC₉₀ of doripenem (0.12 μg/mL) was 4-fold lower than that of imipenem (0.5 μg/mL). Against P. aeruginosa, the MIC₉₀ of doripenem and meropenem was 2 μg/mL, 4-fold lower than that of imipenem (8 μg/mL). At an MIC of ≤2 μg/mL, doripenem, meropenem, and imipenem inhibited 90.5%, 89.6%, and 82.1% of P. aeruginosa isolates, respectively. Doripenem maintained activity against imipenem-nonsusceptible isolates of P. aeruginosa; at an MIC of ≤4 μg/mL, it inhibited 15 of the 25 isolates with MICs for imipenem of >4 μg/mL. Doripenem is active against ESBL-producing Enterobacteriaceae and P. aeruginosa isolates. Its activity is similar to that of meropenem and slightly better than that of imipenem. The results of this study suggest that doripenem could be an alternative therapeutic agent for infections caused by these organisms.     

In vitro antimalarial activity of medicinal plant extracts against Plasmodium falciparum

Malaria is a major global public health problem, and the alarming spread of drug resistance and limited number of effective drugs now available underline how important it is to discover new antimalarial compounds. In the present study, ten plants were extracted with ethyl acetate and methanol and tested for their antimalarial activity against chloroquine (CQ)-sensitive (3D7) and CQ-resistant (Dd2 and INDO) strains of Plasmodium falciparum in culture using the fluorescence-based SYBR Green assay. Plant extracts showed moderate to good antiparasitic effects. Promising antiplasmodial activity was found in the extracts from two plants, Phyllanthus emblica leaf 50% inhibitory concentration (IC₅₀) 3D7: 7.25 μg/mL (ethyl acetate extract), 3.125 μg/mL (methanol extract), and Syzygium aromaticum flower bud, IC₅₀ 3D7:13 μg/mL, (ethyl acetate extract) and 6.25 μg/mL (methanol extract). Moderate activity (30–75 μg/mL) was found in the ethyl acetate and methanol extracts of Abrus precatorius (seed) and Gloriosa superba (leaf); leaf ethyl acetate extracts of Annona squamosa and flower of Musa paradisiaca. The above mentioned plant extracts were also found to be active against CQ-resistant strains (Dd2 and INDO). Cytotoxicity study with P. emblica leaf and S. aromaticum flower bud, extracts showed good therapeutic indices. These results demonstrate that leaf ethyl acetate and methanol extracts of P. emblica and flower bud extract of S. aromaticum may serve as antimalarial agents even in their crude form. The isolation of compounds from P. emblica and S. aromaticum seems to be of special interest for further antimalarial studies.     

Larvicidal effects of various Euro-Asiatic plants against Culex quinquefasciatus Say larvae (Diptera: Culicidae)

Extracts from 56 species of plants in the Euro-Asiatic region were tested for larvicidal activity against the fourth larval instar of the mosquito Culex quinquefasciatus Say (Diptera: Culicidae). All plant extracts showed larvicidal activity after 24 h of exposure to the plant extracts in a maximal dose of 500 ppm. The extracts of the plants Otanthus maritimus and Ammi visnaga displayed the highest larvicidal effect (LD₅₀ 7 and 9 ppm, respectively) followed by Acer pseudoplatanus, Humulus japonicus, Acer platanoides, Satureja hortensis, Ocimum basilicum and Thymus vulgaris (LD₅₀ 23, 25, 28, 28, 32 and 48 ppm respectively). For eight species, the appraisal value of LD₅₀ was between 51 and 100 ppm, another eight species from 101 to 200 ppm, 15 species from 201 to 500 ppm and for 17 species, low mortality showed no lethal dose (LD₅₀ > 500 ppm).     

Antiplasmodial potential of medicinal plant extracts from Malaiyur and Javadhu hills of South India

The emergence and spread of Plasmodium falciparum with resistance to chloroquine (CQ), the safest and cheapest anti-malarial drug, coupled with the increasing cost of alternative drugs especially in developing countries have necessitated the urgent need to tap the potential of plants for novel anti-malarials. The present study investigates the anti-malarial activity of the methanolic extracts of 13 medicinal plants from the Malaiyur and Javadhu hills of South India against blood stage CQ-sensitive (3D7) and CQ-resistant (INDO) strains of P. falciparum in culture using the fluorescence-based SYBR Green I assay. Sorbitol-synchronized parasites were incubated under normal culture conditions at 2% hematocrit and 1% parasitemia in the absence or presence of increasing concentrations of plant extracts. CQ and artemisinin were used as positive controls, while 0.4% DMSO was used as the negative control. The cytotoxic effects of extracts on host cells were assessed by functional assay using HeLa cells cultured in RPMI containing 10% fetal bovine serum, 0.21% sodium bicarbonate and 50???g/mL gentamycin (complete medium). Plant extracts (bark methanol extracts of Annona squamosa (IC₅₀, 30???g/mL), leaf extracts of Ocimum gratissimum (IC₅₀, 32???g/mL), Ocimum tenuiflorum (IC₅₀, 31???g/mL), Solanum torvum (IC₅₀, 31???g/mL) and Justicia procumbens (IC₅₀, 63???g/mL), showed moderate activity. The leaf extracts of Aristolochia indica (IC₅₀, 10???g/mL), Cassia auriculata (IC₅₀, 14???g/mL), Chrysanthemum indicum (IC₅₀, 20???g/mL) and Dolichos biflorus (IC₅₀, 20???g/mL) showed promising activity and low activity was observed in the flower methanol extracts of A. indica , leaf methanol extract of Catharanthus roseus, and Gymnema sylvestre (IC₅₀, >100???g/mL). These four extracts exhibited promising IC₅₀ (??g/mL) of 17, 24, 19 and 24 respectively also against the CQ resistant INDO strain of P. falciparum. The high TC₅₀ in mammalian cell cytotoxicity assay and the low IC₅₀ in anti-malarial P. falciparum assay indicates selectivity and good resistance indices in the range of 0.9?C1.7 for leaf extracts of A. indica, C. auriculata, C. indicum and D. biflorus suggests that these may serve as anti-malarial agents even in their crude form. These results indicate a possible explanation of the traditional use of some of these medicinal plants against malaria or malaria-like conditions.     

Efficacy of medicinal plant extracts against malarial vector, <Emphasis Type="Italic">Anopheles subpictus</Emphasis> Grassi

Insecticides of botanical origin may serve as suitable alternative biocontrol techniques in the future. The aim of this study was to evaluate the adulticidal activity and adult emergence inhibition (EI) of leaf hexane, chloroform, ethyl acetate, acetone, and methanol extracts of Aegle marmelos (Linn.) Correa ex Roxb, Andrographis lineata Wallich ex Nees., Andrographis paniculata (Burm.f.) Wall. ex Nees., Cocculus hirsutus L. Diels, Eclipta prostrata L., and Tagetes erecta L. tested against malarial vector, Anopheles subpictus Grassi (Diptera: Culicidae). All plant extracts showed moderate adulticidal activity and EI effects after 24 h of exposure at 1,000 ppm; however, the highest adulticidal activity was observed in ethyl acetate extract of A.lineata, chloroform extract of A.paniculata, acetone extract of C.hirsutus, and methanol extract of T.erecta (LD₅₀ = 126.92, 95.82, 109.40, and 89.83 ppm; LD₉₀ = 542.95, 720.82, 459.03, and 607.85 ppm); and effective EI was found in leaf acetone extract of the A. marmelos, ethyl acetate extract of A.lineata, methanol extracts of C. hirsutus, and T.erecta, (EI₅₀ = 128.14, 79.39, 143.97, and 92.82 ppm; EI₉₀ = 713.53, 293.70, 682.72, and 582.59 ppm), respectively, against A. subpictus. These results suggest that the leaf methanol extract of C. hirsutus and T.erecta have the potential to be used as an ideal eco-friendly approach for the control of A. subpictus. Therefore, this study provides first report on the mosquito adulticidal activity and EI of plant extracts against malaria vector.     

Susceptibility profile of Candida rugosa (Diutina rugosa) against antifungals and compounds of essential oils

Candida rugosa (recently reclassified Diutina rugosa) is an emerging pathogen affecting humans and animals. Candida resistance to existing drugs is an important factor to be monitored, as well as the need of researching alternatives to conventional antifungals. Here, we evaluated the in vitro effects of some antifungals and major components of essential oils by the broth microdilution method (CLSI M27-A3) against fifteen C. rugosa strains from animals isolated and molecular identificated. The results showed MIC₉₀ of: 0.125 μg/mL to ketoconazole and voriconazole, 0.25 μg/mL to micafungin, 0.5 μg/mL to anidulafungin, 1 μg/mL to caspofungin, 2 μg/mL to amphotericin B, itraconazole and flucytosin, 8 μg/mL to fluconazole, 16 μg/mL to nystatin and >128 μg/mL to terbinafine. The compounds carvacrol (MIC₉₀ 320 μg/mL), thimol (MIC₉₀ 320 μg/mL) and cinnamaldehyde (MIC₉₀ 160 μg/mL) demonstrated antifungal activity against the samples tested.     

Insecticidal and repellent activities of thymol from the essential oil of Trachyspermum ammi (Linn) Sprague seeds against Anopheles stephensi

Essential oil of seeds of Trachyspermum ammi (Linn.) Sprauge and its pure constituent thymol showed promising results when evaluated for larvicidal, oviposition-deterrent, vapor toxicity, and repellent activity against malarial vector, Anopheles stephensi. Thymol was 1.6-fold more toxic than the oil toward fourth-instar larvae of A. stephensi with LD₅₀ values of 48.88 and 80.77 μg/ml, respectively. Egg laying by female adults of A. stephensi was much significantly reduced when exposed to vapors of thymol compared to the oil of T. ammi seeds, and similar effects were recorded for subsequent egg hatching and larval survival. Vapor toxicity assay showed LC₅₀ value of 79.5 mg/mat for thymol against adults of A. stephensi, whereas the crude oil exhibited the LC₅₀ value of 185.4 mg/mat. Thymol provided complete repellency toward A. stephensi adults at the dose of 25.0 mg/mat after 1 h duration, whereas same degree of repellency was obtained by the oil at the dose of 55.0 mg/mat, indicating its double-fold activity than the oil.     

In vitro sensitivity of Plasmodium falciparum field isolates to extracts from Cameroonian Annonaceae plants

In a search for new plant-derived antimalarial extracts, 19 fractions were obtained from three Annonaceae species, Uvariopsis congolana (leaf, stem), Polyalthia oliveri (stem bark), and Enantia chlorantha (stem, stem bark) with yields ranging from 0.33% to 4.60%. The extracts were prepared from 500 g of each plant part, using organic solvents to afford five methanolic fractions (acetogenin rich), five water fractions, five hexane fractions, and four interface precipitates. Evaluation of the activity of fractions in vitro against field isolates of the malaria parasite Plasmodium falciparum showed that acetogenin-rich fractions and interface precipitates were the most potent, with IC₅₀ values ranging from 0.05 to 8.09 μg/ml. Sensitivity of parasite isolates to plant extracts varied greatly, with over 100-fold difference from isolate to isolate in some cases. The active acetogenin-rich fractions and interface precipitates were assessed in combination with chloroquine in the same conditions, and showed additive interaction in the huge majority of cases. Synergistic interactions were found in some cases with acetogenin-rich fractions. Acute toxicity of promising fractions was evaluated through oral administration in Swiss albino mice. Tested fractions appeared to be safe, with LD₅₀ values higher than 2 g/kg. In summary, acetogenin-rich fractions from Annonaceae species showed high potency against P. falciparum field isolates and safety by oral administration in mice, supporting their detailed investigation for antimalarial drug discovery.     

Mosquito larvicidal properties of silver nanoparticles synthesized using Heliotropium indicum (Boraginaceae) against Aedes aegypti,Anopheles stephensi,and Culex quinquefasciatus (Diptera: Culicidae)

Mosquitoes transmit dreadful diseases to human beings wherein biological control of these vectors using plant-derived molecules would be an alternative to reduce mosquito population. In the present study activity of aqueous leaf extract and silver nanoparticles (AgNPs) synthesized using Helitropium indicum plant leaves against late third instar larvae of Aedes aegypti, Anopheles stephensi and Culex quinquefasciatus. The range of varying concentrations of synthesized AgNPs (8, 16, 24, 32, and 40 μg/mL) and aqueous leaf extract (30, 60, 90, 120, and 150 μg/mL) were tested against the larvae of Anopheles stephensi, Aedes aegypti, and Culex quinquefasciatus. The synthesized AgNPs from H. indicum were highly toxic than crude leaf aqueous extract in three important vector mosquito species. The results were recorded from UV–Vis spectrum, Fourier transform infrared spectroscopy, scanning electron microscopy, energy-dispersive X-ray spectroscopy analysis, transmission electron microscopy, and histogram. The synthesized AgNPs showed larvicidal effects after 24 h of exposure. Considerable mortality was evident after the treatment of H. indicum for all three important vector mosquitoes. The LC₅₀ and LC₉₀ values of H. indicum aqueous leaf extract appeared to be effective against A. stephensi (LC₅₀, 68.73 μg/mL; LC₉₀, 121.07 μg/mL) followed by A. aegypti (LC₅₀, 72.72 μg/mL; LC₉₀, 126.86 μg/mL) and C. quinquefasciatus (LC₅₀, 78.74 μg/mL; LC₉₀, 134.39 μg/mL). Synthesized AgNPs against the vector mosquitoes of A. stephensi, A. aegypti, and C. quinquefasciatus had the following LC₅₀ and LC₉₀ values: A. stephensi had LC₅₀ and LC₉₀ values of 18.40 and 32.45 μg/mL, A. aegypti had LC₅₀ and LC₉₀ values of 20.10 and 35.97 μg/mL, and C. quinquefasciatus had LC₅₀ and LC₉₀ values of 21.84 and 38.10 μg/mL. No mortality was observed in the control. These results suggest that the leaf aqueous extracts of H. indicum and green synthesis of silver nanoparticles have the potential to be used as an ideal ecofriendly approach for the control of A. stephensi, A. aegypti, and C. quinquefasciatus. This is the first report on the mosquito larvicidal activity of the plant extracts and synthesized nanoparticles.     

Efficacy of cecropin A-melittin peptides on a sepsis model of infection by pan-resistant <Emphasis Type="Italic">Acinetobacter baumannii</Emphasis>

Pan-resistant Acinetobacter baumannii have prompted the search for therapeutic alternatives. We evaluate the efficacy of four cecropin A-melittin hybrid peptides (CA-M) in vivo. Toxicity was determined in mouse erythrocytes and in mice (lethal dose parameters were LD₀, LD₅₀, LD₁₀₀). Protective dose 50 (PD₅₀) was determined by inoculating groups of ten mice with the minimal lethal dose of A. baumannii (BMLD) and treating with doses of each CA-M from 0.5 mg/kg to LD₀. The activity of CA-Ms against A. baumannii was assessed in a peritoneal sepsis model. Mice were sacrificed at 0 and 1, 3, 5, and 7-h post-treatment. Spleen and peritoneal fluid bacterial concentrations were measured. CA(1–8)M(1–18) was the less haemolytic on mouse erythrocytes. LD₀ (mg/kg) was 32 for CA(1–8)M(1–18), CA(1–7)M(2–9), and Oct-CA(1–7)M(2–9), and 16 for CA(1–7)M(5–9). PD₅₀ was not achieved with non-toxic doses (≤LD₀). In the sepsis model, all CA-Ms were bacteriostatic in spleen, and decreased bacterial concentration (p < 0.05) in peritoneal fluid, at 1-h post-treatment; at later times, bacterial regrowth was observed in peritoneal fluid. CA-Ms showed local short-term efficacy in the peritoneal sepsis model caused by pan-resistant Acinetobacter baumannii.     

Screening for feeding deterrent activity of herbal extracts against the larvae of malaria vector Anopheles subpictus Grassi

This no-choice, laboratory study focuses on the feeding of homogeneous powdered, dried, yeast with different plant extracts on mosquito fourth-instar larvae to determine the effects on their mortality. Screening for antifeedant activity of plant extracts with some known medicinal attributes could lead to the discovery of new agents for vector control. The aim of this study was to investigate the antifeedant activity of crude leaf hexane, ethyl acetate, acetone, and methanol extracts of Andrographis lineata Wallich ex Nees. (Acanthaceae), Anisomeles malabarica (L.) Sims. (Lamiaceae), Argemone mexicana L. (Papaveraceae), Aristolochia bracteolata Lam. (Aristolochiaceae), Chrysanthemum indium L. (Asteraceae), Datura metal L. (Solanaceae), Eclipta prostrata L. (Asteraceae), and Sesbania grandiflora (L.) Pers. (Fibaceae) against the fourth-instar larvae of Anopheles subpictus Grassi (Diptera:Culicidae). All the crude extracts showed antifeedant activity in a dose-dependent manner. The plant extracts exhibited a significant antifeedant activity after 24 and 48 h of exposure; however, the highest larval mortality was found in leaf ethyl acetate extract of A. malabarica, acetone extract E. prostrata, methanol extract of A. lineata, C. indium, and S. grandiflora after 24 h (LC₅₀ = 2.53, 2.82, 2.31, 2.56, and 2.08 mg/mL; LC₉₀ = 6.40, 8.06, 7.45, 6.98, and 6.20 mg/mL), respectively. The hexane extract of A. lineata, D. metal, methanol extract of A. bracteolata and E. prostrata showed larval mortality after 48 h (LC₅₀ = 3.05, 2.11, 3.00, and 2.18 mg/mL; LC₉₀ = 9.06, 6.22, 8.23, and 5.77 mg/mL), respectively. One hundred percent larval mortality was observed in methanol extract of A. lineata, and C. indium after 24 h and the hexane extract of A. lineata and D. metal after 48 h at 10 mg/100 mL. The methanol extracts of A. lineata and C. indium significantly increased larval mortality in comparison to larvae fed with untreated diet. Bacillus thuringiensis subsp. israelensis is widely accepted as a biological pesticide because of its highly specific activity against dipteran insects without adverse effects on other organisms. The feeding deterrent activity of different herbal extracts against the larvae of malaria vector A. subpictus exhibited significantly lower toxicity compare with the bio larvicides, B. thuringiensis. These results suggest that the methanol extract of A. lineata, C. indium, the hexane extract of A. lineata and D. metal have the potential to be used as an ideal eco-friendly approach for the control of the medically important vector A. subpictus. These findings corroborate traditional insecticidal application of selected plants and the results can be extended for the control of mosquitoes.