Hexane Fraction Research Articles

Earias vittella management by utilizing obnoxious weeds extracts of Jammu and Kashmir Himalayas, India

All the three agro-ecological zones (sub-tropical, intermediate and temperate) of the Jammu province were surveyed for potential pesticidal plants. Methanol extracts of all the thirteen plants / plant parts and fractions were assessed for insecticidal activity. Eight treatments (T3 –Boerhavia diffusa stem methanolic extract, T6 –Boerhavia diffusa roots methanolic extract, T7 –Boerhavia diffusa roots hexane fraction, T12 –Arisaema flavum stem + leaves methanol extract, T13 –Arisaema flavum stem + leaves hexane fraction, T14 –Arisaema flavum stem + leaves acetone fraction, T15 –Arisaema flavum roots / tubers methanol extract and T17 –Arisaema flavum roots / tubers acetone fraction) recorded cent percent mortality of first instar larvae, within four hours. All the extracts / fractions evaluated against Earias vitella exhibited contact toxicity, and ovicidal action. The growth indices were also affected. Few extracts / fractions were so toxic that they exhibited 100% control. When larvae were fed on extract / fraction treated food for growth indices studies, in many cases larvae died. These extracts/ fractions have great potential to be developed as botanical pesticide. Active pesticidal compounds from few promising plants may be extracted and further studied for their pesticidal activity. The present studies suggest that the plant extract may be fractionated for better results.

The Inhibition of NLRP3 Inflammasome and IL-6 Production by Hibiscus noldeae Baker f. Derived Constituents Provides a Link to Its Anti-Inflammatory Therapeutic Potentials.

The activation of NOD-, LRR-, and pyrin domain-containing protein 3 (NLRP3) inflammasome and/or its components is associated with the physio-pathogenesis of many respiratory diseases including asthma, COPD (chronic obstructive pulmonary disease), SARS Cov-2 (severe acute respiratory syndrome coronavirus 2), and in several autoimmune diseases. Hibiscus noldeae Baker f. has been widely reported to be traditionally used in the treatment of different ailments, some of which are of inflammatory background such as asthma, wounds, headache, etc. However, the claims have not been supported by evidence at the molecular and functional levels. Here, we report on the bio-guided fractionation of H. noldeae and assessment of the inhibitory properties of some fractions and purified compounds on NLRP3 inflammasome and Interleukin 6 (IL-6). The activation of the NLRP3 inflammasome was determined by detecting the activity of caspase-1 and the production of Interleukin 1β (IL-1β) in Lipopolysaccharide (LPS) and ATP-stimulated Tamm-Horsfall Protein 1 (THP-1) macrophages, while the production of IL-6 was studied in LPS-stimulated RAW264.7 mouse macrophages. It was observed that hexane and ethyl acetate fractions of the crude extract of the aerial parts of H. noldeae, as well as caffeic acid, isoquercetin, and ER2.4 and ER2.7 fractions revealed significant inhibitory effects on Caspase-1 activities, and on IL-1β and IL-6 production. The ER2.4 and ER2.7 fractions downregulated the production of IL-1β and IL-6, in a similar range as the caspase-1 inhibitor AC-YVAD-CHO and the drug Dexamethasone, both used as controls, respectively. Overall, our work does provide the very first scientific based evidence for Hibiscus noldeae anti-inflammatory effects and widespread use by traditional healers in Rwanda for a variety of ailments.

Extracts from Six Native Plants of the Yucatán Peninsula Hinder Mycelial Growth of Fusarium equiseti and F. oxysporum, Pathogens of Capsicum chinense.

Fusarium equiseti strain FCHE and Fusarium oxysporum strain FCHJ were isolated from the roots of wilting habanero pepper (Capsicum chinense Jacq.) seedlings with root rot. Toward developing a biorational control of these serious phytopathogenic strains, ethanolic (EE) and aqueous (AE) extracts of different vegetative parts of 40 tropical native plants of the Yucatán Peninsula were screened for antifungal activity. Extracts of six out of 40 assayed plants were effective, and the most inhibitory extracts were studied further. EEs from Mosannona depressa (bark from stems and roots), Parathesis cubana (roots), and Piper neesianum (leaves) inhibited mycelial growth of both strains. Each active EE was then partitioned between hexane and acetonitrile. The acetonitrile fraction from M. depressa stem bark (MDT-b) had the lowest minimum inhibitory concentration of 1000 µg/mL against both pathogens and moderate inhibitory concentration (IC50) of 462 against F. equiseti and 472 µg/mL against F. oxysporum. After 96 h treatment with EE from M. depressa stem bark, both strains had distorted hyphae and conidia and collapsed conidia in scanning electron micrographs. Liquid chromatography–ultraviolet–high resolution mass spectrometry analysis revealed that the major component of the fraction was α-asarone. Its antifungal effect was verified using a commercial standard, which had an IC50 of 236 µg/mL against F. equiseti and >500 µg/mL against F. oxysporum. Furthermore, the P. cubana hexane fraction and P. neesianum acetonitrile fraction had antifungal activity against both Fusarium pathogens. These compounds provide new options for biorational products to control phytopathogenic fungi.

Phytochemical and antioxidant characterization, cytogenotoxicity and antigenotoxicity of the fractions of the ethanolic extract of in Poincianella bracteosa (Tul.) L.P. Queiroz

ABSTRACT Poincianella bracteosa has been widely used in folk medicine to treat catarrhal infections, diarrhea, and anemia; however, phytochemical and toxicogenetic data are still lacking. The objective of this study was to examine the phytochemical and antioxidant characteristics as well as assess cytogenotoxicity and antigenotoxicity in hexane (HF), ether (EF) and ethyl acetate (AF) fractions of P. bracteosa leaves using Allium cepa bioassay. Phytochemical analysis revealed the presence of saponins and phenolic groups. EF fraction contained a higher content of total phenolics (441.23 ± 1.82 mg GAE/g), while HF fraction showed a higher content of total flavonoids (84.77 ± 5.33 mg QE/g). Higher antioxidant activity was observed in EF (EC50 25.06 ± 0.07 µg/ml). Cytotoxic effect was verified for all fractions, but no chromosomal alterations were observed in the A. cepa assay. With respect to antigenotoxicity, the protective effect of EF and AF fractions was attributed to as evidenced by the modulation of mutagenic action of methyl methanesulfonate (MMS), mainly by inhibiting the development of micronuclei. Among the fractions, EF was considered the most promising, as it exhibited higher antioxidant activity, was not genotoxic, exerted protective activity against the damage induced by MMS and also presented cytotoxic activity, a desired quality in the search for natural anticarcinogenic compounds.

Bioactivities, heavy metal contents and toxicity effect of macroalgae from two sites in Madura, Indonesia

Abstract Sargassum duplicatum and Padina tetrastromatica seaweed species collected from oil and a non-oil extraction site at Madura Island were investigated in this study for selected bioactivities, heavy metals and toxicity effects. The collected seaweeds were evaluated for their phytochemical constituents, total phenolic contents (TPC), antioxidant activities, antidiabetic activities, anticancer activities, toxicities and heavy metals using Folin-Ciocalteus method, the 2,2-diphernyl-1 picrylhydrazyl (DPPH), α-glucosidase enzyme, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT), Brine Shrimp Lethality Test (BSLT) and atomic absorption spectrophotometer, respectively. The crude extracts (C), normal hexane (N), ethyl acetate (E), and methanol residue fractions (M) were studied. The highest TPC (589.79 ± 7.14 mg GAE/g) was observed in ethyl acetate fraction of P. tetrastromatica from the non-oil extraction site. Meanwhile, the crude extracts and all fractions showed potent antioxidant, antidiabetic, and cytotoxic activities with ethyl acetate fraction of P. tetrastromatica from non-oil extraction site displaying the highest effects (IC50 25.25 ± 5.15, 249.12 ± 1.77 and 70.56 ± 2.56 µg/mL: antioxidant, antidiabetic, cytotoxic activities respectively). In the brine shrimp assay, the crude extracts and all fractions of both species from the two sites were non-toxic with exception of the hexane fraction of P. tetrastromatica from oil site which was very toxic after 24 h incubation. However, the crude extract of S. duplicatum and ethyl acetate fraction of P. tetrastromatica from oil extraction site were mildly toxic except the hexane fraction of P. tetrastromatica from oil site which was very toxic after 48 h incubation while samples of both species from the non-oil site were nontoxic. In each species, the concentration of Cd from the oil extraction site was higher than those of the non-oil site with the values of P. tetrastromatica leading and a similar observation occurred Cu in P. tetrastromatica but the same Cu was negligible in S. duplicatum as Pb was negligible in both species. According to the findings of this current study, it is safe to conclude that both S. duplicatum and P. tetrastromatica from Madura Island have antioxidant, antidiabetic and cytotoxic activity, we therefore recommend these species from the non-oil extraction site for drug candidates against the various health abnormally they seem to inhibit.

Uji Aktivitas Antibakteri Ekstrak Metanol dan Fraksi Daun Kenikir (Cosmos caudatus Kunth) terhadap Salmonella typhi

The leaves of kenikir are known to have many benefits, one of which can be used as medicine. Kenikir leaves are reported to have antibacterial activity against the bacteria Salmonella typhi (S.typhi). S. typhi is a bacterium that causes typhoid fever. Typhoid fever is still an endemic disease in Asian countries, especially Indonesia. Typhoid fever became the third largest disease in Indonesia in 2010. The study related to the antibacterial activity of kenikir leaf fraction to S. typhi has never been reported. Therefore, it is necessary to conduct research related to the antibacterial activity of extracts and leaf fractions of kenikir to compare their potential against S. typhi. The study was conducted using the disk diffusion method using 5 series of concentrations namely 5%, 10%, 15%, 20%, and 30%. Tests were carried out on methanol extract, hexane, ethyl acetate, and methanol-water fraction. The results showed that highest inhibition zone diameter is 7,75 mm which is reached by methanol extract. The order of the highest inhibiting zone diameter are extract, hexane, ethyl acetate, and methanol-water fraction.

Process Intensification of Propionic Acid Extraction and its Recovery by Distillation in Microchannel

Extraction in microchannels has been studied extensively. However, the recovery of the solute and the solvent from the extract in microchannels has not been part of any reports. Hence, in this work, extraction of propionic acid (PA) using n-hexane and toluene and its subsequent recovery by distillation (flash) in microchannels is reported. Moreover, a total annual cost comparison between microchannels and conventional extraction and distillation units has been made. Microchannel extraction and distillation were conducted in a serpentine microchannel. The maximum percentage extraction is 36.3% with toluene. The maximum extraction efficiency is 99.6% with toluene and 98.4% with n-hexane. The overall KLa is in the range of 0.01-0.25 s-1. Distillation was conducted in the presence of nitrogen gas. The solvents n-hexane and toluene were recovered with high percentage recovery of 98% and 73% respectively at 0.01 mL/min feed rate. The maximum power requirement is in the range (2.7-3.8) kWh. The overall pressure drop for the distillation is about 3.4 kPa for both the systems. The hexane, toluene and PA mole fractions agree well with the ASPEN Plus results. The total annual cost (TAC) analysis indicates that microchannel can lead to significant capital and operating cost benefits.

In Vitro and In Vivo Screening of Wild Bitter Melon Leaf for Anti-Inflammatory Activity against Cutibacterium acnes.

Cutibacterium acnes (formerly Propionibacterium acnes) is a key pathogen involved in the development and progression of acne inflammation. The numerous bioactive properties of wild bitter melon (WBM) leaf extract and their medicinal applications have been recognized for many years. In this study, we examined the suppressive effect of a methanolic extract (ME) of WBM leaf and fractionated components thereof on live C. acnes-induced in vitro and in vivo inflammation. Following methanol extraction of WBM leaves, we confirmed anti-inflammatory properties of ME in C. acnes-treated human THP-1 monocyte and mouse ear edema models. Using a bioassay-monitored isolation approach and a combination of liquid–liquid extraction and column chromatography, the ME was then separated into n-hexane, ethyl acetate, n-butanol and water-soluble fractions. The hexane fraction exerted the most potent anti-inflammatory effect, suppressing C. acnes-induced interleukin-8 (IL-8) production by 36%. The ethanol-soluble fraction (ESF), which was separated from the n-hexane fraction, significantly inhibited C. acnes-induced activation of mitogen-activated protein kinase (MAPK)-mediated cellular IL-8 production. Similarly, the ESF protected against C. acnes-stimulated mouse ear swelling, as measured by ear thickness (20%) and biopsy weight (23%). Twenty-four compounds in the ESF were identified using gas chromatograph–mass spectrum (GC/MS) analysis. Using co-cultures of C. acnes and THP-1 cells, β-ionone, a compound of the ESF, reduced the production of IL-1β and IL-8 up to 40% and 18%, respectively. β-ionone also reduced epidermal microabscess, neutrophilic infiltration and IL-1β expression in mouse ear. We also found evidence of the presence of anti-inflammatory substances in an unfractionated phenolic extract of WBM leaf, and demonstrated that the ESF is a potential anti-inflammatory agent for modulating in vitro and in vivo C. acnes-induced inflammatory responses.

Antioxidant Enhancing Effect of Azadirachta indica A. Juss. Leaf Fractionated Extracts on Naja nigricollis Reinhardt Venom in Albino Rats

The lethality of snake venom is mainly attributed to its phospholipase A2 component that hydrolyzes cellular phospholipids, leading to the release of arachidonic acid that generates potentially toxic reactive oxygen species (ROS). Imbalance between excessive generation and poor removal of ROS causes lipid peroxidation leading to cellular damage. Hence, this research was aimed at evaluating the antioxidant-enhancing effect of Azadirachta indica leaf fractionated extracts on Naja nigricollis venom in albino rats. A. indica leaf was collected, authenticated and extracted using 95% methanol followed by fractionation using hexane and ethyl acetate. Ferric reducing antioxidant power assay was used for the in vitro test, while, in vivo experiments were conducted using Albino rats. The in vitro antioxidant effect of the hexane and ethyl acetate fractions presented ferric reducing power of 68.80 ± 1.40% and 71.54 ± 2.12% respectively. This are closely related to those of ascorbic acid (78.50 ± 2.80%) and α-tocopherol (75.00 ± 1.85%). The results of the in vivo tests indicated that a single injection (0.195 mg/kg b. wt.) of N. nigricollis venom caused significant (P<0.05) elevation of hepatic and renal ROS levels (7 and 8 folds respectively) with a concomitant increase in lipid peroxidation (LPO) compared to the control group. The ROS levels were decreased significantly leading to the decrease in the level of LPO in the envenomed rats treated with the hexane and ethyl acetate fractions compared to the venom control. The treatments significantly (P<0.05) increased the activities of superoxide dismutase (SOD), glutathione peroxidase (GPx) and catalase (CAT) in both the hepatic and renal homogenates compared to the venom control. The degree of protection against LPO by reducing the levels of ROS as well as increasing the activities of the antioxidant enzymes has significantly (P<0.05) increased when combine treatment of standard antivenin and any of the hexane or ethyl acetate fractions was considered compared to when each of them was used alone. Based on these findings, it has been established that, the tested extracts have antioxidant as well as antioxidant-enhancing effects against the oxidative toxicity of N. nigricollis venom.

In vitro and in silico anticancer evaluation of a medicinal mushroom, Ganoderma neo-japonicum Imazeki, against human colonic carcinoma cells.

Ganoderma neo-japonicum is a well-known medicinal mushroom in Asian countries. However, scientific validations on its curative activities are confined to cirrhosis and diabetes. In this study, the anticancer properties of G. neo-japonicum were evaluated using cellular and computational models. The ethanolic extract (EtOH) with a promising inhibitory effect was fractionated into four different fractions: hexane (Hex), chloroform (Chl), butanol (Btn), and aqueous (Aq). The active fractions were then subjected to cell apoptosis assessment and phytochemical profiling. Molecular docking was conducted to elucidate the affinity of selected constituents towards antiapoptotic Bcl-2 protein. The butanol fraction showed the highest antioxidant activities as well as total phenolic content. Both hexane and chloroform fractions exerted a potent cytotoxic effect on colonic carcinoma cells through the induction of apoptosis. Phytochemical analysis revealed that the chloroform fraction is terpenoid enriched whereas the hexane fraction comprises predominantly sterol constituents. Stellasterol and 1,25-dihydroxyvitamin D3 3-glycoside were demonstrated to have a high affinity towards Bcl-2 protein. Overall, G. neo-japonicum can be considered as a compelling therapeutic candidate for cancer treatment.

Atividade antileishmania de Annona glabra L. (Annonaceae)

Objetivo: Descrever a atividade antileishmania de Annona glabra. Métodos: Foi realizado um estudofitoquímico do extrato etanólico (EE) obtido de cascas de A. glabra e suas frações, a partir do qual a Rutinafoi isolada. A atividade antileishmania frente a Leishmania amazonensis foi avaliada através dos ensaiosantipromastigota (método do MTT) e antiamastigota (determinada pela redução da taxa de infecção emmacrófagos). A citotoxicidade foi avaliada em macrófagos (THP-1) através do MTT. Resultados: Nosestudos fitoquímicos, o EE e suas frações apresentaram cromatogramas sugestivos de flavonoides. Noensaio antipromastigota, o EE, frações e Rutina, foram considerados inativos (CI50>200 µg/mL). Naatividade antiamastigota, o EE e a Rutina não inibiram a infecção de macrófagos por Leishmania, contudo, aFração de Hexano nas concentrações de 250 e 125 µg/mL inibiu a infecção de macrófagos em 39,1% e18,7% respectivamente. No ensaio de viabilidade, nenhuma amostra apresentou citotoxicidade (CC50 > 500µg/mL). Conclusão: Em síntese, o fracionamento do extrato etanólico favoreceu o aumento da atividadeantileishmania, inferindo que as substâncias responsáveis pela ação provavelmente estejam em baixaconcentração no extrato e suas frações e que, essa atividade, pode estar associada à presença deflavonoides.

Avocado kernels, an industrial residue: a source of compounds with insecticidal activity against silverleaf whitefly.

Fruit processing waste, such as kernels (endocarp + seed) of avocado [Persea americana Mill. (Lauraceae)], could be used as raw material in the preparation of botanical insecticides. In light of this potential, this study assessed the insecticidal action of extracts and fractions from kernels of two avocado cultivars (Breda and Margarida) on Bemisia tabaci (Gennadius) (Hemiptera: Aleyrodidae) biotype B, an important pest species in tropical conditions. Ethanolic and aqueous extracts prepared from kernels of P. americana, regardless of the plant cultivar used, caused promising insecticidal activity to whitefly nymphs. Based on yield in crude extracts [10.32 and 9.85% (w/w), respectively, for cultivars Breda and Margarida], on the bioassay results with crude extracts and on the chemical profiles, the ethanolic extract of kernels of P. americana cv. Breda was chose for the continuation of the study. Thus, the ethanolic extract of kernels of cv. Breda (LC50 = 197.84ppm and LC90 = 567.19ppm) was selected and subjected to fractionation by the liquid-liquid partition technique. The hexane and dichloromethane fractions of this extract caused significant mortality of nymphs. The analysis using the ultraviolet (UV) and hydrogen nuclear magnetic resonance (1H NMR) showed the presence of long-chain aliphatic compounds (alkanols or acetogenins of Lauraceae), alkylfurans (or avocadofurans), and unsaturated fatty acids in these fractions, which are possibly related to bioactivity observed in B. tabaci, besides saccharides. The results show that kernels of P. americana are promising sources of compounds with insecticidal action for the control of B. tabaci biotype B, a great opportunity to transform environmental problems into eco-friendly solutions to agriculture.

Verbesina crocata: A pharmacognostic study for the treatment of wound healing.

Ethnopharmacological relevanceVerbesina crocata (Cav.) Less. (Arnica or Capitaneja) is an endemic plant from Mexico restricted to the western part of the country. The aerial parts are used in traditional medicine for the treatment of wounds and burns. The objective of this investigation was to carry out a pharmacognostic study of V. crocata and establish markers that allow for the recognition of the characteristics of the plant and validate its traditional use. The study includes anatomical and chemical characteristics of the plant as well as evaluations of its antioxidant capacity and wound healing ability in a murine model.Materials and methodsAn anatomical study of V. crocata was performed on the middle part of the leaf and stem. A methanolic extract of this species (VcME) was obtained by methanolic maceration of the aerial parts. Subsequently, a partition of the VcME was made to obtain a hexanic fraction (VcH). The phytochemical preliminary screening and characterization by high-performance liquid chromatography/mass spectrometry (HPLC-ESI/MS) of the VcME and VcH were performed. The antioxidant activity and total phenolic content were quantified. The wound healing capacity of the methanolic extract was determined in CD-1 mice by the healing rate, the tensiometric method, and histological analysis.ResultsThe anatomical study of V. crocata showed the presence of two types of secretory structures and their position on the leaves. In addition, the characteristics of the middle vein and trichomes are potentially useful for recognition of the species. Chemical compounds detected by HPLC-ESI/MS reveal the presence of sitosterol glycoside and catechin derivatives as principal constituents of V. crocata. The VcME showed low antioxidant capacity and total phenolic. V. crocata had a similar healing effect to Recoveron® in the tensiometric method, but the rate of healing was higher. According to the histological analysis, the treatment of V. crocata promoted the remodelling phase 15 days after the incisional wound.ConclusionThis is the first pharmacognostic study of this species that covers the plant anatomy, chemical content and biological properties related to its traditional use. V. crocata favours wound healing according to physical and histological evaluations. In addition, the characteristics of the middle vein, trichomes and catechin glycosides are potentially useful for the recognition of this species.

Free radicals and enzymes inhibitory potentials of the traditional medicinal plant Echium angustifolium

IntroductionHerbal medicine has been useful in the treatment of various diseases and has played a critical role in the discovery of new drugs. This study aimed to investigate the phytoconstituents, antioxidant, antidiabetic and antiobesity activities of the traditional medicinal plant, Echium angustifolium Mill. MethodsThe constituents of E.angustifolium four solvents fractions were established utilizing conventional analytical methods. Antioxidant, antilipase, anti-glucosidase, and anti-α-amylase activities of E. angustifolium were conducted using DPPH (1,1-diphenyl-2-picrylhydrazyl α), p-nitrophenyl butyrate, P-NPG (4-nitrophenyl β-d-glucopyranoside), and dinitrosalicylic acid procedures, respectively. ResultsThe methanolic fraction of E. angustifolium displayed inherent antioxidant properties with an IC50 value of 1.95 μg/mL. Moreover, the hexane fraction presented potential α-amylase inhibitory activity with an IC50 value of 92.89 μg/mL. Additionally, the aqueous fraction had the highest anti-lipase activity with an IC50 value of 24.54 μg/mL. ConclusionIt can be concluded that E. angustifolium has high potential for development as an alternative approach for oxidative stress, diabetes, and obesity.

English

Newcastle disease remains a disease of global concern and serious economic challenge to the poultry industry because of its high mortality rate, in spite of the various intervention programs including vaccination. This research is aimed at studying the antiviral activity of the extract and fractions of Boswellia dalzielii against Newcastle disease virus (NDV) using chicken embryonated eggs. Phytochemical analysis was conducted using standard procedure. The methanol extract of Boswellia dalzielii was subjected to solvent- solvent fractionation using solvents of varing polarity. This process generated four fractions namely hexane fraction, ethyl acetate fraction, n-butanol fraction and aqueous fraction. Nine to eleven day-old viable embryonated chicken eggs (ECE) were used for the antiviral assay; these were divided into seven groups of five eggs each. The methanol extract was also screened for its cytotoxicity, prophylatic, therapeutic and neutralization effects against NDV, while the fractions were screened for their cytotoxicity and neutralization effects. The phytochemical screening of the stem bark extract and fractions of B. dalzielii showed the presence of tannins, flavonoids, saponin, terpenoids and steroids. It was observed from the results that the extract was toxic to the embryo at a concentration above 100 mg/ml. At the end of the bioassay, methanol extract and fractions of B. dalzielii showed antiviral activity against NDV. However, the extract seems to possess the most significant anti-NDV activity than the fractions. The results of the study are very promising and support the use of B. dalzielii in the treatment of viral infections in animals and humans. Key words: Antiviral, Boswellia dalzielii, Newcastle disease virus (NDV), embryonated chicken eggs (ECE).

Lethality of Naja nigricollis Reinhardt venom and antivenom activity of Azadirachta indica A. Juss. leaf extracts on albino rats

Snakebite remains an important cause of morbidity and mortality in Nigeria. Conventionally, the means of treatment is parenteral administration of serum-based antivenins. But due to the limitations of these antivenins, snakebite victims in many Nigerian communities are mostly treated with herbal antidotes. Hence, this research was designed to evaluate the lethality of Naja nigricollis Reinhardt venom and screen the antivenom activity of Azadirachta indica A. Juss. leaf extracts with a view to replacing the serum-based antivenin. The methanol extract of A. indica leaf was screened against venom-induced lethal effect in albino rats using standard methods. The crude methanol extract was subjected to solvent-fractionation, and the fractions were also screened against the venom-induced lethal effect in albino rats. The lethal doses, 50% (LD50) and 100% (LD100) of the venom were 0.389 and 3.891 mg/kg b. wt. respectively. The crude extract and its fractions exhibited antivenom activities with varying degrees of efficacy. The crude methanol extract and its hexane and ethyl acetate fractions presented animal mean survival time of 22.51 ± 2.38 h, 23.68 ± 0.89 h and 21.98 ± 1.36 h respectively against LD100 of the venom. These are significantly different when compared with the mean survival time of the venom control groups. Hence, these findings suggest that A. indica leaf has potent antivenom activity and this can serve as leads for the development of safe, readily available and affordable antivenoms.

Preclinical studies indicate that INFLATIV, an herbal medicine cream containing Pereskia aculeata, presents potential to be marketed as a topical anti-inflammatory agent and as adjuvant in psoriasis therapy

A previous study reported that the hexane fraction (HF) obtained from Pereskia aculeata leaves showed promising topical anti-inflammatory activity. Intending its future use in clinical practice, a herbal medicine cream named INFLATIV was developed. Its anti-inflammatory and antipsoriatic potential were investigated. INFLATIV was subjected to preliminary accelerated stability tests and to a degradation profile assessment. INFLATIV was prepared at 6% and 12%. The anti-inflammatory activity was assessed by croton oil single and multiple application challenge in mice. Mouse tail test was used for antipsoriatic potential investigation. Cutaneous atrophy test was performed. Preliminary accelerated stability tests were performed together with a degradation profile by GC-MS analysis. The anti-inflammatory activity shown by INFLATIV was comparable to dexamethasone. However, the skin atrophy caused by that drug was not observed. INFLATIV modified skin parakeratotic differentiation into orthokeratosis, which revealed its antipsoriatic potential. The ingredients used were suitable to carry the bioactives as they were well permeated by the skin. The preliminary accelerated stability tests indicated that INFLATIV 6% is more stable than 12%. The results demonstrated the relevant therapeutic and marketing potentials of INFLATIV, which is likely to be further evaluated in clinical trials for drug registration process with regulatory agencies.

Larvicide potential of genus Croton L. (Euphorbiaceae) in biological control of Aedes aegypti L. (Diptera: Culicidae)

The reemerging diseases caused by Aedes aegypti are one of the main public health problems in the world. The control of mosquitoes using larvicidal compounds from products of plant origin is an excellent alternative. This study aims to evaluate the larvicidal potential of fractions in hexane, chloroform, ethyl acetate and hydromethanol from the ethanolic leaf extract of two species of the genus Croton L. (Euphorbiaceae) against larval forms of A. aegypti, as an alternative tool to control this vector. Dry leaves of Croton betaceus Baill. and Croton lundianus (Didr.) Müll. Arg. were used for biological tests. The compounds were extracted with ethanol (99.8%). The ethanolic extracts of the leaves were suspended in a methanol / water solution and were successively subjected to the liquid-liquid division process with solvents of different polarities: hexane, chloroform and ethyl acetate, giving rise to the four fractions. Larvicidal tests were performed with the ethanol extract and fractions resulting from the partition. In the study, the crude extract and the fractions showed larvicidal potential, being hexane fraction the one with greatest activity. Mortality in C. betaceus fractions was up to 40%. Croton lundianus presented mortality of up to 93.33% of the larvae submitted to the test. Data analysis showed larvicidal activity in the crude extract and fractions. The hexane fraction was more effective, especially in C. lundianus.

Chemical profile and gastroprotective effect of Jatropha elliptica (Pohl) Oken roots

Jatropha elliptica (Pohl) Oken (Euphorbiaceae) roots are used in folk medicine to treat gastric ulcers. The purpose of this work was to evaluate the gastroprotective activity of ethanol extract (JER) and hexane fraction (ERH) of J. elliptica roots in mice, as well as to analyze the acute toxicity of the extract and identify the potential active compounds. No signs of toxicity were observed in JER. In both acidified ethanol and indometacin-induced gastric ulcer models, all doses tested of JER and ERH significantly reduced gastric lesions. Dereplication of JER was performed by HPLC-DAD-ESI-MS/MS and resulted in the annotation of compounds fraxetin, propacin, jatrophone and jatropholones A and B. GC–MS analysis of ERH revealed the diterpenes jatrophone, jatropholone A and jatropholone B as the major components. The chemical study of this fraction has led to the isolation of these compounds, in addition to the sequiterpene cyperenoic acid and the diterpene 2β-hydroxyjatrophone, both reported for the first time in J. elliptica. The isolated compounds were tested against L929 cells and only cyperenoic acid and the mixture of jatropholones A and B did not show toxicity, being then selected as good candidates for bioassays using acidified ethanol-induced gastric ulcer model. Cyperenoic acid significantly decreased gastric lesions and preserved gastric mucus layer. The mixture of jatropholones A and B caused a smaller reduction of gastric lesions, without preservation of the gastric mucus layer. The study showed that J. elliptica roots present gastroprotective activity in mice, without causing acute toxic effects. The activity is related, at least in part, to the occurrence of terpenes, mainly the sesquiterpene cyperenoic acid.

Metabolome modulatory effects of Kigelia africana (Lam.) Benth. fruit extracts on oxidative stress, hyperlipidaemic biomarkers in STZ-induced diabetic rats and antidiabetic effects in 3T3 L1 adipocytes.

The management of diabetes is considered a global problem, and a cure is yet to be discovered. This study investigated the modulatory effect of Kigelia africana fruit on oxidative stress and hyperlipidaemic biomarkers in STZ-induced diabetic rats, profiled phytoconstituents using GC-TOF-MS and evaluated antidiabetic effects on 3T3 L1 adipocytes. Thirty male Wistar rats (120-150g) were divided into six groups (n=5). Diabetes was induced by a single intraperitoneal injection of STZ (60mg/kg) and treated with 100, 200 and 400 of hexane fraction of KA for 28days. Immunohistochemical evaluation was carried out using avidin-biotin immunoperoxidase (ABI) method. Catalase and SOD activities as well as the levels of total protein, albumin, bilirubin, triglyceride, cholesterol, and high-density lipoprotein were measured. The expressions of oxidative stress and hyperlipidaemic biomarkers alongside fasting blood glucose concentrations were remarkedly decreased in KA-treated diabetic rats. Moreover, there was a significant increase in endocrine cell distribution, area covered with increase in β-cell mass, composition and morphology of KA-treated animals. Additionally, there was constant up-regulation in 3T3 L1 adipocytes due to the presence of phytoconstituents. Kigelia africana fruit can act as a modulatory agent due to its ameliorative effects against oxidative stress.