Crude Compounds Research Articles

Development of recombinant major capsid protein Vaccine and assessment of its efficacy against SRDV in similar damselfish (Pomacentrus similis)

Viral vaccines against emerging viral diseases are crucial for encouraging successful aquaculture production. In this research, an experimental recombinant major capsid protein vaccine of similar damselfish virus was prepared and examined for its efficacy in marine ornamental fish, similar damselfish (Pomacentrus similis). The MCP gene of the SRDV was amplified from the viral DNA by a specific primer set viz bamHI and XhoI- restriction sites and confirmed by agarose gel electrophoresis with a target size of 1416 bp. The gel-purified PCR product was double-digested with the said enzymes and incorporated into the pTriEx1.1 vector, which was subsequently transformed to E. coli DH5α. The plasmids of the two clones pTriEx-MCP-1416-1 and pTriEx-MCP-1416-3 were transformed to E. coli BL21 (DE-3) pLacI. A crude protein compound derived from a colony of E. coli BL21 (DE-3) with expressed MCP inserts was used to evaluate efficacy in similar damselfish by intra-peritoneal injection. After the challenge with SRDV, damselfish vaccinated with recombinant protein showed a lower protection level, while the fish vaccinated with recombinant protein supplemented Quil-A® adjuvant showed an RPS of 26%. According to RPS values recorded from the vaccinated and non-vaccinated damselfish group, the recombinant protein vaccine conferred only marginal protection against the SRDV challenge.

Growth and nutritional potential of selected grasses and legumes for ruminants’ production

The production of legumes and grasses are a sustainable strategy to feed ruminants. These species are rich in nutrients which can improve animal health with less treatment. Therefore, the objective of this work was to assess the performance of the middle and edge plants of five legumes and two grasses for morphological traits, fresh and dry matter yields and nutritional potential as feed for ruminants. The collected data were subjected to statistical analysis using R software. The results indicated that very highly significant differences (P<0.001) were observed among the nutritional values, morphological and biomass yield traits except for stem diameter. There was also significant difference(P<0.001) between the edge plants and middle plants. The mean values of the number of leaves and number of stem were higher in the edge plants than in the middle plants for all the seven species. Carbohydrate was the most abundant (42.40), followed by protein (17.81), crude fiber (15.79) and crude fat (7.32). The element analyses of leaf showed N, K, Ca and Mg are suitable for ruminant production in all species. A strong positive correlation was observed among the protein, crude fat and crude fiber compounds. Edge effects were observed showing the highest values when compared to the middle plants. Centrosema pubescens out performed in terms of overall protein, crude fat and crude fiber, while Mucuna pruriens recorded the highest mean value of dry biomass yield. The production of both grasses and legumes, because of their diverse proximate and mineral compositions, constitutes one of the mainstay for sustainable and competitive animal production systems. We recommend ruminant farmers to plant the grasses and legumes at the edges of their farms for sustainable fodder production.

Effects of crude alkaloid compounds extract of Ammi majus leaves and flowers on some aspects of biological performance Oryzaephilus surinamensis (Coleoptera: Silvanidae)

This in vitro study evaluated the effects of crude alkaloid compounds extract of plant A. majus leaves and flowers on some biological performance aspects of the insect. The results showed that the alkaloid extract of flowers at concentrations of 10, 20 and 30 mg/ml significantly affected cumulative mortality at the different stages. The concentration ( 30) mg/ml had the most noticeable effects, causing the highest mortality rate in the second and fourth larval instars (86.7 and 73. 3 %, respectively) after 72 hours. At the same time, the mortality rates upon applying the same concentrations but of the alkaloid extract of the leaves were 73.3, and 53.3 %, respectively, following 72 hours of treatment. Keywords: Oryzaephilus surinamensis; Ammi majus; crude alkaloid compounds extract.

The deasphalting of heavy crude oil by silicone oil is a green method of removing heavy compounds and producing bitumen

Deasphalting of heavy crude oil (HCO) with silicone oil (SO), which is immiscible with the crude oil and extracts light compounds from it, has been carried out for the first time. The yield of the extracted light fraction increases linearly with increasing SO/HCO ratio from 0.5/1 to 10/1 and then reaches a constant level of about 50%. An analysis of the composition and properties of the precipitated heavy fractions showed that they are enriched with asphaltenes and resins but contain admixtures of saturated and aromatic compounds. Compared with the original crude oil, the heavy fractions have a higher viscosity that correlates with sulfur concentration and tends to become higher as the SO/HCO ratio increases. Moreover, the viscoelastic properties of the heavy fractions are similar to those of bitumen binders, allowing their potential use in road construction. In this case, SO/HCO ratios of 15/1 and 25/1 make it possible to produce bitumens as a byproduct that meet existing standards for binder's viscosity and thermal stability. A comparative evaluation of energy consumption has shown the advantage of silicone oil usage for deasphalting of heavy oil in comparison to usual solvent deasphalting with volatile and environmentally unfriendly aliphatic hydrocarbons.

Antibacterial, antifungal, antifeedent and larval mortality percent of solvent extraction of mango kernel (Mangifera indica L.) cv. Totapuri

Mango (Mangifera indica L.) is a seasonal fruit and is cultivated extensively in tropical and subtropical region in India and worldwide. The fruit is processed and mango pulp is extracted in fruit processing industries and kernel is unutilized as industrial waste. Hence, in the present study focused on Totapuri mango kernel cultivar was taken to utilize for bio product development. Soxhlet apparatus with different solvents was used for the crude bioactive compounds extraction from mango kernel powder. The extracted bioactive mass was evaluated for its antibacterial activity against bacterial strains such as Escherichia coli, Pseudomonas putida, Pseudomonas aeruginosa, Shigella sonnei, Klebsiella pneumonia, Xanthomonas oryzae and Staphylococcus aureuss. Further, the extracted crude bioactive compound was tested for antifungal activity against Rhizactonia solani, Curvularia lunata, Alternaria alternate and Fusarium oxysporum. The antifeedent and larval mortality of Spodoptera litura and Helicoverpa armigera activity was studied using the bioactive compound extract. The Methanol Mango Kernel extract (MeOH MK) recorded growth inhibition zone for all the bacteria tested ranging from 21±0.31 to 24±1.55 mm. At 5 % MeOH MK crude extract concentration, the fungal mycelia growth of R. solani was inhibited by 92.90 ± 0.31 %. The highest percent of antifeedent activity was observed in 5% MeOH MK extract recorded as 77.37 %± 0.75 for S.litura and 55. 1.06 for H.armigera. The crude extract of MeOH MK at 5 % concentration recorded 17.8 %± 2.2 mortality rate for S. leutira larva and 100 % mortality rate for H. armigra. The MeOH MK extract was effective as antibacterial, antifungal, antifeedent and larval mortality.

Comparative Study of&amp;lt;i&amp;gt; Mbuja &amp;lt;/i&amp;gt;and&amp;lt;i&amp;gt; daddawa &amp;lt;/i&amp;gt;Oils in View of Their Use in the Treatment of Some Chronic Diseases

<i>Mbuja</i> and <i>daddawa</i> are food condiments obtained by traditional uncontrolled fermentation of <i>Hibiscus sabdariffa </i>and<i> Parkia biglobosa </i>seeds respectively in African countries (Burkina Faso, Mali, Niger, Nigeria, Cameroon and Sudan etc...). These condiments are known for their nutritive values and for their health properties in traditional medicine to cure some chronic diseases. In spite of their nutritional and healthy properties the consumption of <i>Mbuja </i>and<i> daddawa </i>are less appreciated in urban areas. This is due to their strong smell, to their bad condition of manufacturing practices which leads to the rapid alteration of nutraceutic values. The main problem now is how to lead people to consume these condiments which nevertheless contains bioactive molecules, and can help in the treatment or in the prevention of some cardiovascular diseases. Among those bioactive molecules, the lipidic is one of the main element which has an impact on some chronic diseases. The fact that <i>daddawa</i> and <i>mbuja</i> are used for the same treatment, means that oils of both condiments could have same contents. For this reason the goal of this study target the comparative analyses of bioactive compounds of <i>daddawa</i> and <i>mbuja</i> oils that can justify the used of both condiments in the treatment of chronic diseases. To overcome this, the physicochemical composition of different oils were assessed by using classical methods. The results obtained show similitude values in colour, acid index, iodine value, saponification value, crude phenolic compounds, tannin as well as SFA, MUFA, PUFA. Based on these results, the physicochemical composition of <i>daddawa</i> and <i>mbuja</i> seem to be identic and can be applied for the same treatment.

Extracts of Jamun seeds inhibited the growth of human (Hep-2) cancer cells.

In the last century, the human laryngeal epithelioma has become a life-threatening disease leading to a high rate of mortality worldwide. The current investigation is focusing on the antiproliferative effect of Eugenia jambolana seed extracts against Hep-2 cancer cells. The active compounds from the seeds of E. jambolana were extracted by the decoction extraction method using acetone, ethanol, and methanol. The filtrates from the different solvents were subjected to liquid-liquid separation before drying by a rotary evaporator. In various doses, the crude extracts and carcinoma were subjected to a methylthiazolyl diphenyl tetrazolium bromide assay. Cell viability was determined under ultraviolet visualization at an absorbance of 540 nm. The data of the viable cells were subjected to analysis of variance at P ≤ .01. Crude compounds of E. jambolana seeds extracted by acetone, methanol, and methanol extract had an anticarcinoma effect. Among the extracts, methanol extract possessed a recommendable anti-carcinoma effect compared to acetone and ethanol crude extracts. At a concentration of 125 µg/mL, the crude extracts of methanol, acetone, and ethanol destroyed 49.57, 35.01, and 27.67 carcinomas, respectively. The concentration of 31.25 µg/mL of acetone extract and 125 µg/mL of ethanolic extract affected 28.11 and 27.67 carcinomas, respectively. E.jambolana seeds possess anticarcinoma potency and thus can be administered in the reduction of proliferative carcinoma. The study recommended further studies which will involve the elution of pure compounds from the methanol extract of E. jambolana that possess antitumour and antiproliferative activity against Hep-2 cell lines.

Hippophae rhamnoides L.: A Comprehensive Review on the Botany, Traditional Uses, Phytonutrients, Health Benefits, Quality Markers, and Applications

Hippophae rhamnoides L. (sea buckthorn), consumed as a food and health supplement worldwide, has rich nutritional and medicinal properties. Different parts of H. rhamnoides L. were used in traditional Chinese medicines for relieving cough, aiding digestion, invigorating blood circulation, and alleviating pain since ancient times. Phytochemical studies revealed a wide variety of phytonutrients, including nutritional components (proteins, minerals, vitamins, etc.) and functional components like flavonoids (1-99), lignans (100-143), volatile oils (144-207), tannins (208-230), terpenoids (231-260), steroids (261-270), organic acids (271-297), and alkaloids (298-305). The pharmacological studies revealed that some crude extracts or compounds of H. rhamnoides L. demonstrated various health benefits, such as anti-inflammatory, antioxidant, hepatoprotective, anticardiovascular disease, anticancer, hypoglycemic, hypolipidemic, neuroprotective, antibacterial activities, and their effective doses and experimental models were summarized and analyzed in this paper. The quality markers (Q-markers) of H. rhamnoides L. were predicted and analyzed based on protobotanical phylogeny, traditional medicinal properties, expanded efficacy, pharmacokinetics and metabolism, and component testability. The applications of H. rhamnoides L. in juice, wine, oil, ferment, and yogurt were also summarized and future prospects were examined in this review. However, the mechanism and structure-activity relationship of some active compounds are not clear, and quality control and potential toxicity are worth further study in the future.

Cytotoxicity of the methanol extracts and compounds of Brucea antidysenterica (Simaroubaceae) towards multifactorial drug-resistant human cancer cell lines

BackgroundCancer remains a global health concern and constitutes an important barrier to increasing life expectancy. Malignant cells rapidly develop drug resistance leading to many clinical therapeutic failures. The importance of medicinal plants as an alternative to classical drug discovery to fight cancer is well known. Brucea antidysenterica is an African medicinal plant traditionally used to treat cancer, dysentery, malaria, diarrhea, stomach aches, helminthic infections, fever, and asthma. The present work was designed to identify the cytotoxic constituents of Brucea antidysenterica on a broad range of cancer cell lines and to demonstrate the mode of induction of apoptosis of the most active samples.MethodsSeven phytochemicals were isolated from the leaves (BAL) and stem (BAS) extract of Brucea antidysenterica by column chromatography and structurally elucidated using spectroscopic techniques. The antiproliferative effects of the crude extracts and compounds against 9 human cancer cell lines were evaluated by the resazurin reduction assay (RRA). The activity in cell lines was assessed by the Caspase-Glo assay. The cell cycle distribution, apoptosis via propidium iodide (PI) staining, mitochondrial membrane potential (MMP) through 5,5′,6,6′-tetrachloro-1,1′,3,3′-tetraethylbenzimidazolylcarbocyanine iodide (JC-1) staining, and the reactive oxygen species (ROS) via 2´,7´-dichlorodihydrofluoresceine diacetate (H2DCFH-DA) staining, were investigated by flow cytometry.ResultsPhytochemical studies of the botanicals (BAL and BAS) led to the isolation of seven compounds. BAL and its constituents 3, (3-(3-Methyl-1-oxo-2-butenyl))1H indole (1) and hydnocarpin (2), as well as the reference compound, doxorubicin, had antiproliferative activity against 9 cancer cell lines. The IC50 values varied from 17.42 µg/mL (against CCRF-CEM leukemia cells) to 38.70 µg/mL (against HCT116 p53−/− colon adenocarcinoma cells) for BAL, from 19.11 µM (against CCRF-CEM cells) to 47.50 µM (against MDA-MB-231-BCRP adenocarcinoma cells) for compound 1, and from 4.07 µM (against MDA-MB-231-pcDNA cells) to 11.44 µM (against HCT116 p53+/+ cells) for compound 2. Interestingly, hypersensitivity of resistant cancer cells to compound 2 was also observed. BAL and hydnocarpin induced apoptosis in CCRF-CEM cells mediated by caspase activation, the alteration of MMP, and increased ROS levels.ConclusionBAL and its constituents, mostly compound 2, are potential antiproliferative products from Brucea antidysenterica. Other studies will be necessary in the perspective of the discovery of new antiproliferative agents to fight against resistance to anticancer drugs.

Effect of deposit chemistry on microbial community structure and activity: Implications for under-deposit microbial corrosion.

The deposition of solid particles carried by production fluids from oil and gas companies in horizontal surfaces of different assets has shown to cause severe localised corrosion. Sand, one of the most common deposits in the energy sector pipelines, is frequently mixed with crude, oil, asphaltenes, corrosion inhibitors, and other organic compounds. For this reason, they might favour the metabolic activity of native microbial communities. This study aimed to determine the impact of sand-deposit chemical composition on the microbial community structure and functional attributes of a multispecies consortium recovered from an oilfield and the resulting risk of under-deposit microbial corrosion of carbon steel. Sand deposits recovered from an oil pipeline were used in their raw form and compared against the same deposits exposed to heat treatment to remove organic compounds. A four-week immersion test in a bioreactor filled with synthetic produced water and a two-centimeter layer of sand was set up to assess corrosion and microbial community changes. The raw untreated deposit from the field containing hydrocarbons and treatment chemicals resulted in a more diverse microbial community than its treated counterpart. Moreover, biofilms developed in the raw sand deposit exhibited higher metabolic rates, with functional profile analysis indicating a predominance of genes associated with xenobiotics degradation. Uniform and localized corrosion were more severe in the raw sand deposit compared to the treated sand. The complex chemical composition of the untreated sand might have represented an additional source of energy and nutrients to the microbial consortium, favoring the development of different microbial genera and species. The higher corrosion rate obtained under the untreated sand suggests that MIC occurred due to syntrophic relationships between sulphate reducers or thiosulphate reducers and fermenters identified in the consortium.

The Effect of the Crude Terpenoids Compounds of Melia Azedrach Leaves and Fruits on Some Biological Aspects of Whitefly Bemisia tabaci

This study was carried out to determine the effects of crude terpenoid compound extracts of Melia azedarach L. leaves and fruits on some biological aspects of whitefly Bemisia tabaci (Genn.) under laboratory conditions of 25 ± 2°C and relative humidity of 65-70%. The results indicated a significant effect on eggs and immature stages when treated with 0.5, 1, 1.5, and 2 mg/ml of leaves and fruits. The mortality rate increased with concentration. It reached 98.68, 100, 100, 95.70, 86.30, and 42.68% for eggs, 1st, 2nd, and 3rd nymphal instars, pupa, and adults, respectively, at a concentration of 2 mg/ml for leaves extract. At the same time, it reached 94.86, 100,100, 100, 87.89, and 44.90% for eggs, 1st, 2nd, and 3rd nymphal instars, pupa, and adults, respectively, at a concentration of 2 mg/ml for fruit extract. Also, the proportion of adults who emerged from sprayed eggs reduced to 91.53% and 95.72% when treated with 2 mg/ml of leaves and fruit extracts, respectively. While the developmental period increased to 23.50 and 24.00 days at 2 mg/ml when treated with terpenoid extracts of the leaves and fruits, respectively, compared with 21.00 and 20.83 days at control.

Antioxidant Potential of Ethiopian Medicinal Plants and Their Phytochemicals: A Review of Pharmacological Evaluation.

Free radicals are very reactive molecules produced during oxidation events that in turn initiate a chain reaction resulting in cellular damage. Many degenerative diseases in humans, including cancer and central nervous system damage, are caused by free radicals. Scientific evidence indicates that active compounds from natural products can protect cells from free radical damage. As a result, the aim of this review is to provide evidence of the use of diverse Ethiopian medicinal plants with antioxidant properties that have been scientifically validated in order to draw attention and foster further investigations in this area. The keywords antioxidant, radical scavenging activities, reactive oxygen species, natural product, Ethiopian Medicinal plants, and 2, 2-Diphenyl-1-picrylhydrazyl radical scavenging assay (DPPH) were used to identify relevant data in the major electronic scientific databases, including Google Scholar, ScienceDirect, PubMed, Medline, and Science domain. All articles with descriptions that were accessed until November 2022 were included in the search strategy. A total of 54 plant species from 33 families were identified, along with 46 compounds isolated. More scientific studies have been conducted on plant species from the Brassicaceae (19%), Asphodelaceae (12%), and Asteraceae (12%) families. The most used solvent and extraction method for plant samples are methanol (68%) and maceration (88%). The most examined plant parts were the leaves (42%). Plant extracts (56%) as well as isolated compounds (61%) exhibited significant antioxidant potential. The most effective plant extracts from Ethiopian flora were Bersama abyssinica, Solanecio gigas, Echinops kebericho, Verbascum sinaiticum, Apium leptophyllum, and Crinum abyssinicum. The best oxidative phytochemicals were Rutin (7), Flavan-3-ol-7-O-glucoside (8), Myricitrin (13), Myricetin-3-O-arabinopyranoside (14), 7-O-Methylaloeresin A (15), 3-Hydroxyisoagatholactone (17), β-Sitosterol-3-O-β-D-glucoside (22), Microdontin A/B (24), and Caffeic acid (39). Many crude extracts and compounds exhibited significant antioxidant activity, making them excellent candidates for the development of novel drugs. However, there is a paucity of research into the mechanisms of action as well as clinical evidence supporting some of these isolated compounds. To fully authenticate and then commercialize, further investigation and systematic analysis of these antioxidant-rich species are required.

Family Araliaceae in Southern Africa: A Review of Ethnobotanical Uses, Phytochemistry, Pharmacology, and Toxicology

There is widespread use of species belonging to family Araliaceae in traditional medicine in southern Africa. The aim of this review was to assess medicinal uses, phytochemistry, pharmacology and toxicological properties of indigenous species belonging to family Araliaceae in southern Africa. Relevant articles, books, theses, dissertations, patents, and other English-only reports on the medicinal uses, phytochemistry, pharmacological and toxicological properties of species belonging to the family Araliaceae in southern Africa (Angola, Botswana, Eswatini, Lesotho, Malawi, Mozambique, Namibia, South Africa, Zambia and Zimbabwe) were reviewed. Databases such as PubMed, Web of Science, Elsevier, Google Scholar, Scopus, Springer, Science Direct, Taylor and Francis between January and July 2022. Eleven species, namely Cussonia. arborea, C. arenicola, C. natalensis, C. nicholsonii, C. paniculata, C. sphaerocephala, C. spicata, C. transvaalensis, C. thyrsiflora, C. zuluensis and Neocussonia umbellifera are used as traditional medicines against 48 human and animal diseases. This study showed that alkaloids, anthocyanins, anthracene glycosides, botulin, flavonoids, free gallic acid, iridoids, phenolics, saponins, steroids, tannins, triterpenoids and volatile oils have been identified from these species. Pharmacological research revealed that the crude extracts and compounds demonstrated isolated from these species are characterized by Aβ42 protein reduction, acetylcholinesterase, analgesic, antibacterial, antifungal, antiviral, anticancer, antihyperglycemic, anti-inflammatory, antileishmanial, antioxidant, antiplasmodial, antiprotozoal, anti-ulcer, immunomodulatory, larvicidal, molluscicidal, spermicidal, cytotoxicity and toxicity activities. Reports of medicinal uses, phytochemistry, pharmacology and toxicological properties of species belonging to the family Araliaceae in southern Africa could only be found for 11 species, suggesting that further investigation of largely unexplored family members is necessary.

Biosurfactant Production from the Biodegradation of n-Paraffins, Isoprenoids and Aromatic Hydrocarbons from Crude Petroleum by Yarrowia lipolytica IMUFRJ 50682

Yarrowia lipolytica is a unique, strictly aerobic yeast with the ability to degrade efficiently hydrophobic substrates. In the present work, we evaluated the degrading potential of Yarrowia lipolytica IMUFRJ 50682, isolated from tropical estuarine water in Rio de Janeiro (Brazil), and the possible biomolecules produced during this process. To investigate which crude oil compounds are degraded by Y. lipolytica IMUFRJ 50682, this microorganism was grown in a medium containing Marlim petroleum (19 °API, American Petroleum Institute gravity) at 28 °C and 160 rpm for 5 days. The residual petroleum was submitted to gas chromatograph-mass spectrometric analysis (GC-MS). The chromatographic fingerprints of the residual petroleum were compared with the abiotic control test incubated in the same conditions. Y. lipolytica assimilates high molecular weight hydrocarbons, such as n-alkanes (C11-C19), isoprenoids (pristane and phytane), aromatics with two or three aromatics rings (naphthalene, methylnaphthalenes, dimethylnaphthalenes, trimethylnaphthalenes, phenanthrene, methylphenanthrenes, dimethylphenanthrenes, anthracene). This strain was also capable of consuming more complex hydrocarbons, such as tricyclic terpanes. During this biodegradation, the emulsification index of the culture medium increased significantly, showing that biosurfactant molecules can be produced from this process. Therefore, Y. lipolytica IMUFRJ 50682 showed to be a potential crude oil degrading yeast, which can be used for bioremediation processes and simultaneously produce bioproducts of commercial interest.

Medicinal uses, chemical constituents and biological activities of Rumex abyssinicus: A Comprehensive review

Rumex abyssinicus is a valuable medicinal plant species that is native to tropical Africa. Traditionally, R. abyssinicus is used to treat different disease such as, liver diseases, hepatitis, malaria, scabies, blood pressure, jaundice, wound and pneumonia. The purpose of the current study was to review the literature on the ethnomedicinal uses, chemical constitutes and biological activities of R. abyssinicus in an attempt to create information for future studies aimed towards exploring the therapeutic ability of the species. A scientific search engines, namely Google Scholar, PubMed, Scopus, Science Direct and Web of knowledge for the search terms: Rumex abyssinicus, ethnomedicinal studies, phytochemical investigations, and pharmacological activities were undertaken. The search strategy included all articles with descriptors that were available until December 30, 2021. Only published works in English have been used on this study. The data was collected using textual descriptions of the studies, tabulation, grouping, and figures. The principal phytochemicals of R. abyssinicus are anthraquinones, flavonoids, terepenoids and phenolic compounds. The in vitro and in vivo studies on the crude extracts and compounds of R. abyssinicus showed antibacterial, antioxidant, anticancer, anti-inflammatory, antifungal, wound healing, antialzeimer’s and hepatoprotective activities of it. R. abyssinicus afforded drug leads such as helminthosporin (4) with anti-alzheimer and physicon (3) with antifungal and antioxidant activity. R. abyssinicus have traditionally been used to cure a variety of diseases. Pharmacological actions of phytochemicals were shown to be promising. Despite this, further studies on crude extracts and promising compounds are needed to find new drug candidates.

Synthesis and Studies of Fused Benzo-Benzisapphyrins.

A series of rare examples of fused benzo-benzisapphyrins were synthesized readily by (3 + 2) condensation of benzodipyrrole-derived diol and para-benzitripyrrane in the presence of 0.5 equiv of TFA in CH2Cl2 under inert atmosphere conditions accompanied by DDQ oxidation in open air. The crude compounds were separated by basic alumina column chromatography and afforded pure fused benzo-benzisapphyrins in 20-22% yields. The fused sapphyrins were characterized in detail by high-resolution mass spectrometry (HRMS) and one-dimensional (1D) and two-dimensional (2D) NMR spectroscopy. The 1H NMR spectra recorded at both 298 and at 233 K clearly exhibited the presence of a strong diatropic ring current in benzo-benzisapphyrins, and the macrocycles are of aromatic nature. The DFT-optimized structure of benzo-benzisapphyrin revealed that the macrocycle was planar to a great extent due to the rigid structure of the dibenzopyrrole moiety, and the NICS(0) value of -11.2 ppm supports the aromatic nature of macrocycles. The absorption spectra of benzo-benzisapphyrins showed three weak Q bands approximately in the region of 650-900 nm and a strong Soret band at 480 nm, along with a shoulder band at ∼510 nm. The diprotonated derivative generated by the addition of excess TFA to the benzo-benzisapphyrin macrocycle exhibited bathochromically shifted absorption bands compared to the free base macrocycle.

Bioassay-guided isolation and characterization of lead antimicrobial compounds from Acacia hydaspica plant extract

Acacia hydaspica possesses varied pharmacological attributes. We aimed to examine the antimicrobial potential and isolate the active antimicrobial metabolites. The plant extract was fractionated and the antimicrobial activity of the crude extract, fractions and compounds was tested by agar well diffusion and agar tube dilution and broth dilution methods. Bacterial strains selected for bioactivity testing were Staphylococcus aureus, Enterococcus faecalis, Bacillus subtilis, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Acinetobacter baumannii while selected strains from kingdom fungi were Candida albicans, Cryptococcus neoformans, Fusarium solani and Aspergillus. The active compounds were isolated from Acacia hydaspica by bioassay-guided fractionation and identified by nuclear magnetic resonance and spectroscopic techniques. S. aureus cell surface proteins, Autolysins (Atl), Clumping factor A (ClfA), and Fibronectin Binding Proteins (FnBP), were molecularly docked with Catechin 3-O-gallate (CG) and Methyl gallate (MG) and binding energy and molecular interactions between the proteins and compounds were analyzed. Ethyl acetate (AHE) and Butanol (AHB) fractions of A. hydaspica were the most active fractions against tested microbial strains. Therefore, both were subjected to bioassay-directed fractionation which led to the isolation of one pure active antimicrobial AHE and one active pure compound from AHB fraction besides active enriched isolates. Methyl-gallate (MG) and catechin-3-gallate (CG) are active compounds extracted from AHE and AHB fractions respectively. In antibacterial testing MG significantly inhibited the growth of E. coli (MIC50 = 21.5 µg/ml), B. subtilus (MIC50 = 23 µg/ml) and S. aureus (MIC50 = 39.1 µg/ml) while moderate to low activity was noticed against other tested bacterial strains. Antifungal testing reveals that MG showed potent antifungal activity against F. solani (MIC50 = 33.9 µg/ml) and A. niger (MIC50 = 41.5 µg/ml) while lower antifungal activity was seen in other tested strains. AHB fractions and pure compound (CG) showed specific antibacterial activity against S. aureus only (MIC50 = 10.1 µg/ml) while compound and enriched fractions showed moderate to no activity against other bacterial and fungal strains respectively. Molecular docking analysis revealed that CG interacted more strongly with the cell surface proteins than MG. Among these proteins, CG made a stronger complex with ClfA (binding affinity − 9.7) with nine hydrophobic interactions and five hydrogen bonds. Methyl gallate (MG) and catechin 3-O-gallate (CG) are the major antimicrobial compound from A. hydaspica that inhibit the growth of specific microbes. The occurrence of MG and CG endorse the traditional antimicrobial applicability of A. hydaspica, and it can be a legitimate alternative to control specific microbial infections.

Chemical Constituents of Macaranga occidentalis, Antimicrobial and Chemophenetic Studies.

Medicinal plants are known as sources of potential antimicrobial compounds belonging to different classes. The aim of the present work was to evaluate the antimicrobial potential of the crude extract, fractions, and some isolated secondary metabolites from the leaves of Macaranga occidentalis, a Cameroonian medicinal plant traditionally used for the treatment of microbial infections. Repeated column chromatography of the ethyl acetate and n-butanol fractions led to the isolation of seventeen previously known compounds (1-17), among which three steroids (1-3), one triterpene (4), four flavonoids (5-8), two stilbenoids (9 and 10) four ellagic acid derivatives (11-14), one geraniinic acid derivative (15), one coumarine (16), and one glyceride (17). Their structures were elucidated mainly by means of extensive spectroscopic and spectrometric (1D and 2D NMR and, MS) analysis and comparison with the published data. The crude extract, fractions, and isolated compounds were all screened for their antimicrobial activity. None of the natural compounds was active against Candida strains. However, the crude extract, fractions, and compounds showed varying levels of antibacterial properties against at least one of the tested bacterial strains, with minimal inhibitory concentrations (MICs) ranging from 250 to 1000 μg/mL. The n-butanol (n-BuOH) fraction was the most active against Escherichia coli ATCC 25922, with an MIC value of 250 μg/mL. Among the isolated compounds, schweinfurthin B (10) exhibited the best activity against Staphylococcus aureus NR 46003 with a MIC value of 62.5 μg/mL. In addition, schweinfurthin O (9) and isomacarangin (6) also exhibited moderate activity against the same strain with a MIC value of 125 μg/mL. Therefore, pharmacomodulation was performed on compound 6 and three new semisynthetic derivatives (6a-c) were prepared by allylation and acetylation reactions and screened for their in vitro antimicrobial activity. None of the semisynthetic derivatives showed antimicrobial activity against the same tested strains. The chemophenetic significance of the isolated compounds is also discussed in this paper.

Testicular heat shock protein effects of Methanolic and Phenolic extracts of N. sativa seed in chronic heat-stressed male Wistar rats

In order to evaluate the efficacy of crude methanolic and phenolic extracts of Nigella sativa seed in modulating protective role response in mammals under chronic heat stress. Forty nine mature male Wister rats (weighted: 250 ± 10 g, aged: 8 weeks) has been randomly divided into 7 equal groups. Four groups were reared under normal room temperature (20±1ºC) which included negative control (Nc) was reared without any treatment, positive control (C) was drenched with drinking water, treated group (M) was drenched with metanolic extract of N. sativa (1 g/ kg bw), and treated group (P) was drenched with phenolic extract of N. sativa (0.3 g/ kg bw). Other three groups has been reared under high room temperature (35 ± 1 cº) which included heated positive control (Hc) was drenched drinking water, heated treated group (Hm) was drenched with methanolic extract of N. sativa (1 g/ kg bw), and heated treated group (Hp) was drenched with phenolic extract of N. sativa (0.3 g/ kg bw). The experiment extended for 18 days.Twenty four hours after the last day of experiment, male rats has been sacrificed and body organs testis was removed and weighted .Testis samples (100 mg) were quickly obtained and putted in liquid nitrogen for heat shock protein 70 (HSP70) gene expression analysis using reverse transcriptase polymerase chain reaction (RT-PCR). Revealed insignificant differences in testes weights among the experimental groups. RT-PCR results showed that level of mRNA expression of HSP70 gene in testis tissues in treatment groups methanolic extract (M, Hm) (1g/ kg, BW, daily) and phenolic compound (P, Hp, 0.3g/ kg, BW, daily) of Nigella sativa seed was significantly higher than that of non-treated groups (Nc, C, and Hc). We have suggested that crude methanolic extract and phenolic compounds obtained from Nigella sativa seed have an efficient role in modulating protective role response of mammals under chronic heat stress in mature male Wistar rats.

Anti-Salmonella activity on multidrug-resistant strains and cytotoxicity of extracts and constituents of Garcinia brevipedicellata and Garcinia epunctata

The morbidity of Salmonella infections remains high partly due to emergence of multidrug-resistant (MDR) strains. Garcinia species have demonstrated activity against a wide range of infectious organisms including bacteria. Two species, Garcinia brevipedicellata and G. epunctata were investigated for activity against MDR clinical isolates of Salmonella. Methanol extracts of the leaves of both plants were serially re-extracted using ethyl acetate (EtOAc), acetone (Ace) and methanol (MeOH); and the three extracts tested for antibacterial activity by disc diffusion and microdilution methods, and cytotoxicity effects against monkey kidney epithelial (LLCMK2) cells. Five of eighteen pure compounds isolated, identified and tested for activity include β-sitosterol (1), stigmasterol (2), epunctosides A (3), B (4) from G. epunctata and brevipedicelone D (5) from G. brevipedicellata; among which three are new compounds (3, 4 and 5). The EtOAc extract of G. epunctata and brevipedicelone D (5), recorded maximum diameters of zones of inhibition of 18 and 17 mm respectively corresponding to moderate activity. All the four crude extracts recorded the lowest minimum inhibitory concentration (MIC) of 0.125 µg/mL, corresponding to high activity against MDR Salmonella isolates and control strains. Brevipedicelone D (5) showed moderate activity with the lowest MIC of 16 µg/mL. All the crude extracts and compound 5 were not cytotoxic (CC50 = 250 - 809µg/mL). Low minimum bactericidal concentrations (≤ 2 mg/mL) were recorded against most bacteria strains which may indicate bactericidal activity. This is the first report of moderate to high activity against MDR Salmonella and no cytotoxicity of the leaves and pure compounds from G. brevipedicellata and G. epunctata; hence, the leaves should be further investigated as a potential alternative treatment for infections of these strains and source of an antibacterial natural product lead.