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Prostate cancer is a leading cause of morbidity and mortality among men globally. In this study, we employed an in silico approach to predict the possible mechanisms of action of selected novel compounds reported against prostate cancer epigenetic targets and their derivatives, exhausting through ADMET profiling, drug-likeness, and molecular docking analyses. The selected compounds: sulforaphane, silibinin, 3, 3'-diindolylmethane (DIM), and genistein largely conformed to ADMET and drug-likeness rules including Lipinski's. Docking studies revealed strong binding energy of sulforaphane with HDAC6 (- 4.2 kcal/ mol), DIM versus HDAC2 (- 5.2 kcal/mol), genistein versus HDAC6 (- 4.1 kcal/mol), and silibinin against HDAC1 (- 7.0 kcal/mol) coupled with improved binding affinities and biochemical stabilities after derivatization. Findings from this study may provide insight into the potential epigenetic reprogramming mechanisms of these compounds against prostate cancer and could pave the way toward more success in prostate cancer phytotherapy.
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Introduction: For decades, viral diseases have been treated using medicinal plants and herbal practices in the northern part of Nigeria. Though scarcely investigated, these medicinal plants could serve as potential sources for novel antiviral drugs against emerging and remerging viral diseases. Therefore, this study is aimed at investigating the medicinal practices and plants used to treat emerging and re-emerging viral diseases including hepatitis, poliomyelitis, monkeypox, smallpox, yellow fever, Lassa fever, meningitis, and COVID-19 in some northern states; Katsina, Kebbi, Kwara and Sokoto states. Method: Administered questionnaires and oral interviews were used to collect information on medicinal plants, method of preparation of herbal formulations, diagnosis, and treatment of viral diseases. Medicinal plants were collected, botanically identified, and assigned voucher numbers. The plant names were verified using www.theplantlist.org, www.worldfloraonline.org and the international plant names index. Result: A total of 280 participating herbal medicine practitioners (HMPs) mentioned 131 plants belonging to 65 families. Plant parts such as roots, bark, leaf, seed, and fruit were prepared as a decoction, concoction, infusion, or ointment for oral and topical treatment of viral diseases. Moringa oleifera (75.3%), Elaeis guineensis Jacq. (80%), and Acacia nilotica (70%) were the most frequently mentioned plants in Kebbi, Kwara and Sokoto states, respectively. Conclusion: The study revealed scarcely investigated and uninvestigated medicinal plants used to treat hepatitis, poliomyelitis, monkeypox, smallpox, yellow fever, Lassa fever, meningitis, and COVID-19. Future studies should be conducted to determine the antiviral potency and isolate novel bioactive agents from these plants against viral diseases.
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Background: The presence of diabetes mellitus (DM) among COVID-19 patients is associated with increased hospitalization, morbidity, and mortality. Evidence has shown that hyperglycemia potentiates SARS-CoV-2 (severe acute respiratory syndrome coronavirus 2) infection and plays a central role in severe COVID-19 and diabetes comorbidity. In this review, we explore the therapeutic potentials of herbal medications and natural products in the management of COVID-19 and DM comorbidity and the challenges associated with the preexisting or concurrent use of these substances. Methods: Research papers that were published from January 2016 to December 2021 were retrieved from PubMed, ScienceDirect, and Google Scholar databases. Papers reporting clinical evidence of antidiabetic activities and any available evidence of the anti-COVID-19 potential of ten selected natural products were retrieved and analyzed for discussion in this review. Results: A total of 548 papers (73 clinical trials on the antidiabetic activities of the selected natural products and 475 research and review articles on their anti-COVID-19 potential) were retrieved from the literature search for further analysis. A total of 517 articles (reviews and less relevant research papers) were excluded. A cumulative sum of thirty-one (31) research papers (20 clinical trials and 10 others) met the criteria and have been discussed in this review. Conclusion: The findings of this review suggest that phenolic compounds are the most promising phytochemicals in the management of COVID-19 and DM comorbidity. Curcumin and propolis have shown substantial evidence against COVID-19 and DM in humans and are thus, considered the best potential therapeutic options.
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Cancer is a rapidly growing non-communicable disease worldwide that is responsible for high mortality rates, which account for 9.6 million death in 2018. Dihydroartemisinin (DHA) is an active metabolite of artemisinin, an active principle present in the Chinese medicinal plant Artemisia annua used for malaria treatment. Dihydroartemisinin possesses remarkable and selective anticancer properties however the underlying mechanism of the antitumor effects of DHA from the structural point of view is still not yet elucidated. In the present study, we employed molecular docking simulation techniques using Autodock suits to access the binding properties of dihydroartemisinin to multiple protein targets implicated in cancer pathogenesis. Its potential targets with comprehensive pharmacophore were predicted using a PharmMapper database. The co-crystallised structures of the protein were obtained from a Protein Data Bank and prepared for molecular docking simulation. Out of the 24 selected protein targets, DHA has shown about 29% excellent binding to the targets compared to their co-crystallised ligand. Additionally, 75% of the targets identified for dihydroartemisinin binding are protein kinases, and 25% are non-protein kinases. Hydroxyl functional group of dihydroartemisinin contributed to 58.5% of the total hydrogen interactions, while pyran (12.2%), endoperoxide (9.8%), and oxepane (19.5%) contributed to the remaining hydrogen bonding. The present findings have elucidated the possible antitumor properties of dihydroartemisinin through the structural-based virtual studies, which provides a lead to a safe and effective anticancer agent useful for cancer therapy.Communicated by Ramaswamy H. Sarma.
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Artemisininas , Neoplasias , Artemisininas/farmacología , Artemisininas/uso terapéutico , Detección Precoz del Cáncer , Humanos , Simulación del Acoplamiento Molecular , Neoplasias/tratamiento farmacológicoRESUMEN
The possible evolutionary trend of COVID-19 in South Africa was investigated by comparing the genome of SARS-CoV-2 isolated from a patient in KwaZulu-Natal, South Africa with those isolated from China, Spain, Italy, and United States, as well as the genomes of Bat SARS CoV, Middle East Respiratory Syndrome Coronavirus (MERS-CoV), Mouse Hepatitis Virus (MHV), and Infectious Bronchitis Virus (IBV). Phylogenetic analysis revealed a strong homology (96%) between the genomes of SARS-CoV-2 isolated from KwaZulu-Natal, South Africa and those isolated from the study countries as well as those isolated from bat SARS CoV, MERS-CoV, MHV and IBV. The ability of phytocannabinoids from Cannabis sativa infusion to interact with gene segments (mRNAs) coding for proteins implicated in viral replication, assembly and release were also investiagted using computational tools. Hot water infusion of C. sativa leaves was freeze-dried and subjected to Gas Chromatography-Mass Spectroscopy analysis which revealed the presence of tetrahydrocannabivarin, cannabispiran, cannabidiol tetrahydrocannabinol, cannabigerol, and cannabinol. Molecular docking analysis revealed strong binding affinities and interactions between the phytocannabinoids and codon mRNAs for ORF1ab, Surface glycoprotein, Envelope protein and Nucleocapsid phosphoprotein from SARS-CoV-2 whole genome which may be due to chemico-biological interactions as a result of nucleophilic/electrophilic attacks between viral nucleotides and cannabinoids. These results depict the spread of SARS-CoV-2 is intercontinental and might have evolved from other coronaviruses. The results also portray the phytocannabinoids of C. sativa infusion as potential therapies against COVID-19 as depicted by their ability to molecularly interact with codon mRNAs of proteins implicated in the replication, translation, assembly, and release of SARS-CoV-2. However, further studies are needed to verify these activities in pre-clinical and clinical studies.
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The use of toxic and less bioavailable inorganic selenium can now be supplemented with an alternative organic source from bacterial species in nutrition for human and animal benefit. This study investigated the effects of selenium sources on laying performance, egg quality characteristics, intestinal morphology, caecum microbial population, and digesta volatile fatty acids in laying hens. One hundred and forty-four Lohman Brown Classic laying hens, at 23 weeks of age, were divided into four experimental groups (36 hens in each), differing in form of Se supplementation: no Se supplementation (Con), 0.3 mg/kg of inorganic Se in the form of sodium selenite (Na2SeO3), 0.3 mg/kg of organic Se from selenium yeast (Se-Yeast), and 0.3 mg/kg of organic Se from Stenotrophomonas maltophilia (bacterial organic Se, ADS18). The results showed that different dietary Se sources significantly affected laying rate, average egg weight, daily egg mass, feed conversion ratio (FCR), and live bodyweight (LBW) (p < 0.05). However, average daily feed intake and shell-less and broken eggs were unaffected (p > 0.05) among the treatment groups. The findings revealed that selenium sources had no (p > 0.05) effect on egg quality (external and internal) parameters. However, eggshell breaking strength and Haugh unit were significantly (p < 0.05) improved with organic (ADS18 or Se-yeast) Se-fed hens compared to the control group. In addition, egg yolk and breast tissue Se concentrations were higher (p < 0.05) in the dietary Se supplemented group compared to the control. Intestinal histomorphology revealed that hens fed ADS18 or Se-Yeast groups had significantly (p < 0.05) higher villi height in the duodenum and jejunum compared to those fed Na2SeO3 or a basal diet. However, when compared to organic Se fed (ADS18 or Se-Yeast) hens, the ileum villus height was higher (p < 0.05) in the basal diet group; with the lowest in the SS among the treatment groups. A significant increase (p < 0.05) of Lactobacilli spp. and Bifidobacteria spp., and a decrease of Escherichia coli and Salmonella spp. population were observed in the organic (ADS18 or Se-yeast) compared to inorganic supplemented and control hens. The individual digesta volatile fatty acid (VFA) was significantly different, but with no total VFA differences. Thus, bacterial selenoprotein or Se-yeast improved the performance index, egg quality characteristics, egg yolk and tissue Se contents, and intestinal villus height in laying hens. Moreover, caecum beneficial microbes increased with a decrease in the harmful microbe population and affected individual cecal volatile fatty acids without affecting the total VFA of the laying hens digesta.
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The 2019 coronavirus disease (COVID-19) is a potentially fatal multisystemic infection caused by the severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2). Currently, viable therapeutic options that are cost effective, safe and readily available are desired, but lacking. Nevertheless, the pandemic is noticeably of lesser burden in African and Asian regions, where the use of traditional herbs predominates, with such relationship warranting a closer look at ethnomedicine. From a molecular viewpoint, the interaction of SARS-CoV-2 with angiotensin converting enzyme 2 (ACE2) is the crucial first phase of COVID-19 pathogenesis. Here, we review plants with medicinal properties which may be implicated in mitigation of viral invasion either via direct or indirect modulation of ACE2 activity to ameliorate COVID-19. Selected ethnomedicinal plants containing bioactive compounds which may prevent and mitigate the fusion and entry of the SARS-CoV-2 by modulating ACE2-associated up and downstream events are highlighted. Through further experimentation, these plants could be supported for ethnobotanical use and the phytomedicinal ligands could be potentially developed into single or combined preventive therapeutics for COVID-19. This will benefit researchers actively looking for solutions from plant bioresources and help lessen the burden of COVID-19 across the globe.
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The chicken egg is one of nature's flawlessly preserved biological products, recognized as an excellent source of nutrients for humans. Selenium (Se) is an essential micro-element that plays a key role in biological processes. Organic selenium can be produced biologically by the microbial reduction of inorganic Se (sodium selenite). Therefore, the possibility of integrating Se enriched bacteria as a supplement in poultry feed can provide an interesting source of organic Se, thereby offering health-related advantages to humans. In this study, bacterial selenoproteins from Stenotrophomonas maltophilia was used as a dietary supplement with other Se sources in Lohman brown Classic laying hens to study the egg yolk color, egg yolk and breast antioxidant profile, oxidative stability, and storage effect for fresh and stored egg yolk at 4 ± 2 °C for 14-days. The results showed that dietary Se supplementation significantly (p < 0.05) improved egg yolk color, the antioxidant profile of egg yolk, and breast meat (total carotenoid and phenol content). When the Se treated groups were compared to control groups, there was a significant (p < 0.05) decrease in total cholesterol in fresh and stored egg yolk and breast muscle. In hens that were fed ADS18-Se, the primary oxidation products (MDA) concentrations in the eggs, breast, and thigh muscle, and plasma were significantly (p < 0.05) lower. However, the MDA content increased (p < 0.05) with an extended storage time in egg yolk. In comparison to inorganic Se and basal diets, egg yolk from hens fed organic Se remained fresh for two weeks. The egg yolk color, antioxidant profile, and oxidative status of egg yolk and tissue improve with dietary Se organic supplementation (ADS18 > Se-Yeast). The source of supplemented organic Se is critical for egg enrichment and antioxidant properties. As a result, ''functional eggs'' enriched with organic Se becomes possible to produce.
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Vitex doniana leaves are used traditionally in West Africa for the treatment of swellings and cancer. We investigated if Vitex doniana leaves extract could ameliorate 7, 12-dimethylbenz[a]anthracene (DMBA)-induced mammary damage. Female Wistar rats aged 52 ± 2 day were administered 80 mg/kg DMBA. After monitoring for 150 day, rats were administered 0, 50, 100, 200 mg/kg Vitex doniana and 20 mg/kg Tamoxifen for 14 day. Serum estrogen receptor-α, IL-1ß and TNF -α levels were determined using ELISA kits. Oxidative stress markers in mammary tissue homogenates were determined using standard spectrophotometric methods. Histopathological examination was done using hematoxylin and eosin staining and cyclooxygenase-2 (COX-2) expression using immunohistochemistry. Liquid chromatography-mass spectrometry was used to determine components present in the extract. Although tumors were not observed, significantly (p < 0.05) lower estrogen receptor-α, malondialdehyde, IL-1ß and TNF -α levels, significantly (p < 0.05) higher glutathione and catalase activity, attenuation of malignant epithelial hyperplasia and mild COX-2 expression were observed in rats administered Vitex doniana when compared to DMBA-induced untreated control. Liquid chromatography-mass spectrometry analysis of the V. doniana extract revealed the presence of 4,5-dihydroxy-7-methoxy-6-methylflavone and vanillylamine, which are compounds with reported antioxidant and anti-inflammatory effects. Collectively, treatment with Vitex doniana ameliorated some derangement observed in DMBA-induced rats.
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Neoplasias Mamarias Experimentales , Vitex , 9,10-Dimetil-1,2-benzantraceno , Animales , Antracenos , Femenino , Extractos Vegetales , Hojas de la Planta , Ratas , Ratas WistarRESUMEN
Background: Myopathy is a disorder of skeletal muscles and has a rare occurrence in pregnancy. It may present with numbness/weakness. The occurrence of isolated weakness involving all the limbs is alarming to the patient and the diagnosis can be challenging to the Obstetrician. We present a case of hypokalaemic paralysis in pregnancy. Case report: A 32-year-old grand multipara presented at 31 weeks gestation with numbness in all limbs for nine days and one-day history of weakness in all limbs. She had a similar episode in her last pregnancy with complete resolution by the end of puerperium. On examination, she was conscious with a Glasgow Coma Scale score was 15/15, had no signs of meningeal irritation, and no cranial nerve palsy. She had normal muscle bulk; the power of 4/5 in both upper limbs and 3/5 in both lower limbs. There was no clearly defined sensory level. Planter reflex was flexor symmetrically. A review of other systems was unremarkable. Her PCV was 35% and random blood glucose was 4.2mmol/l. Serum biochemistry showed severe hypokalaemia of 1.8mmol/l with normal levels of sodium and chloride. Urinary potassium level was normal. She had parenteral correction of potassium with complete resolution of weakness, and she was maintained on oral potassium supplements. She had an uneventful delivery at 37 weeks gestation. Conclusion: Measuring the serum level of potassium should be part of the initial workup when evaluating pregnant women presenting with muscle weakness. Multidisciplinary management leads to early diagnosis, prompt management, and a good prognosis.
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This study was designed to explore and record various medicinal plants integrated into the traditional system of medicine for the treatment of cancer. The traditional system of medicine is a routine practiced among the indigenous ethnic groups of Sokoto state. A semi-structured questionnaire was designed and used for data collection around the selected Local Government Areas. A substantial number of plant species were identified, recorded, and collected for preservation. Data collected for each specie was analysed to assess its frequent use among the medicinal plants. A total of 67 species belonging to 31 families have been identified and recorded. Out of the 473 frequency of citation (FC), Acacia nilotica was the most frequently cited specie (32 FC, 64% FC, 0.6 RFC), followed by Guiera senegalensis (27 FC, 54% FC, 0.5 RFC), Erythrina sigmoidea (17 FC, 34% FC, 0.3 RFC), and subsequently Combretum camporum (15 FC, 30% FC, 0.3 RFC). The most common parts of the plants used include the barks (55.2%), the roots (53.2%), and the leaves (41.8%). Additionally, decoction (74.6%), powdered form (49.3%), and maceration (46.3%) are the most frequently used mode of preparation. The historical knowledge of a traditional system of medicine practiced by the native traditional healers of Sokoto for the treatment of cancer has been documented. The present study further provides a baseline for future pharmacological investigations into the beneficial effects of such medicinal plants for the treatment of cancer.
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Type 2 diabetes is the most prominent of all diabetes types, contributing to global morbidity and mortality. Availability and cost of treatment with little or no side effect especially in developing countries, remains a huge burden. This has led to the search of affordable alternative therapies especially from medicinal plants. In this study, the antidiabetic effect of the methanolic extract, dichloromethane (DCM), butanol (BuOH) and aqueous fractions of Clerodendrum volubile leaves were investigated in type 2 diabetic rats for their effect on glucose homeostasis, serum insulin level and hepatic biomarkers, lipid profile, pancreatic redox balance and Ca2+ levels, and ß-cell distribution and function. The DCM was further fractionated to isolate the active compounds, biochanin and 5,7,4'-trimethoxykaempferol. They were investigated for their toxicity and ADMET properties, α-glucosidase and angiotensin I converting enzyme (ACE) inhibitory activities in silico. There were significant (p < 0.05) decrease in blood glucose, cholesterol, LDL-C, vLDL-C, triglyceride, AST and ALT levels in all treated groups, with DCM fraction showing the best activity. All treated rats showed significantly (p < 0.05) improved anti-oxidative activities. Treatment with the DCM fraction led to significant (p < 0.05) increased serum insulin and pancreatic Ca2+ levels, as well as improved ß-cell distribution and function. DCM fraction also showed improved glucose tolerance. DCM fraction dose-dependently inhibited ACE activity. The toxicity class of the isolated compounds was predicted to be 5. They were also predicted to be potent inhibitors of cytochrome P (CYPs) 1A2, 2D6 and 3A4. They docked well with α-glucosidase and ACE. These results indicate the therapeutic potential of the plant against type 2 diabetes, with the DCM fraction being the most potent which may be attributed to the isolated flavones. It further suggests antihypertensive potentials of the DCM fraction. However, inhibition of CYPs by the flavones may suggest caution in usage with other prescribed drugs metabolized by these enzymes.
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Vascular endothelial growth factor (VEGF) is a glycoprotein vital to the regulation of vascular endothelial cells proliferation, migration and angiogenesis. The expression of VEGF is required for the formation of new blood vessels critical in supplying oxygen and nutrition in the course of tumorigenesis. The present study investigated the effect of 5,6-dehydrokawain isolated from the rhizomes of Alpinia mutica on VEGF expression in vitro using HT-29 cell line. The results revealed that 5,6-dehydrokawain induced the expression of proangiogenic tumour-derived VEGF of HT-29 cells, which may explain the inability of 5,6-dehydrokawain in suppressing cancer cells proliferation.
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Alpinia/química , Neoplasias Colorrectales/metabolismo , Pironas/farmacología , Rizoma/química , Factor A de Crecimiento Endotelial Vascular/efectos de los fármacos , Alpinia/anatomía & histología , Moduladores de la Angiogénesis/aislamiento & purificación , Moduladores de la Angiogénesis/farmacología , Proliferación Celular/efectos de los fármacos , Neoplasias Colorrectales/patología , Células HT29 , Humanos , Neovascularización Patológica/inducido químicamente , Extractos Vegetales/farmacología , Pironas/aislamiento & purificación , Factor A de Crecimiento Endotelial Vascular/genética , Factor A de Crecimiento Endotelial Vascular/metabolismoRESUMEN
BACKGROUND: Cancer is a multifaceted metabolic disease that affects sizeable dwellers of rural and urban areas. Among the various types of cancer, mammary cancer is one of the most frequently diagnosed cancers in women. Its menace can be curbed with locally consumed spices due to their multiple bioactive phytochemicals. AIMS: This review focuses on the breast cancer chemopreventive and therapeutic potentials of locally consumed spices. METHODS/RESULTS: The most commonly consumed spices with breast cancer chemopreventive and chemotherapeutic phytochemical include pepper, onions, ginger, garlic, curry and thyme containing many biologically active metabolites ranging from vitamins, fatty acids esters, polyphenols/phenolics, sulfurcontaining compounds and anthraquinones with proven antioxidant, anti-inflammatory, immuno-modulatory, antitumor and anticancer properties against breast cancer/carcinogenesis. Therefore, extracts and active principles of these spices could be explored in breast cancer chemoprevention and possibly therapeutically which may provide an avenue for reducing the risk and prevalence of breast cancer.
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Antineoplásicos/farmacología , Neoplasias de la Mama/tratamiento farmacológico , Neoplasias de la Mama/prevención & control , Quimioprevención , Antineoplásicos/química , Neoplasias de la Mama/patología , Proliferación Celular/efectos de los fármacos , Femenino , HumanosRESUMEN
The antidiabetic effects of the ethyl acetate (EtOAc) fraction of Clerodendrum volubile leaves was investigated in this study. EtOAc extract was also fractionated to isolate the active compounds. The structure of the isolated compound (Protocatechuic acid) was established using 1H and 13C NMR spectroscopies and mass spectrometry. Protocatechuic acid was investigated for its anti-oxidative burst in polymorphonuclear neutrophils (PMNs) and macrophages. It was also docked with α-glucosidase and TNF-α. Acute treatment with EtOAc fraction of Clerodendrum volubile leaves significantly (p<0.05) decreased blood glucose level and hepatic biomarkers, and significantly (p<0.05) increased serum insulin level and ß-cell function. It had little or no effect on serum lipid profile and atherogenic indices. Protocatechuic acid significantly (p<0.05) suppressed phagocytic oxidative burst and docked well with α-glucosidase and TNF-α. These results indicate the therapeutic effect of EtOAc fraction of C. volubile on type 2 diabetes and its complications, which can be attributed to the main bioactive compound, protocatechuic acid.
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Acetatos/uso terapéutico , Clerodendrum , Citocinas/antagonistas & inhibidores , Hidroxibenzoatos/uso terapéutico , Hipoglucemiantes/uso terapéutico , Fagocitos/efectos de los fármacos , Estallido Respiratorio/efectos de los fármacos , Acetatos/aislamiento & purificación , Acetatos/farmacología , Animales , Citocinas/metabolismo , Humanos , Hidroxibenzoatos/aislamiento & purificación , Hidroxibenzoatos/farmacología , Hipoglucemiantes/aislamiento & purificación , Hipoglucemiantes/farmacología , Mediadores de Inflamación/antagonistas & inhibidores , Mediadores de Inflamación/metabolismo , Masculino , Simulación del Acoplamiento Molecular , Fagocitos/metabolismo , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Ratas , Ratas Wistar , Estallido Respiratorio/fisiologíaRESUMEN
The immunomodulatory potentials of the crude methanolic extract and fractions [n-hexane (Hex), n-dichloromethane (DCM), ethyl acetate (EtOAc) and n-butanol (BuOH)] of Clerodendrum volubile flowers were investigated on whole blood phagocytic oxidative burst using luminol-amplified chemiluminescence technique. They were also investigated for their free radicals scavenging activities. The DCM fraction showed significant (p<0.05) anti-oxidative burst and free radical scavenging activities indicating high immunomodulatory and antioxidant potencies respectively. Cytotoxicity assay of the DCM fraction revealed a cytotoxic effect on CC-1 normal cell line. GCMS analysis revealed the presence of triacetin; 3,6-dimethyl-3-octanol; 2R - Acetoxymethyl-1,3,3-trimethtyl - 4t - (3-methyl-2-buten-1-yl) - 1c - cyclohexanol and Stigmastan - 3,5-diene in DCM fraction. These compounds were docked with the active sites of cyclooxygenase-2 (COX-2). Triacetin, 3,6-dimethyl-3-Octanol, and 2R-Acetoxymethyl-1,3,3-trimethtyl-4t-(3-methyl-2-buten-1-yl)-1c-cyclohexanol docked comfortably with COX-2 with good scoring function (-CDocker energy) indicating their inhibitory potency against COX-2. 3,6-dimethyl-3-Octanol, displayed the lowest predicted free energy of binding (-21.4kcalmol-1) suggesting its stronger interaction with COX-2, this was followed by 2R - Acetoxymethyl-1, 3, 3-trimethtyl-4t-(3-methyl-2-buten-1-yl)-1c-cyclhexanol (BE=-20.5kcalmol-1), and triacetin (BE=-10.9kcalmol-1). Stigmastan - 3,5-diene failed to dock with COX-2. The observed suppressive effect of the DCM fraction of C. volubile flower methanolic extract on phagocytic oxidative burst indicates an immunomodulatory potential. This is further reflected in its free scavenging activities and synergetic modulation of COX-2 activities by its identified compounds in silico.
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Clerodendrum , Ciclooxigenasa 2/metabolismo , Flores , Fagocitosis/fisiología , Extractos Vegetales/farmacología , Estallido Respiratorio/fisiología , Cristalografía por Rayos X , Ciclooxigenasa 2/química , Relación Dosis-Respuesta a Droga , Activación Enzimática/efectos de los fármacos , Activación Enzimática/fisiología , Depuradores de Radicales Libres/química , Depuradores de Radicales Libres/aislamiento & purificación , Depuradores de Radicales Libres/farmacología , Humanos , Inmunomodulación/efectos de los fármacos , Inmunomodulación/fisiología , Simulación del Acoplamiento Molecular/métodos , Fagocitosis/efectos de los fármacos , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Estructura Secundaria de Proteína , Estallido Respiratorio/efectos de los fármacosRESUMEN
The search for novel drugs and alternative medicine has led to increased research in medicinal plants. Among such plants is the orange fruit. Its peels have been utilized for long as an active ingredient in most traditional medicines. This study aims at investigating the chemical properties of the hexane and dichloromethane (DCM) extracts of orange peel as well as their biological potentials. Blended peels were extracted with n-hexane and n-dichloromethane, respectively. The resulting extracts were subjected to gas chromatography mass spectrometry (GCMS) characterization. The extracts were also assayed for free radical scavenging ability against 1,1 -diphenyl -2 picrylhydrazyl (DPPH), antioxidative burst via measuring luminol -amplified chemiluminescence response in human blood, and phytotoxicity against lemna minor. GCMS analysis revealed a predominance of fatty acid methyl esters in the hexane extract, while the DCM extract had more ketone metabolites. The DCM extract had significant (p < .05) higher free radical scavenging and antioxidative burst activities compared to the hexane. Both extracts revealed a significantly (p < .05) high phytotoxicity activity. Results from this study indicated that solvent type played a vital a role in the extraction of secondary metabolites, which are responsible for the observed biological activities. The higher activities by the DCM extract can be attributed to its constituents as revealed by GCMS analysis. There is great need to explore the phytotoxicity potentials of both extracts as natural herbicides.
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Antioxidantes/farmacología , Citrus/química , Extractos Vegetales/química , Extractos Vegetales/farmacología , Araceae/efectos de los fármacos , Frutas/química , Cromatografía de Gases y Espectrometría de Masas , Herbicidas/química , Hexanos/química , Humanos , Cloruro de Metileno/química , Pruebas de ToxicidadRESUMEN
Recent advances in functional foods-based research have increasingly become an area of major interest because it affects human health and activities. Functional foods are classes of foods with health promoting and disease preventing properties in addition to multiple nutritional values and of such type is honey. Acacia honey is a type of honey produced by bees (Apis mellifera) fed on Acacia flowers, hence the name. This review focuses on the potential biological activities of Acacia honey which includes quality, antioxidant, immuno-modulatory, antiproliferative and neurological properties at in vitro and in vivo levels. Based on our review, Acacia honey used from various researches is of high purity, contains some bioactive compounds ranging from vitamins, phenolics, flavonoids and fatty acids. It's highly nutritional with strong antioxidant and immuno-modulatory potentials which may therefore be considered a potential candidate for both cancer prevention and treatment. Neurologically, it may be considered as a viable therapeutic agent in the management of Alzheimer's disease.
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Miel , Adyuvantes Inmunológicos/farmacología , Antioxidantes/farmacología , Proliferación Celular/efectos de los fármacos , HumanosRESUMEN
AIM: This study aims at reporting the isolation, structure elucidation, and antioxidant potentials of ajugoside from C. volubile leaves in sodium nitroprusside (SNP)-induced oxidative stressed rat brain and hepatic tissues. MATERIALS AND METHOD: An iridoid monoterpene, ajugoside was isolated from the n-butanol fraction of C. volubile and evaluated for its antioxidant protective potential on brain and liver tissues of male Wister rats in an ex vivo model. Two molar concentrations (6.4 × 10(-4) M and 1.28 × 10(-3) M) of the metabolite and SNP were incubated with the tissues homogenate at 37°C for 2 hr prior to the test and assayed for catalase, superoxide dismutase (SOD) activities, and lipid peroxidation. α tocopherol (6.4 × 10(-4) M) was used as standard. RESULTS: Both molar concentrations exhibited high catalase activity in the tissues. However, 6.4 × 10(-4) M ajugoside exhibited a very high SOD activity (liver: 96.45 and brain: 96.30%) and inhibition of lipid peroxidation (liver: 88.11 and brain: 93.27%) compared to the standard. 1.28 × 10(-3) M ajugoside also exhibited good activities but lower than that of the standard and 6.4 × 10(-4) M ajugoside. DISCUSSION AND CONCLUSION: Ajugoside showed potent antioxidant activities as evidenced by the synergistic high activities of SOD and catalase as well as inhibition of lipid peroxidation in the studied tissues.