Antiviral potential of anthraquinones from Polygonaceae, Rubiaceae and Asphodelaceae: Potent candidates in the treatment of SARS-COVID-19, A comprehensive review.

Medicinal plants are being used as an alternative source of health management to cure various human ailments. The healing role is attributed to the hidden dynamic groups of various phytoconstituents, most of which have been recorded from plants and their derivatives. Nowadays, medicinal plants have gained more attention due to their pharmacological and industrial potential. Aromatic compounds are one of the dynamic groups of secondary metabolites (SM) naturally present in plants; and anthraquinones of this group are found to be attractive due to their high bioactivity and low toxicity. They have been reported to exhibit anticancer, antimicrobial, immune-suppressive, antioxidant, antipyretic, diuretic and anti-inflammatory activities. Anthraquinones have been also shown to exhibit potent antiviral effects against different species of viruses. Though, it has been reported that a medicinal plant with antiviral activity against one viral infection may be used to combat other types of viral infections. Therefore, in this review, we explored and highlighted the antiviral properties of anthraquinones of Polygonaceae, Rubiaceae and Asphodelaceae families. Anthraquinones from these plant families have been reported for their effects on human respiratory syncytial virus and influenza virus. They are hence presumed to have antiviral potential against SARS-CoV as well. Thus, anthraquinones are potential candidates that need to be screened thoroughly and developed as drugs to combat COVID-19. The information documented in this review could therefore serve as a starting point in developing novel drugs that may help to curb the SARS-COVID-19 pandemic.

Response Surface Methodology Applied to the Optimization of the Preparation of Antioxidant and Antidiabetic Extracts from Phragmanthera capitata (Spreng.) Balle: Effect of Particle Size, Powder-to-Solvent Ratio, and Temperature.

Phragmanthera capitata is a medicinal plant used in traditional medicine to treat several diseases, including diabetes. Its antioxidant properties and inhibitory effects on enzyme-carbohydrate digestion activities have been demonstrated. The present study aimed to provide data that can contribute to rationalizing the preparation of antioxidant and antidiabetic extracts from this plant. P. capitata (whole plant) growing on Persea americana was harvested at the fruiting stage. A response surface design-type central composite was applied to maximize the extraction yield, phenolic contents, and antioxidant and antidiabetic properties of the ethyl acetate extract of P. capitata. The influencing extraction factors were temperature, powder particle size, and solvent-to-powder ratio. The total phenolic content, total antioxidant capacity (TAC), DPPH scavenging ability, ferric reducing antioxidant power (FRAP), and antidiabetic (α-amylase and α-glucosidase inhibitory) effects of the extracts were determined using conventional methods. A temperature above 55°C contributed to the degradation of the extract, which was reflected in the GC-MS profile by a significant reduction in the number of compounds it contained. The optimal conditions were defined as 24.42°C for temperature, 250 µm powder particle size, and 8.30 (v:w) solvent-to-powder ratio. This extraction protocol resulted in more than twice the extraction yield (3.05%), TTC (62.30 mg TAE/g), TAC (41.41 mg AAE/g), FRAP (186.56 mg AAE/g), and α-amylase (IC50 15.05 µg/mL) and α-glucosidase (IC50 21.14 µg/mL) inhibitory activities compared to our previous results. Additionally, these optimal conditions led experimentally to the extraction of higher phenolic content and to the attainment of higher antioxidant and antidiabetic activity, which closely matched the predicted values. Using these conditions, it is possible to prepare an antidiabetic phytomedicine from P. capitatathat can prevent oxidative stress complications. However, further complementary studies should be carried out considering other factors that influence the composition and pharmacological properties of the extract.

Polyphenol-Rich Extracts of Xylopia and Aframomum Species Show Metabolic Benefits by Lowering Hepatic Lipid Accumulation in Diet-Induced Obese Mice.

Metabolic syndrome is a complex condition associated with a series of pathologies featuring glucose intolerance, diabetes, high blood pressure, dyslipidemia, microalbuminuria, overweight, and obesity. It is also related to nonalcoholic fatty liver disease (NAFLD), recognized as the most familiar cause of chronic liver disease worldwide. The overall prevalence of metabolic syndrome and, consequently, the one of NAFLD is constantly increasing worldwide. The initial management of these diseases involves lifestyle modifications, including changes in diet and physical exercise. In addition to conventional drugs like orlistat, botanicals are traditionally used to counteract these disorders, and some of them are currently under evaluation. The present work evaluated the in vivo beneficial effects of hydroalcoholic extracts of two Cameroonian spices, focusing on obesity-related hepatic lipid injury in high-fat-fed C57BL/6 mice. Hydroethanolic extracts were prepared and characterized by reverse phase-high-performance liquid chromatography (HPLC)-photodiode array detection and ultra performance liquid chromatography-triple time-of-flight electrospray ionization tandem mass spectroscopy (TOF-ESI-MS/MS) analysis. Plant extracts were orally administered for 30 days at different dose levels (100 and 200 mg kg-1 body weight (BW)) to obese C57BL/6 mice. Food intake (FI) and BW were recorded daily. Plasma biochemical parameters and lipid content were estimated at the beginning and at the end of the experiment. Liver tissues were subjected to histological examinations, lipid content, as well as oxidative stress markers, and FAME (fatty acid methyl esters) were estimated. Oral administration of extracts at 200 mg kg-1 BW significantly reduced FI and prevented BW gain. A decrease in the weight of the liver and a decrease in the hepatic and plasma lipid content were observed. Plasma enzyme (serum glutamic-oxaloacetic transaminase, SGOT; serum glutamic pyruvic transaminase, SGPT; alkaline phosphatase, ALP) activities were not indicative of any organ damage. Chemical analysis suggested that phenolic acids (4-caffeoylquinic acid, p-coumaric acid 4-O-glucoside, 5-caffeoylshikimic acid, caffeic acid hexose, and 4-O-methyl gallic acid) and flavonoids (morusin derivatives, naringenin-7-O-glucoside, and homoisoflavanone) identified in the extracts could potentially justify the biological properties observed. The main findings of this study showed that Xylopia parviflora (A. Rich.) Benth and Aframomum citratum (Pereira ex Oliv. et Hanb.) K. Shum decreased hepatic lipid accumulation in high-fat-diet (HFD)-induced obese C57BL/6 mice and confirmed, at least in part, our previous in vitro and ex vivo studies. The molecular mechanisms underlying these effects are still unclear and will be explored in the future.

Cameroonian Spice Extracts Modulate Molecular Mechanisms Relevant to Cardiometabolic Diseases in SW 872 Human Liposarcoma Cells.

The molecular pathophysiology of cardiometabolic diseases is known to be influenced by dysfunctional ectopic adipose tissue. In addition to lifestyle improvements, these conditions may be managed by novel nutraceutical products. This study evaluatedthe effects of 11 Cameroonian medicinal spice extracts on triglyceride accumulation, glucose uptake, reactive oxygen species (ROS) production and interleukin secretion in SW 872 human adipocytes after differentiation with 100 µM oleic acid. Triglyceride content was significantly reduced by all spice extracts. Glucose uptake was significantly increased by Tetrapleura tetraptera, Aframomum melegueta and Zanthoxylum leprieurii. Moreover, Xylopia parviflora, Echinops giganteus and Dichrostachys glomerata significantly reduced the production of ROS. Concerning pro-inflammatory cytokine secretion, we observed that Tetrapleura tetraptera, Echinops giganteus, Dichrostachys glomerata and Aframomum melegueta reduced IL-6 secretion. In addition, Xylopia parviflora, Monodora myristica, Zanthoxylum leprieurii, and Xylopia aethiopica reduced IL-8 secretion, while Dichrostachys glomerata and Aframomum citratum increased it. These findings highlight some interesting properties of these Cameroonian spice extracts in the modulation of cellular parameters relevant to cardiometabolic diseases, which may be further exploited, aiming to develop novel treatment options for these conditions based on nutraceutical products.

The Influence of Solvent, Host, and Phenological Stage on the Yield, Chemical Composition, and Antidiabetic and Antioxidant Properties of Phragmanthera capitata (Sprengel) S. Balle.

Phragmanthera capitata was reported to possess many biological properties making it a good candidate for the formulation of a phytomedicine with multiple effects. In this work, we studied some factors likely to modify these therapeutic properties with the aim to contribute to its standardization as an improved traditional medicine. P. capitata parasitizing Persea americana, Psidium guajava, and Podocarpus mannii were harvested at three phenological stages (vegetative, flowering, and fruiting stages). The extracts were prepared by maceration in n-hexane, ethyl acetate, ethanol, methanol, and distilled water. The total phenolic, flavonoid, flavonol, and tannin contents were measured using appropriate methods. The antioxidant potential of extracts was investigated using TAC, DPPH scavenging, and FRAP methods. The α-amylase and α-glucosidase inhibitory activities of extracts were determined using enzymatic methods. The ethyl acetate extracts with the best phenolic content were subjected to HPLC analysis. The extraction yields were higher with methanol. The ethyl acetate extract of P. capitata harvested from P. guajava showed a stable HPLC profile during the development of the plant, while extracts from the plant collected from P. americana and P. mannii showed both qualitative and quantitative variations according to phonological stages of the plant. The inhibition of α-amylase was more pronounced for P. capitata harvested from P. guajava, decreasing during flowering and fruiting, while inhibition of α-glucosidase was not influenced by the phenological stage and the host of the plant. The α-amylase inhibitors were better extracted by ethyl acetate and those of α-glucosidase by ethanol or methanol. The phenolic contents and antioxidant properties of the extracts were influenced by the phenological stage of P. capitata and its hosts. These results suggest that it is preferable to harvest P. capitata during flowering or during fruiting stages on any host. None of the used solvents permitted an optimal extraction of active principles form P. capitata, suggesting that the mixture of solvents must be considered in further studies.

Dietary Cameroonian Plants Exhibit Anti-Inflammatory Activity in Human Gastric Epithelial Cells.

In Cameroon, local plants are traditionally used as remedies for a variety of ailments. In this regard, several papers report health benefits of Cameroonian spices, which include antioxidant and anti-microbial properties, whereas gastric anti-inflammatory activities have never been previously considered. The present study investigates the antioxidant and anti-inflammatory activities of hydro-alcoholic extracts of eleven Cameroonian spices in gastric epithelial cells (AGS and GES-1 cells). The extracts showed antioxidant properties in a cell-free system and reduced H2O2-induced ROS generation in gastric epithelial cells. After preliminary screening on TNFα-induced NF-κB driven transcription, six extracts from Xylopia parviflora, Xylopia aethiopica, Tetrapleura tetraptera, Dichrostachys glomerata, Aframomum melegueta, and Aframomum citratum were selected for further studies focusing on the anti-inflammatory activity. The extracts reduced the expression of some NF-κB-dependent pro-inflammatory mediators strictly involved in the gastric inflammatory process, such as IL-8, IL-6, and enzymes such as PTGS2 (COX-2), without affecting PTGS1 (COX-1). In conclusion, the selected extracts decreased pro-inflammatory markers by inhibiting the NF-κB signaling in gastric cells, justifying, in part, the traditional use of these spices. Other molecular mechanisms cannot be excluded, and further studies are needed to better clarify their biological activities at the gastric level.

Hydroethanolic plant extracts from Cameroon positively modulate enzymes relevant to carbohydrate/lipid digestion and cardio-metabolic diseases.

Cardiovascular diseases are the greatest cause of death globally and are frequently associated with type 2 diabetes mellitus and metabolic syndrome, a condition including visceral obesity, hypertension, elevated triglycerides and low HDL cholesterol and hyperglycaemia. Several medicinal plants, including spices, are used in Cameroon as herbal medicines and are traditionally employed for the treatment of several ailments such as diabetes and related diseases. In this study, we chemically characterized eleven Cameroonian spice extracts and evaluated their effects on some enzyme activities relevant to carbohydrate and lipid digestion and cardio-metabolic diseases. Hydroethanolic spice extracts were characterized by GC-MS analysis and screened for their ability to modulate the activity of α-glucosidase, α-amylase, pancreatic lipase, 3-hydroxy-3-methylglutaryl-coenzyme A reductase and angiotensin-converting enzyme (ACE). Among the spice extracts tested, those from Xylopia parviflora showed the widest inhibitory spectrum, with a relevant effect on all enzyme activities. Dichrostachys glomerata and Aframomum citratum extracts were more selective. The selected and strong activity of some plants, such as that of Aframomum citratum on pancreatic lipase and that of Xylopia aethiopica on ACE, suggests their specific use in obesity and hypertension, respectively. Chemical analysis indicated that for some spice extracts such as Xylopia parviflora and Aframomum citratum their secondary metabolites (chlorogenic acid, pimaric acid, and catechin and its derivatives) could potentially justify the biological properties observed. Our findings clearly show significant inhibition of cardio-metabolic enzymes by hydroethanolic Cameroonian spice extracts, suggesting the potential usefulness of nutraceuticals derived from these plants to develop novel management strategies for obesity and diabetes complications.

Curative effects of Distemonanthus benthamianus Baillon. Trunk-bark extracts on enteropathogenic Escherichia coli 31-induced diarrhea in rats.

Background Distemonanthus benthamianus is used in the Western part of Cameroon to treat diarrheal episodes and infections. This study assessed its trunk-bark extracts activity against enteropathogenic Escherichia coli 31 (EPEC 31)-induced diarrhea in rats. Methods Aqueous and methanolic extracts were analyzed through high-performance liquid chromatography (HPLC). In vitro minimum inhibitory and bactericidal concentrations (MICs/MBCs) were evaluated on Enterococcus faecalis (ATCC 10,541), E. coli (ATCC 6539), Klebsiella pneumoniae (ATCC 13,883), Salmonella typhi (ATCC 6539) strains and on Proteus mirabilis, Pseudomonas aeruginosa (PA 01) and Shigella flexneri isolates using the microdilution method. Diarrhea was induced by inoculating rats with EPEC 31 (1.5 × 108 CFU/mL; p.o). Serum transaminases level assay and enzyme-linked immunosorbent assay (ELISA) for cytokines determination were performed. Hematoxylin-eosin (H-E) staining was used for intestinal tissue analysis. Results HPLC fingerprints of extracts showed presence of gallic acid and other unidentified compounds. The lowest MIC of 256 µg/mL was obtained with methanolic extract. At 100 mg/kg, both extracts significantly (p<0.001) inhibited diarrhea, with the methanolic extract being the most active. In addition, the methanolic extract significantly (p<0.001) increased the relative mass of the liver compared to negative control (Tween-DMSO 8%). The aqueous extract (100 mg/kg) significantly (p<0.01) increased alanine aminotransferase (ALT) serum concentration; while the methanolic extract (100 mg/kg) exhibited similar effect over aspartate aminotransferase (AST). At 50 and 100 mg/kg, the methanolic extract significantly (p<0.05 and p<0.01) decreased the Interleukin-1ß (IL-1ß) serum level, compared to negative control (Tween-DMSO 8%). Serum level of tumor necrosis factor alpha (TNF-α) significantly (p<0.001) decreased with 100 mg/kg of aqueous extract and all doses of methanolic extract. Inhibition of inflammatory cells tissue infiltration and epithelial regeneration was highly noticed in the ileum and colon of extracts-treated rats than in ciprofloxacin-treated animals. Conclusion These findings suggest that D. benthamianus trunk-bark extracts displayed therapeutic effects against infectious diarrhea in rats.

Effect of fractioning on antibacterial activity of n-butanol fraction from Enantia chlorantha stem bark methanol extract.

BACKGROUND: Enantia chlorantha is a plant belonging to Annonaceae Family. The Barks and leaves are used traditionally to treat infectious diseases. Earlier studies highlighted the antibacterial activity of stem barks methanol extract. This study is thus aimed at investigating the effect of fractionation on antibacterial activity of its n-butanol fraction. METHODS: The extract of E. chlorantha stem barks was obtained by maceration in methanol and then subjected to a liquid/liquid partition by successive depletion with solvents of increasing polarity. The n-butanol fraction was fractionated by adsorption chromatography on silica gel. A product was isolated from the dichloromethane/methanol (2%) fraction and the structure was determined on the basis of spectroscopic data; Proton Nuclear Magnetic Resonance (1H NMR), Carbon-13 Nuclear Magnetic Resonance (13C NMR), Heteronuclear Multiple Bond Correlation (HMBC), H-correlation spectroscopy (H-COSY), attached proton test (APT), heteronuclear multiple quantum coherence (HSQC). The antibacterial activity was evaluated by broth microdilution method against six reference strains and eight clinical bacterial strains. RESULTS: The n-butanol fraction was found to be active with MIC values ranging from 32 to 256 µg/mL. The FA sub-fraction was more efficient among the eight sub-fractions, the n-butanol fraction and comparable to Chloramphenicol used as reference antibiotic. The product obtained was elucidated as palmitin. The antibacterial activity of the latter was comparable to that of Chloramphenicol on one reference strain and 4 of the 6 clinical strains. CONCLUSION: The FA sub-fraction had better antibacterial activity than the n-butanol fraction and other sub-fractions, and possibly palmitin was the active substance responsible for the antibacterial activity of E. chlorantha.

Anticancer Properties of Graviola (Annona muricata): A Comprehensive Mechanistic Review.

Graviola (Annona muricata) is a small deciduous tropical evergreen fruit tree, belonging to the Annonaceae family, and is widely grown and distributed in tropical and subtropical regions around the world. The aerial parts of graviola have several functions: the fruits have been widely used as food confectionaries, while several preparations, especially decoctions of the bark, fruits, leaves, pericarp, seeds, and roots, have been extensively used in traditional medicine to treat multiple ailments including cancers by local communities in tropical Africa and South America. The reported therapeutic benefits of graviola against various human tumors and disease agents in in vitro culture and preclinical animal model systems are typically tested for their ability to specifically target the disease, while exerting little or no effect on normal cell viability. Over 212 phytochemical ingredients have been reported in graviola extracts prepared from different plant parts. The specific bioactive constituents responsible for the major anticancer, antioxidant, anti-inflammatory, antimicrobial, and other health benefits of graviola include different classes of annonaceous acetogenins (metabolites and products of the polyketide pathway), alkaloids, flavonoids, sterols, and others. This review summarizes the current understanding of the anticancer effects of A. muricata and its constituents on diverse cancer types and disease states, as well as efficacy and safety concerns. It also includes discussion of our current understanding of possible mechanisms of action, with the hope of further stimulating the development of improved and affordable therapies for a variety of ailments.

Effect of Fractioning on Antibacterial Activity of Enantia chlorantha Oliver (Annonaceae) Methanol Extract and Mode of Action.

Infectious diseases caused by bacteria constitute the main cause of morbidity and mortality throughout the world and mainly in developing countries. In this work, the influence of fractioning and the mode of action of stem barks methanol extract of Enantia chlorantha were investigated. The aim was to optimize the antibacterial activity of the methanol extract. The extract was prepared by maceration of barks powder in methanol. Fractioning was done using increasing solvents polarity. Standard phytochemical methods were used for phytochemical screening. Minimum Inhibitory Concentrations (MIC) and Minimum Bactericidal Concentration (MBC) of the methanol extract and fractions were determined using broth microdilution method. The studied mode of action of both methanol extract and n-butanol fraction included antibiofilm activity, H+-ATPase-mediated proton pumping assay, salt tolerance, and cells cycle. The methanol extract of E. chlorantha stem barks was found to be active on all the bacteria tested (32 ≤ MIC ≤ 512 µg/mL), its activity being significant (MIC < 100 µg/ml) out of 5 of the 28 clinical isolates used. Salmonella enterica serovar paratyphi A was the most sensitive (32 µg/mL). Compared to the extract and other fractions, the n-butanol fraction was found to be more active (32 ≤ MIC ≤ 256). Significant antibacterial activity of this fraction was observed out of 10 of the 28 bacterial isolates and 3 out of 7 bacterial strains. Lowest MIC values (32 µg/ml) of this fraction were obtained with Escherichia coli (136), Pseudomonas aeruginosa (CIP 76110), and Salmonella enterica serovar typhi 9. The methanol extract of E. chlorantha and its n-butanol fraction revealed several modes of action including the prolongation of the latency phase of the bacterial growth, the inhibition of the pump with protons H+ - ATPases bacterial, the loss of the salt tolerance of the Staphylococcus aureus, and inhibition of the formation of the bacterial biofilm. The present results showed that the n-butanol fraction of the methanol stem barks extract of E. chlorantha possess the essential antibacterial components and could best be used to fight against bacterial infections as compared to methanol extract.

Costus afer Protects Cardio-, Hepato-, and Reno-Antioxidant Status in Streptozotocin-Intoxicated Wistar Rats.

Medicinal plants are efficient modulators of oxidative stress associated with diabetes mellitus. This study evaluated the cardio-, reno-, and hepato-antioxidant status of hydroethanolic extract of Costus afer on streptozotocin-intoxicated diabetic rats. Experimental animals were daily administered with hydroethanolic extract of C. afer by oral intubation for eight weeks (60 days), after which the levels of catalase (CAT), superoxide dismutase (SOD), glutathione (GSH), and lipid peroxidation marker (MDA) were evaluated in the heart, liver, and kidney homogenates. Plasma biochemical parameters such as aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP), lactate dehydrogenase (LDH), total protein, creatinine, and urea were determined. Meanwhile, parts of the heart, kidneys, and liver were histopathologically examined. Streptozotocin administration induced toxicity in the cardiac, hepatic, and renal tissues by stimulating significant increases (p<0.05) in the levels of CAT and SOD, GSH, and MDA. Similarly, significant increases (P<0.05) in the levels of ALT, AST, urea, and total protein were observed in streptozotocin treated rats, whereas decreases were observed in the levels of ALP, LDH, and creatinine. Following the treatments with C. afer hydroethanolic extract prevented the effect of streptozotocin by maintaining the tissue antioxidant status (CAT, SOD, GSH, and MDA) and the plasma biochemical parameters (AST, ALT, ALP, LDH, creatinine, and urea) towards the normal ranges. The histopathological examination revealed hepatovascular congestion and leucocyte infiltration as well as renovascular congestion, glomerulosclerosis, and tubular clarification in the untreated diabetic control and their absence in the group of animals treated with a high dose of C. afer extract. The findings of the present investigation suggest that C. afer possesses antioxidant activities capable of regulating drug induced tissue damage.

Antibacterial and antibiotic resistance modulatory activities of leaves and bark extracts of Recinodindron heudelotii (Euphorbiaceae) against multidrug-resistant Gram-negative bacteria.

BACKGROUND: Recinodindron heudelotii (Euphorbiaceae) is a plant used in Africa, particularly in Cameroon to treat various ailments including bacterial infections. In this study, we evaluated the extracts of the leaves (RHL) and bark (RHB) of R. heudelotii for their antibacterial and antibiotic resistance modulating activities against 29 Gram-negative bacteria, including multidrug-resistant (MDR) phenotypes. METHODS: The broth micro-dilution assay was used to evaluate the antibacterial activity, and the antibiotic resistance modulating effects of the plant extracts. RESULTS: RHL displayed the most important spectrum of activity with minimal inhibitory concentrations (MICs) values ranging from 256 to 1024 µg/mL against 75.86% of the 29 tested bacteria strains while RHB was not active. RHL also showed killing effects with minimal bactericidal concentrations (MBCs) ranging from 256 to 1024 µg/mL. The activities of tetracycline and kanamycin associated with RHL were improved on 88.89% and 77.78% of the tested MDR bacteria, at MIC/2 at MIC/4 respectively, with 2 to 16-folds decreasing of MIC. This suggests the antibiotic resistance modulating effects of these antibiotics. CONCLUSION: The present study provides data indicating a possible use of the leaves extract of Recinodindron heudelotii alone or in association with common antibiotics in the fight against bacterial infections including those involving MDR bacteria.

Antibacterial and antioxidant properties of crude extract, fractions and compounds from the stem bark of Polyscias fulva Hiern (Araliaceae).

BACKGROUND: In our previous work, the dichloromethane-methanol (1:1 v/v) extract, fractions and isolated compounds from Polyscias fulva stem bark showed interesting antifungal activity. As a continuity of that work, this study aimed to bring out complementary informations about the antimicrobial properties of P. fulva stem bark that may be useful in the standardization of phytomedicine from this plant. METHODS: The antibacterial activities of the crude extract, fractions (n-hexane, ethyl acetate, n-butanol and residual) and isolated compounds from Polyscias fulva stem bark were assayed by broth microdilution techniques. Their antioxidant activity were evaluated using 2,2-diphenyl-1-picrylhydrazyl (DPPH), pyrogallol (superoxide anion) and ß-carotene - linoleic acid assays. RESULTS: The crude extract presented antibacterial activities against S. typhi (ATCC 6539), E. aerogenes (ATCC 13045), P. aeruginosa (PA01) and E. coli (ATCC 10536) with MIC values of 2000 to 8000 µg/ml. The fractionation led the ethyle acetate and n-butanol fractions relatively more active (MIC = 500 to 1000 µg/ml) as compared to the crude extract. ß-sitosterol and 3-O-α-L- arabinopyranosyl-hederagenin were the most active compounds on the tested bacteria with MIC values ranging from 6.25 to 100 µg/ml. The most sensitive was P. aeruginosa (PA01) on which all the tested compounds were active with MICs ranging from 6.25 to 400 µg/ml. Among all the tested substances, the crude extract (RSa50 = 84.86 µg/ml) and the methyl atrarate (RSa50 = 14.77 µg/ml), showed the highest scavenging activities against DPPH free radicals and those arising from the oxidation of the linoleic acid respectively. CONCLUSION: From this study, the results obtained reveal that the stem bark of P. fulva possesses antibacterial and antioxidant activities. It may then be useful in the development of an antimicrobial phytomedicine with a large spectrum of actvity endowed with antioxidant properties which can be standardised based on the isolated compounds.

Iridoids from Canthium subcordatum iso-butanol fraction with potent biological activities.

BACKGROUND: The continuous emergence of multi-drug-resistant bacteria drastically reduces the efficacy of antibiotic armory and, consequently, increases the frequency of therapeutic failure. The discovery of new antibacterial drugs is an urgent need. The present study reports the antibacterial and antioxidant activities of the methanol extract, fractions and iridoids from Canthium subcordatum, a plant traditionally used as antidiabetic, anti-inflammatory, and antimicrobial. METHODS: Broth microdilution assay was used to determine minimum inhibitory concentrations (MICs) and minimum bactericidal concentrations (MBCs) of extracts and iridoids against Staphylococcus aureus, Vibrio cholerae and Shigella flexneri. Antioxidant activity was evaluated using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and gallic acid equivalent antioxidant capacity (GAEAC) assays. The samples were also tested for their cytotoxicity against human red blood cells (RBC). RESULTS: The methanol extract, hexane, ethyl acetate and iso-butanol fractions from C. subcordatum fruits displayed different degrees of antioxidant (EC50 = 62.83-70.17 µg/ml; GAEAC = 45.63-58.23 µg/ml) and antibacterial (MIC = 128-512 µg/ml) activities. Canthiumoside 1(1) and linearin (7) were the most active antioxidant (EC50 = 1.12-2.03 µg/ml; GAEAC = 79.82-92.35 µg/ml) and antibacterial (MIC = 8-64 µg/ml) compounds while the most sensitive bacterium was Staphylococcus aureus. The tested samples were non-toxic to normal cells. CONCLUSION: Our results demonstrated that compounds 1 and 7 were potent antibacterial agents and DPPH/ABTS·+ radical scavengers, so they warrant further investigation.

Complex secondary metabolites from Ludwigia leptocarpa with potent antibacterial and antioxidant activities.

Diarrhea continues to be one of the most common causes of morbidity and mortality among infants and children in developing countries. The aim of the present study was to evaluate the antibacterial and antioxidant activities of extracts and compounds from Ludwigia leptocarpa, a plant traditionally used for its vermifugal, anti-dysenteric, and antimicrobial properties. A methanol extract was prepared by maceration of the dried plant and this was successively extracted with ethyl acetate to obtain an EtOAc extract and with n-butanol to obtain an n-BuOH extract. Column chromatography of the EtOAc and n-BuOH extracts was followed by purification of different fractions, leading to the isolation of 10 known compounds. Structures of isolated compounds were assigned on the basis of spectral analysis and by comparison to structures of compounds described in the literature. Antioxidant activity was evaluated using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and gallic acid equivalent antioxidant capacity (GAEAC) assays. Antibacterial activity was assessed with the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) with respect to strains of a Gram-positive bacterium, Staphylococcus aureus (a major cause of community and hospital-associated infection), and Gram-negative multi-drug-resistant bacteria, Vibrio cholerae (a cause of cholera) and Shigella flexneri (a cause of shigellosis). All of the extracts showed different degrees of antioxidant and antibacterial activities. 2ß-hydroxyoleanolic acid, (2R,3S,2''S)-3''',4',4''',5,5'',7,7''-heptahydroxy-3,8"-biflavanone, and luteolin-8-C-glucoside displayed the most potent antibacterial and antioxidant properties, and these properties were in some cases equal to or more potent than those of reference drugs. Overall, the present results show that L. leptocarpa has the potential to be a natural source of anti-diarrheal and antioxidant products, so further investigation is warranted.

Anti-Staphylococcus aureus activity of methanol extracts of 12 plants used in Cameroonian folk medicine.

BACKGROUND: The emergence of bacterial infections including those associated with Staphylococcus aureus causes a benefit of interest to medicinal plants as an effective means of control. The present study was designed to investigate the activities of 12 selected Cameroonian medicinal plants against S. aureus isolates. METHODS: The plant extracts were prepared by maceration in methanol at laboratory temperature. Qualitative phytochemical analysis was performed by chemical reaction methods. The broth microdilution method was used to evaluate the activities of plant extracts against 11 S. aureus clinical isolates. RESULTS: Dacryodes edulis was found to have significant antibacterial activity on all the S. aureus isolates (MIC = 64-256 µg/ml). Occimum gratissimum revealed significant inhibitory activity on 9 of the 11 isolates while Commelina erecta and Spilanthes filicaulis revealed similar results on 6 of the 11 clinical isolates. CONCLUSION: The present findings showed that D. eduli, O. gratissimum, C. erecta and S. filicaulis possess interesting inhibitory properties against S. aureus species. These plants could therefore be good candidates to overcome infectious diseases associated with these microorganisms.

Antibacterial activity of ethanolic extract and compounds from fruits of Tectona grandis (Verbenaceae).

BACKGROUND: Well known as teak, Tectona grandis is widely used in African folk medicine for its pharmacological relevance. In Cameroon, this species is a reputed laxative in the Northern Region while in the Western Region, it is used in the treatment of skin diseases and diarrhoea. MATERIALS AND METHODS: Separation and isolation of compounds were performed using different chromatographic methods while their structures were elucidated by spectroscopic techniques including MS and NMR, and by comparison of data with those reported in the literature. Isolated compounds as well as crude ethanol extract were tested for their antibacterial activities using broth micro-dilution method against four Gram negative bacteria strains Escherichia coli (ATCC 8739), Pseudomonas aeruginosa (PA 01), Klebsiella pneumonia (ATCC 11296) and Escherichia aerogenes (ATCC 13048). RESULTS: Three known compounds were isolated, including two quinones and one triterpene. They were identified as tectograndone (1), 6-methyl-1,4-dihydroxyanthraquinone (2), and 2ß-hydroxyursolic acid (3) respectively. Crude ethanol extract showed good activity against the bacteria strains tested with MIC of 64-256 µg/mL. Among the isolated metabolites, 6-methyl-1,4-dihydroxyanthraquinone exhibited a strong activity against Escherichia aerogenes with MIC of 16 µg/mL, while tectograndone showed a moderate activity against Escherichia coli with MIC of 32 µg/mL. The antibacterial screening of the fruits of this plant as well as that of compounds 1 and 2 is reported herein for the first time. CONCLUSION: The research work presented here shows that Tectona grandis fruits possess compounds which could be developed in the treatment of bacterial diseases.