Antimalarial resistance remains one of the main obstacles in the fight against malaria, which continues to be a leading cause of death in Africa. This study aimed to evaluate the antiplasmodial, cytotoxic, and antioxidant properties of the extracts and compounds from the stem bark of Senegalia polyacantha (Willd.) Seigler Ebinger (syn. Acacia polyacantha Willd.). The DCM/MeOH crude extract (SPDM) of S. polyacantha was further extracted with EtOAc (SPEA) and chromatographed, leading twenty-four compounds (1–24) which were all characterized using NMR and MS data. The SPDM, SPEA, and compounds (1–24) were assessed for their in vitro/in silico (PDB Id: 7QC1) antiplasmodial activities against asexual-blood stages of chloroquine-sensitive (3D7) and multiresistant (Dd2) strains of Plasmodium falciparum, as well as for their cytotoxic activities on Vero and RAW 264.7 and antioxidant potential using DPPH, ABTS, and FRAP assays. Compounds 1 and 2 were identified as previously unreported E/Z isomeric mercaptoacrylate derivatives, while compounds 3–24 were known. The antiplasmodial activity ranged from IC50 2.03 to > 50 μg/mL. Compound 17 was the most potent (2.03 μg/mL, 11.3 μM against 3D7; 3.08 μg/mL, 17.1 μM against Dd2), followed by 24 (2.50 μg/mL, 5.38 μM against 3D7; 5.05 μg/mL, 10.9 μM against Dd2). Antioxidant assays showed that 16 and 20 were the most active DPPH scavengers (IC50 9.8 and 9.7 μg/mL, respectively), while 21 exhibited the strongest reducing power (5120 μmol FeSO4/g). Cytotoxicity was low (CC50 56 to > 300 μg/mL), with selectivity indices > 10 for active compounds. Molecular docking against P. falciparum prolyl‑tRNA synthetase (PfProRS) suggested that compounds 4, 5, and 24 may interact with 7QC1 target (− 10.73, − 10.55, and − 7.42 kcal/mol, respectively), while ADME profiling indicated favorable drug‑like properties for 1/2. The tested samples showed limited cytotoxicity against Vero and RAW 264.7 cells for active compounds, and displayed potent antioxidant activities. These preliminary in vitro findings suggest that S. polyacantha stem bark extracts and isolated compounds possess antiplasmodial and antioxidant properties with favorable cytotoxicity profiles, warranting further in vivo studies to evaluate safety and therapeutic potential.
IntroductionBreast cancer killed 665,684 patients globally in 2022 despite government efforts and conventional therapies. The hydro-ethanolic extract of Acacia seyal, a sub-Saharan African ethnomedicinal plant, showed moderate cytotoxicity, significant anti-migration and in vivo preventive effects against breast cancer cells. The aim of this study was to propose an improved traditional extract and to evaluate its efficacy and potential mechanism of action.MethodsTo achieve this, A. seyal hydro-ethanolic extract (ASHE) was fractionated in polyphenol-enriched (ASpo), polysaccharides (ASsu) and residue (ASre) fractions. Fractions along with the crude extract were tested for their ability to inhibit cell growth (MTT) and proliferation (CCK-8). The promising fraction (ASpo) was further investigated on clone formation, caspase-3, wound healing, chemotaxis and cell adhesion to understand its underlying mechanisms of action. Moreover, ASpo at 18.75 and 37.5 mg/kg, p.o compared to standard drugs (tamoxifen and letrozole) and control (distilled water) were assessed in a 20-week preventive study of DMBA (50 mg/kg, s.c)-induced breast cancer by considering tumor incidence, tumor volume, organ mass, histopathological, hematological, antioxidant and anti-inflammatory/immunomodulatory markers.ResultsAmong the 3 fractions, ASpo compared to control, inhibited (p < 0.01) MDA-MB 231 cells growth, proliferation and clone formation at 50 μg/mL. It increased caspase-3 and inhibited cell migration and invasion (p < 0.01) with increase (p < 0.01) adherence to collagen and fibronectin. In vivo, comparable to reference drugs, ASpo reduced tumor incidence (50%), and tumor volume from 7827.30 mm3 (adenocarcinoma SBRIII, 10% lymphocytes infiltration) in DMBA to 804.32 mm3 (adenocarcinoma SBRII, 30% lymphocytes infiltration) at 37.5 mg/kg. It increased femur and thymus’mass, lymphocytes and monocyte levels (p < 0.001) in serum, reduced (p < 0.001) TNF-α, IL-6, IL-12, EGF, nitrites levels whereas increased SOD, catalase and major IFN-γ cytokine (p < 0.001). ASpo additionally showed a safety profile on toxicity organs.ConclusionOverall, ASpo mainly contributed to anti-breast cancer activities of total crude extract and involved immunomodulatory effects to consider with optimized bioactivity to further investigate it as a promising natural and inexpensive alternative to costly and efficient current immunotherapy.
Chemical and biological studies of the n-hexane fraction of the stem bark extract of Strombosia grandifolia led to the isolation and characterisation of one undescribed lup-20(29)-ene derivative named, grandifolione (1), alongside with nine known compounds 2-10. These compounds were isolated from this species for the first time. Their structures were elucidated based on NMR and MS spectroscopic data as well as by comparison with existing data of the literature. The antibacterial activity of the crude extract (CH2Cl2/MeOH 1:1), the n-hexane fraction and some of the isolated compounds were evaluated against ten bacterial strains including gram positive (Staphylococcus aureus) and gram negative (Acinetobacter baumannii, Pseudomonas aeruginosa, Escherichia coli, Shigella flexneri, Klebsiella pneumoniae and Salmonella typhimirium). The crude extract (CH2Cl2/MeOH 1:1) exhibited moderate activity against S. aureus (ATCC12600 and ATCC700698), P. aeruginosa HM801 and S. typhimirium with MIC values of 125, 125, 250 and 500 µg/mL respectively. The n-hexane fraction exhibited moderate activity against P. aeruginosa NR-48982 and S. aureus NR-46003 with MIC values of 250 µg/mL for both. Sub-fraction F3 exhibited significant activity against S. aureus (ATCC12600 and ATCC700698) and P. aeruginosa HM801 with MIC values of 62.5 µg/mL. Lupeol (3) demonstrated moderate activity against A. baumannii NR-41897, S. aureus ATCC12600, ATCC700698 and NR-46003 with MIC values of 25, 15.6, 31.2 and 25 µg/mL respectively.
This study aimed to investigate the chemical constituents of the trunk bark of Xylopia quintasii and evaluate the antibacterial potential of its isolated terpenoids, with a focus on the structural characterisation and polymorphism of (−)-rhinocerotinoic acid (1). The petroleum ether fraction of the methanol extract was subjected to chromatographic separation, leading to the isolation of eight terpenoids, including six diterpenoids and two lupane-type triterpenoids. Single-crystal X-ray diffraction was employed to determine the molecular framework and relative stereochemistry of (−)-rhinocerotinoic acid (1). Optical rotation, Flack parameter analysis, and complementary spectroscopic techniques (CD, VCD, or chiral HPLC) were considered to assess stereochemistry. Antibacterial activity was evaluated against Gram-negative enterobacteria, and molecular docking was performed on the MurA enzyme to explore potential mechanisms. Among the diterpenoids, (−)-rhinocerotinoic acid (1) was identified as a labdane-type compound, crystallising in a triclinic P1 system representing a new polymorph. Optical rotation ( [ ]_D^24 −2.04, c = 0.2, MeOH) and Flack parameter (0.20) indicated that the absolute configuration could not be unambiguously assigned. Several diterpenoids exhibited higher antibacterial activity than the crude extract, with 3β-hydroxy-copalic acid (3) showing the most potent effect (MIC = 50 µg/mL against E. coli). Docking studies suggested potential interactions with the MurA catalytic site, although predictions for compound 1 were less reliable (RMSD = 4.48 Å). Xylopia quintasii trunk bark contains chemically diverse labdane- and kaurane-type diterpenoids. The identification of a new polymorphic form of (−)-rhinocerotinoic acid (1), together with the selective antibacterial activity of certain diterpenoids, highlights their chemotaxonomic significance and potential as scaffolds for further pharmacological studies.
From the leaves of Coula edulis, fourteen compounds were isolated and identified: D-mannitol (1), a mixture of β-sitosterol (2) and stigmasterol (3), α-amyrin (4), betulin (5), lupeol (6), lupenone (7), betulinic acid (8), taraxerol (9), 3β-(E)-coumaroyltaraxerol (10), 3β-(Z)-coumaroyltaraxerol (11), ursolic acid (12), stigmasterol 3-O-β-D-glucoside (13), and β-sitosterol 3-O-β-D-glucoside (14). These compounds were analysed through NMR spectroscopy (both 1D and 2D) and by comparing them to previously published data. Compounds 1, 4, 5, and 7-9 have been identified from this species for the first time. Antibacterial activity was assessed, with compound 12 displaying the best efficacy against Staphylococcus aureus (MIC: 15.6 μg/mL). Molecular docking of compound 12 led to twenty lead compounds, among which 12 F displayed the highest score (-10.1 kcal/mol). Most lead compounds showed better scores compared to Vancomycin (-8.8 kcal/mol). Biovia Discovery Studio analysis reveals lead compounds interacting with CASTp-predicted active pocket amino acids.
Phytochemical analysis of the dichloromethane-methanol (1:1) extract from Sclerocarya birrea inner bark led to the identification of three compounds: a novel glycoside, 3α-sorbithoxyglucose (1), and two known compounds, retusasterol (2) and β-sitosterol-3-O-D-glycoside (3), isolated for the first time from this plant. Structural elucidation via NMR confirmed their identities. Cytotoxicity studies against MCF7 breast cancer and DU145, PC3, LNCaP prostate cancer cell lines revealed that compounds 1 and 2 lacked inhibitory effects on cell proliferation, while retusasterol exhibited cytotoxicity with CC50 values of 38 μg/mL (DU145), 40 μg/mL (PC3), and 32 μg/mL (LNCaP). However, further analysis indicated that retusasterol promoted tumour cell proliferation. Antimicrobial screening of 3α-sorbithoxyglucose against Bacillus subtilis, Enterococcus faecalis, Staphylococcus epidermidis, Staphylococcus aureus, Mycobacterium smegmatis, Enterobacter cloacae, Proteus vulgaris, Klebsiella oxytoca, Klebsiella pneumoniae, Proteus mirabilis, Escherichia coli, and Pseudomonas aeruginosa revealed MIC values of 15.625-250 μg/mL, suggesting potential as an antimicrobial agent compared to standard antibiotics.
Malaria is a significant concern due to the emergence of artemisinin-resistant parasites. This study aims to unveil the selective inhibitory potential of extracts and derivatives of some Niger's plants against Plasmodium falciparum. Plant extracts were screened on chloroquine-sensitive (Pf3D7) and multidrug-resistant (PfDd2) P. falciparum strains using the SYBR Green method, followed by bio-guided fractionation of active extracts. Bio-guided method was used for the isolation. Resazurin-based and hemoglobin quantification assays were used to assess the selectivity on normal RAW cells and erythrocytes, respectively. Among the 27 extracts, five exhibited pronounced activity (IC50 < 5 µg/mL) against multidrug-resistant (PfDd2) and three against sensitive (Pf3D7) strains of P. falciparum. The methanolic extract from Phyllanthus pentandrus displayed the most promising activity the most active on both strains (IC50PfDd2 = 1.85 µg/mL and IC50Pf3D7 = 4.25 µg/mL). Its fractionation led to five fractions, among which the ethyl acetate fraction was the most active (IC50PfDd2 = 3.10 µg/mL). Four compounds were isolated from the ethyl acetate fraction: kaempferol, quercetin, gallic acid, and quercetin-3-O-rutinoside. Active extracts and fractions showed good selectivity on normal RAW cells and erythrocytes. This study validates the medicinal use of Niger ethnomedicine for the treatment of malaria.
Prostate cancer (PC) therapy is fraught with various limitations, underscoring the urgency for new therapeutic approaches. Cola lateritia K. Schum is a medicinal plant traditionally used against prostate ailments. This finding aimed to assess Cola lateritia isolates' cytotoxic potential and investigate their potential underlying mechanisms. Through column chromatography, the C. lateritia twigs dichloromethane-methanol extract of was fractionated, yielding eleven known compounds. The later were subsequently tested in cell growth, cell proliferation and/or cell migration/invasion. Among these, compounds (3) and (4) exhibited substantial, concentration-driven inhibition of cell growth [DU145 (CC50 of 25 and 22 mu g/ml), PC3 (CC50 of 22 and 21 mu g/ ml), and LNCaP (CC50 of 17 and 18 mu g/ml), respectively], cell proliferation (DU145 cells), and the formation of cell clones (DU145 cells). These compounds also induced an increased proportion of apoptotic cells at 2.5 and 10 mu g/ml in DU145 ( 25%) and LNCaP ( 35%) cells, as well as an increment in the G0/G1 phase arrested cells versus control. Both compounds (3) and (4) demonstrated an anti-migratory effect, decreased collagen and fibronectin cell adhesion. Compound (3) down-regulated proteins such as cdk1, cdk2, pcdk2, cyclin A, Bcl-2, and vimentin, while concurrently up-regulating p19, p27, p53, Bax, caspase-3, and E-cad proteins. Additionally, it elevated ,B-1 and ,B-4 integrins at 2.5 and 10 mu g/ml concentrations. The anticancer potential of Cola lateritia is attributed to oleanic acid (3) and maslinic acid (4), which exhibit the potential to impede cell growth by initiating the intrinsic apoptosis pathway and exert an anti-migratory impact. (c) 2025 SAAB. Published by Elsevier B.V. All rights are reserved, including those for text and data mining, AI training, and similar technologies.
The aim of this study was to evaluate the influence of fermentation, variety and legume incorporation on the structural properties of cassava starch granules. It appears that, there was a surface degradation of the granules characterised by an increase in the OH group and a decrease in the C-H, C-C, H-O-H groups and crystallinity of the starch responsible for the bread-making ability on the 30th day of fermentation for varieties 96/1414 and YARA, and day 25th for variety TME15. In addition, there was a decrease in crystallinity and an increase in C-H, -CH2/-CH3 groups, as well as the appearance of C=O groups with the incorporation of legumes. This study suggests that variety, fermentation, solar drying, and the incorporation of legumes influence the structural, morphological, rheological, and bread-making properties of cassava starch.
Gluten intolerance, as well as the scarcity of wheat flour in some parts of the world, has prompted the development of gluten-free bread. Gluten-free bread, on the other hand, results in a low specific volume and to remedy this, the use of hydrocolloids and bases has proved to be very successful. The current study aims to determine the optimal proportions of Triumffeta pentendra gum extract and bicarbonate in the breadmaking of a composite flour based on sour cassava starch, peanut flour, and cowpea flour. A Box Benkhen design was used to achieved this, with the variables being the amount of gum extract, the amount of bicarbonate, and the amount of water. The specific volume and texture properties were evaluated as responses. The specific volume was calculated using standard methods, and the textural properties were determined using a texture analyzer. It appears that the incorporation of gums extract, bicarbonate, and water significantly increased the specific volume. The incorporation rate of gum extract significantly increases the hardness, consistency, and masticability which decreases with the incorporation rate of bicarbonate and water. Cohesion and elasticity, on the other hand, increased with the incorporation rate of bicarbonate and water but decreased with the incorporation of gum extract. The optimal gum extract, bicarbonate, and water proportions are 0.28 g, 1.99 g, and 112.5 ml, respectively. As a result, the specific volume is 1.51cm3/g, the hardness is 38.51(N), the cohesion is 0.88, the consistency is 32.86 (N), the elasticity is 5.57(1/L), and the masticability is 162.35(mj). According to this findings, gum extracts and sodium bicarbonate can be used to improve the quality of gluten-free bread made with sour cassava starch, peanut and cowpea flour.
This research is to investigate the breadmaking ability of three cassava starch varieties (96/1414, TME15, and YARA) grown in Cameroon. To achieve this, starch samples from each variety are collected before and during fermentation to determine chemical, rheological, and bread-making properties. They are analyzed for pH, titratable acidity (TTA), lactic acid (LA), specific volume (SPV), and pasting properties using known method; These parameters are used to perform a principal component analysis (PCA). The morphological characteristics are studied by scanning electron microscope (SEM). Result shows that, there is a decrease in pH (6.21-3.8) with an increase in TTA (0.34-7.05) and LA (0.15-6.46) with fermentation time. In parallel, a decrease of pasting properties and an increase in SPV (1.15-2.82 cm(3) g(-1)) are observed. The PCA surrounds 96/1414 day 30, YARA day 30, and TME15 day 25 alpha 30 as the best samples, and the SEM shows a superficial degradation of the granules after fermentation. Thus, this study suggests that the optimal sour cassava starch for bread-making can be obtained from 96/1414 day 30, TME15 day 25 alpha 30, and YARA day 30. The variety 96/1414 appears to have the best bread-making ability while TME15 appears to be most suitable for short fermentation time.
Diabetes causes many deaths around the world, making the search for treatments a real challenge. Plant secondary metabolites are promising candidates because they act as scaffolds in biological processes. This study investigates anti-hyperglycaemic effect of two terpenoids isolated from Coula edulis and in silico study of their potential inhibitors on α-amylase and dipeptidypeptidase 4. After extraction and isolation of the two terpenoids, their structures were characterized using 1D and 2D NMR spectroscopic techniques. Subsequently the anti-hyperglycemic effect was achieved following an overload of starch on the one hand and glucose on the other hand in normoglycemic rats. Each isolated terpenoids was tested at a dose of 3 mg/kg.bw, the same for the reference compounds (Acarbose and glibenclamide). Conformational site analysis and docking parameters such as binding energy, inhibition constant, interaction profiles with diabetes target residues (α-amylase and dipeptidypeptidase 4) were determined using AutoDock 4.2 and Discovery Studio visualizer. The results showed that the terpenoids isolated from coula edulis were Taraxerol and 3β-(Z)-coumaroyltaraxerol, each of its two terpenoids considerably decreased the blood sugar levels in rats after overloading of starch and glucose solutions respectively. Their effects were similar to the reference drugs. Furthermore, the in-silico approach showed that these compounds have good docking scores with α-amylase and with DPP4. Taraxerol exhibited a docking score more than three times than the acarbose docking score. Only 3β-(Z)-coumaroyltaraxerol reacts with at least one amino acid of the α-amylase catalytic triad (Asp 300). Both interact with histidine (His 740) of the DPP4 catalytic triad. In view of this results, taraxerol and 3β-(Z)-coumaroyltaraxerol have anti-hyperglycemic effects and are good candidates for the development of new multitarget antidiabetics. Keywords: Coula edulis, RMN 1D and 2D, tarxerol, 3β-(Z)-coumaroyltaraxerol and Anti-hyperglycemia
This title compound, C20H26O2, was isolated from the benzene fraction of the stem bark of Staudtia kamerunensis Warb. (Myristicaceae) using column chromatography techniques over silica gel. The compound was fully characterized by single-crystal X-ray diffraction, one and two-dimensional NMR spectroscopy, IR and MS spectrometry. The compound has two fused cyclohexane rings attached to a benzene ring, with a carboxylic acid on C-4. This cyclohexene ring has a chair conformation while the other adopts a half-chair conformation. The benzene ring is substituted with a propenyl moiety. The structure is characterized by intermolecular O—H...O hydrogen bonds, two C—H...O intramolecular hydrogen bonds and two C—H...π interactions. The molecular structure confirms previous studies carried out by spectroscopic techniques.
Flavonoids based on the flavone 1-3 and a biflavanoid 4 with a flavan nucleus were isolated from Beilschmiedia obscura (Stapf). These compounds which include 5- hydroxy - 7,8-dimethoxyflavanone (5), (2 S,4 R)-5, 6,7-trimethoxyflavan-4-ol (6), beilschmieflavonoid B (7), (2 R,3 S)-5,6,7-trimethoxyflavan-3-ol (8), as well as pipyahyine (9), (E,E)-1,6-bis(4-hydroxy-3-methoxyphenyl) hexa-1,5-diene-3,4-dione (10), beta-sitosterol (11), pentadecanoic acid (12), pentadecan-1-ol (13), stearic acid (14) and docosane-1,2,4-triol (15), were evaluated as alpha-glucosidase inhibitors. The most abundant compound 5, was structurally modified by acetylation to compound 16 and NaBH4 reduction to compound 17 which represent two new derivatives of this compound class. These compounds 5-10, 16-17 including kaempferol 18, and epicatechin 19 were screened for alpha-glucosidase from Bacillus stearothermophyllus and showed good inhibitory activity with IC50 values = (30.55 +/- 0.12, 31.8 +/- 0.12, 32.47 +/- 0.17, 46.53 +/- 0.16, 36.43 +/- 0.12, 33, 48 +/- 0,12, 32.63 +/- 0.11 and 43.31 +/- 0.12 mu M respectively) compared to acarbose (IC50 = 63.77 +/- 0.08 mu M) as reference drug. Molecular docking and SAR studies further confirmed the plausible binding interactions between the flavonoids and the enzyme alpha-glucosidase. The results show that these compounds bind effectively to the active site of the protein X-ray structure 3wy1, which is in accordance of the observed alpha-glucosidase inhibitory activity.
Ethnopharmacological relevance: Prostate cancer remains a significant burden in low- and middle-income countries and the second leading cause of death around the world. Spices used in daily cuisine contain interesting phytochemical components capable of helping prevent and cure cancer. Aim: This study aims to give sufficient phytochemical information on two understudied species, Staudtia kamerunensis Warb. (Myristicaceae) and Hypodaphnis zenkeri Engl. Stapf. (Lauraceae), and to study their cytotoxicity against prostate cancer cells in its early form and when they have developed metastasis. Materials and methods: To reach this goal, normal procedures for phytochemical analysis were followed; these include collection, drying, crushing and extraction of plant materials using organic solvents. GC-MS (Gas chromatography- Mass Spectrometry) was used to evaluate the volatile phytochemicals contained in the extracts, and open-column chromatography was used to isolate the pure compounds used in this study. A bio-guided exploration of Hypodaphnis zenkeri (Lauraceae) (leaves, seeds, stems) guided us in selecting the extract for further analysis. An established MTT assay was used to measure cell proliferation. Three prostate cancer cell lines were considered in this study, DU145 and PC3, human androgens-independent prostate carcinoma cells and LNCaP, which are cells derived from metastasis of a human prostate and respond to androgens, oestrogens and progestins. The eight compounds isolated were characterized using HREIMS, 1D and 2D NMR. Results: Among the three extracts from Hypodaphnis zenkeri, considered for biological testing, the leaf extract displayed better activities with a CC50 of 180 mu g/mL against DU 145 cells, 184 mu g/mL against PC3 cells and 194 mu g/mL against LNCaP cells. These results were justified when GC-MS analysis of the different extracts was performed. Fifty compounds were identified from the leaves, representing 96.06% of the volatile components, with most displaying anticancer activities or activities against vectors favorizing cancer growth (inflammation, etc.). An attempt to isolate the active principle responsible for the cancer activity led to the isolation of five pure compounds, namely Eicosane [1], Nonacos-1-ene [2], Palmitic acid [3], Glucoside Stigmasterol [4] and Butane-1,2,3,4-tetraol [5]. Eicosane was identified as being responsible in part for the observed activity, even though it exhibited weak cytotoxicity with the lowest CC50 equal to 30 mu g/mL against DU 145 cells. Staudtia kamerunensis sap was investigated in our previous studies with the isolation of Oleanan-12-ene-2 alpha,3 beta -diol [6] and 2 alpha, 3 beta -dihydroxylup-20-ene [7] among the major components, with significant antibacterial properties. Oleanan-12-ene-2 alpha,3 beta -diol [7] in this study displayed a CC50 of 20 mu g/mL against DU145 cells, 22 mu g/mL against PC3 cells, 18 mu g/mL against LNCaP cells, and 32 mu g/mL in HMEC affording a selectivity index >2. Contrary to what was observed in our previous study, the activity of Oleanan-12-ene-2 alpha,3 beta -diol was lost in the presence of 2 alpha, 3 beta -dihydroxylup-20-ene. Conclusion: the cytotoxic effect of extract from Staudtia and Hypodaphnis genera and pure isolates are here reported for the first time, as well as the pure isolates. These studies exhibit the cytotoxic potential of two traditional African spices and, more specifically, Oleanan-12-ene-2 alpha,3 beta -diol and eicosane, isolated from these plant species.
We present the results of the analysis of 2,2,6,6-tetramethyl-4-oxo-piperidinium nitrate isolated from the stem bark of Vitex doniana, a tree growing in Nigeria. The low-temperature molecular structure comprises one 2,2,6,6-tetramethyl-4-oxopiperidinium cation and one nitrate anion as one molecule in the asymmetric unit. The compound crystallizes in the monoclinic space group P21/n. A portion of the nitrate anion exhibits positional disorder with the main disorder component present 66.253(2) % of the time and the minor disorder component present 33.279(2) % of the time. In comparison with the previously reported room-temperature structure of C9H18N2O4 . The low-temperature structure shows similarity with the piperidinium ring adopting a slightly deformed chair conformation while the nitrate anion is disordered. DFT method was used to complement the experimental study.
Introduction: Mycobacterial infections remain a global problem that demands an urgent solution. Lecaniodiscus cupanioides Planch. ex Benth. is traditionally used as a medicinal plant to treat coughs, skin infections, cancers, sexual dysfunction, and malaria. This study focused on the antimycobacterial activity, cytotoxicity, and isolation of bioactive constituents of L. cupanioides chloroform leaves extract. Methods: Antimycobacterial activity was assessed using the micro-dilution assay. Cytotoxic activity of the plant was evaluated using MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide, a tetrazole) assay. Column chromatography was used to purify the extract. Results: Phytochemical investigation of L. cupanioides resulted in the isolation of three compounds, including eicosene (1), nonadecanol (2), and stigmasterol (3). The isolates 1-3 as well as the column fractions displayed antimycobacterial activity, with minimum inhibitory concentration (MIC) ranging from 0.50 to 1.0 mg/mL. The studied extract, column fractions, and isolated compounds exhibited no cytotoxicity against the human cervical cancer (HeLa) cell line. Conclusion: The current results indicate that L. cupanioides has the potential to be employed in the formulation of herbal products or the development of new drugs against mycobacterial infections. However, more studies should be carried out using normal human cell lines to further unravel plant safety.
Ethnopharmacological relevance: Tetrapleura tetraptera (Schumach. and Thonn.) Taub. (Fabaceae) is a tropical plant that is used in Cameroon pharmacopeia for the treatment of many cancers including prostate cancer (PCa), which is a major cause of men's death worldwide. The objective of this study was to evaluate the anticancer properties as well as underlying mechanisms of isolates from T. tetraptera on DU145, PC3 and LNCaP cancer cell lines.Materials and methods: Eight (8) compounds were purified from T. tetraptera stem bark extract through silica gel column chromatography (CC) and characterized using spectroscopic techniques (1D and 2D NMR), HRESIMS. Cell growth was assessed by a well-characterized MTT assay, while BrdU and clonogenicity assays provided information on the cell proliferation index. Further, the impact of the compounds on cell cycle progression and cell death were performed through Flow cytometry. Cell adhesion, cell migration and chemotaxis along with some proteins of epithelial-mesenchymal transition (EMT) were assayed.Results: Out of the eight (1-8) isolates from T. tetraptera only oleanane-3-O-beta-D-glucoside-2 '-acetamide and aridanin showed potent cell growth arrest with an estimated CC50 of 15, 23, 16 and 17, 26, 16 mu g/mL on DU145, PC3 and LNCaP cells, respectively. A 15% (DU145) and 25% (LNCaP) increase in apoptotic cells induced by oleanane-3-O-beta-D-glucoside-2 '-acetamide and aridanin at 10 mu g/mL were noticed. Oleanane-3-O-beta-D-glucoside-2 '-acetamide and aridanin at 2.5 and 10 mu g/mL reduced the number of cells in S-phase and raised cells in G2/M phase. At the same concentrations, they decreased the number of invading DU145 cells and increased the adherence of DU145 cells to fibronectin and collagen matrix at tested concentrations, accompanied by an increase in integrin beta-1 (10 mu g/mL) and integrin beta-4 (2.5 mu g/mL) expression. Furthermore, a down-regulation of pcdk1, cdk2, Bcl-2, N-Cad, vimentin and cytokeratine 8-18 was noticed while, p19, p27, p53 pAKT, Bax, caspase-3 and E-Cad were up-regulated.Conclusions: This study outlines for the first time, the anticancer ability of compounds oleanane-3-O-beta-D-glucoside-2 '-acetamide (4) and aridanin (6) from Tetrapleura tetraptera and proposes their putative mechanisms of action.
Acacia nilotica Linn is used traditionally in the treatment of various diseases, such as diarrhea, ulcer, dysentery, asthma, inflammation and cancer. The present study aimed at isolation and characterization of a steroidal compound and evaluating the gastroprotective activity of the ethyl acetate portion of A. nilotica seeds in indomethacin-induced ulcer model. Fractionation of the ethyl acetate portion using standard chromatographic techniques led to the isolation of a compound (B2-I) which on further purification and characterisation using physical, chemical and spectral analysis, and by comparison with literature values was identified as stigmasterol. The effect of ethyl acetate portion of A. nilotica on experimentally induced ulcer was dose-dependent with curative ratios of 40%, 60% and 75% at concentrations of 100, 200 and 300 mg/kg body weights respectively. It significantly (P<0.05) decreased free and total acidity and increased the pH of gastric juice with respect to the indomethacin treated group. This justifies the ethnomedicinal use of A. nilotica seed as an antiulcer agent. The study recommends that A. nilotica seeds be evaluated against other ulcer models such as ethanol and stress induced ulcers.
The present work aims to evaluate the influence of varieties and malting conditions on the liquefying and sweetening capacities of germinated flours of two new maize varieties (Atp-Y and Coca-sr). Five (5) factors such as soaking time (18-42 h), vegetable salt concentration (0.5-1.2%), soaking temperature (25-41 degrees C), germination time (80-195 h) and maturation time (17.5-42 h) were used to potentiate the liquefying and sweetening capacities of the two flours. The dehulled flours of the two maize varieties were also used as a substrate for the evaluation of these responses. The optimal flours were then subjected to physicochemical analysis. From these analyses, it follows that the responses were affected (p < 0.05) by the malting conditions, the variety of germinated flours and the variety of substrate flours. Overall, the sprouted flours respectively from the Coca-sr variety showed the highest liquefying (190 and 282.50 mm/30 s on the gruels from the Atp-Y and Coca-sr dehulled flours) and sweetening (7193.10 and 8735.63 mg/100 mL on the gruels from the Atp-Y and Coca-sr dehulled flours) potential of the two dehulled flours. A positive correlation was observed between the sweetening and liquefying potential of the germinated flours. The combination of these different flours (malted and dehulled flours) allowed to potentiate the responses up to 3.5 times compared to the previous data. The optimal conditions obtained in this study could be applied to reduce the energy and nutrient deficiency and improve the fluidity of infant formula.