Dichloromethane Extract Research Articles

Portulaca oleracea L seed extracts counteract diabetic nephropathy through SDF-1/IL10/PPARγ–mediated tuning of keap1/Nrf2 and NF-κB transcription in Sprague Dawley rats

Background & objective: While oxidative stress is the key player driving diabetic nephropathy (DN), firm glycemic control remains the pillar prophylactic measure. Purslane was extensively described as a potent hypoglycemic and hypolipidemic agent owing to its rich content of antioxidants. Therefore, this report aimed to assess the renoprotective potentials of methanol (MO) and methylene chloride (MC) fixed oil extracts of purslane seeds in a diabetic nephropathy (DN) model.MethodsPurslane seeds were extracted using absolute methanol and methylene chloride, and type-1 diabetes was induced with a single 55 mg/kg dose of Streptozotocin (STZ) dissolved in 100 mmol/L citrate buffer (pH 4.5), and then diabetic animals were received MO, MC, for 42 consecutive days to compare their antidiabetic effect relative to the reference drug “Losartan”. Renal functions and DN biomarkers were weekly assessed, and the relative expression of different oxido-inflammatory mediators was quantified in diabetic kidneys by RT-PCR. Data were statistically analyzed using GraphPad Prism 9.0.2.ResultsThe oral administration of MO and MC extracts (250 mg/kg/day) significantly ameliorated the body weight loss (P < 0.0001 / each), fasting blood glucose levels (FBG) (P < 0.0001 / each), urine volume (P < 0.0001 / each), as well as serum creatinine (P < 0.0001 / each), uric acid (P = 0.0022, 0.0052), and blood urea nitrogen (BUN) (P = 0.0265, 0.0338); respectively, compared with the untreated diabetic rats. In addition, both extracts restored the effectuality of antioxidative machinery in diabetic kidneys as indicated by a significant reduction of ROS accumulation and lipid peroxidation; higher GSH content, and promoted activity of glutathione reductase and superoxide dismutase antioxidant enzymes (P < 0.0001 / each). Histologically, both extracts alleviated the DN-structural alterations including the glomerular congestion and tubular degeneration, with MC-treated kidneys showing near to normal architecture. The transcription profiles of all treated kidneys revealed a significantly downregulated expression of TNF-α, IL-6, Keap1 and NF-κB genes, concomitant with a significant upregulation of SDF-1, IL-10, Nrf2, HO-1, and PPARγ gene expression (P < 0.0001 / all).ConclusionThese findings highlight the remarkable DN-prophylactic potentials of purslane extracts mediated by neutralizing the hyperglycemia-induced ROS accumulation, and circumventing the downstream inflammatory cascades, surpassing the reference angiotensin receptor blocker; i.e. Losartan.

Development of emulgel formulation from Markhamia tomentosa leaf extract: Characterization and in vitro antimicrobial activity against skin isolates

Objectives: Skin infections are mild to severe infections often treated with antimicrobial agents. There is an increase in resistance to antimicrobial agents necessitating the search for new medicines. This study developed an emulgel formulation of Markhamia tomentosa leaf extract and evaluated its antimicrobial activity against skin isolates. Materials and Methods: A successive extraction of M. tomentosa leaves in five solvents – n-hexane, dichloromethane, ethyl acetate, ethanol, and distilled water was carried out. The activity of the extracts against skin isolates of Staphylococcus aureus, Staphylococcus epidermidis, and Bacillus subtilis was carried out. The distilled water extract was formulated into emulgel, characterized, and evaluated for antimicrobial activity. Results: The n-hexane and dichloromethane extracts of M. tomentosa were inactive against all organisms at concentrations used. The ethanol extract was active against S. aureus and S. epidermidis at 200 mg/mL. The ethyl acetate and distilled water extracts were active against S. epidermidis and B. subtilis at 100 and 50 mg/mL, respectively. All emulgel formulations of distilled water extract of M. tomentosa leaves were brown, smooth, and easy to spread on the skin and had a pH of 4.73–5.55. The formulation containing the distilled water extract was more viscous (7784cP) than the blank formulation (6328cP). The formulation was active against S. epidermidis. Conclusion: The distilled water extract of M. tomentosa leaves was the most active against S. epidermidis and B. subtilis. Its emulgel formulation had desirable physicochemical properties for application to the skin. Further studies can be carried out toward its development for the treatment of skin infection caused by organisms investigated.

Dictyostelium discoideum -assisted pharmacognosy of plant resources for discovering antivirulence molecules targeting Klebsiella pneumoniae

The rise of antibiotic-resistant bacterial strains represents an important challenge for global health, underscoring the critical need for innovative strategies to confront this threat. Natural products and their derivatives have emerged as a promising reservoir for drug discovery. The social amoeba Dictyostelium discoideum is a potent model organism in this effort. Employing this invertebrate model, we introduce a novel perspective to investigate natural plant extracts in search of molecules with potential antivirulence activity. Our work established an easy-scalable developmental assay targeting a virulent strain of Klebsiella pneumoniae, with Helenium aromaticum as the representative plant. The main objective was to identify tentative compounds from the Helenium aromaticum extract that attenuate the virulence of K. pneumoniae virulence without inducing cytotoxic effects on amoeba cells. Notably, the methanolic root extract of H. aromaticum fulfilled these prerequisites compared to the dichloromethane extract. Using UHPLC Q/Orbitrap/ESI/MS/MS, 63 compounds were tentatively identified in both extracts, 47 in the methanolic and 29 in the dichloromethane, with 13 compounds in common. This research underscores the potential of employing D. discoideum-assisted pharmacognosy to discover new antivirulence agents against multidrug-resistant pathogens.

Antifungal Potential of Secondary Metabolites Derived from Arcangelisia flava (L.) Merr.: An Analysis of In Silico Enzymatic Inhibition and In Vitro Efficacy against Candida Species

Considering the escalating resistance to conventional antifungal medications, it is critical to identify novel compounds that can efficiently counteract this challenge. The purpose of this research was to elucidate the fungicidal properties of secondary metabolites derived from Arcangelisia flava, with a specific focus on their efficacy against Candida species. This study utilized a combination approach comprising laboratory simulations and experiments to discern and evaluate the biologically active constituents present in the dichloromethane extract of A. flava. The in vitro experiments demonstrated that compounds 1 (palmatine) and 2 (fibraurin) exhibited antifungal properties. The compounds exhibited minimum inhibitory concentrations (MICs) ranging from 15.62 to 62.5 µg/mL against Candida sp. Moreover, compound 1 demonstrated a minimum fungicidal concentration (MFC) of 62.5 µg/mL against Candida glabrata and C. krusei. In contrast, compound 2 exhibited an MFC of 125 µg/mL against both Candida species. Based on a molecular docking study, it was shown that compounds 1 and 2 have a binding free energy of −6.6377 and −6.7075 kcal/mol, respectively, which indicates a strong affinity and specificity for fungal enzymatic targets. This study utilized pharmacophore modeling and Density Functional Theory (DFT) simulations to better understand the interaction dynamics and structural properties crucial for antifungal activity. The findings underscore the potential of secondary metabolites derived from A. flava to act as a foundation for creating novel and highly efficient antifungal treatments, specifically targeting fungal diseases resistant to existing treatment methods. Thus, the results regarding these compounds can provide references for the next stage in antifungal drug design. Further investigation is necessary to thoroughly evaluate these natural substances’ clinical feasibility and safety characteristics, which show great potential as antifungal agents.

Isolation of a Marker Olean-12-en-28-butanol Derivative from Viscum continuum E. Mey. Ex Sprague and the Evaluation of Its Antioxidant and Antimicrobial Potentials.

Viscum continuum E. Mey. Ex Sprague (Mistletoe) is a semi-parasitic plant that grows on the branches of other trees with reported numerous biological activities. This study was aimed at isolating a compound/s that will be used as a standard reference for quality control of South African-based commercialized mistletoe products and to further perform antioxidant and antimicrobial tests on the isolated compound. A dried sample of mistletoe was ground and extracted successively with hexane, dichloromethane (DCM), acetone and methanol using a serial exhaustive cold maceration procedure. The compound was isolated using column chromatography, and its chemical structure was elucidated using two-dimensional nuclear magnetic resonance (2D NMR) and ultrahigh-performance liquid chromatography-mass spectrometry (UPLC-MS). The antioxidant activity of the compound was determined using DPPH, hydrogen radical scavenging activity and reducing power assays, whereas antimicrobial activity was assessed using the minimum inhibitory concentration (MIC) method. Subjection of the DCM extract to column chromatography resulted in the isolation of a compound elucidated as olean-12-en-28-butanol-1-one, 3-hydroxy-4,4,10, 14, 20-pentamethyl (D4). Both the DPPH, H2O2 radical scavenging activity and reducing power assays revealed a significant antioxidant potential of compound D4 with an IC50 of 0.701 mg/mL, lower than that of gallic acid (0.793 mg/mL) for the H2O2 radical scavenging assay. The results also indicated good antibacterial activity of D4 with an IC50 of 0.25 mg/mL, compared to ciprofloxacin with an IC50 of 0.0039 mg/mL, against two Gram-negative (Pseudomonas aeruginosa, Escherichia coli) and three Gram-positive (Streptococcus pyogenes, Bacillus cereus and Staphylococcus aureus) bacteria. This study is the first to report on the isolation of the olean-12-en-28-butanol derivative from mistletoe of the South African ecotype.

Determination of vancomycin and meropenem in serum and synovial fluid of patients with prosthetic joint infections using UPLC-MS/MS.

Numerous studies have suggested that intra-articular administration of antibiotics following primary revision surgery may be one of the methods for treating prosthetic joint infection (PJI). Vancomycin and meropenem are the two most commonly used antibiotics for local application. Determining the concentrations of vancomycin and meropenem in the serum and synovial fluid of patients with PJI plays a significant role in further optimizing local medication schemes and effectively eradicating biofilm infections. This study aimed to establish a rapid, sensitive, and accurate ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method for determining the concentrations of vancomycin and meropenem in human serum and synovial fluid. Serum samples were processed using acetonitrile precipitation of proteins and dichloromethane extraction, while synovial fluid samples were diluted before analysis. Chromatographic separation was achieved in 6min on a Waters Acquity UPLC BEH C18 column, with the mobile phase consisting of 0.1% formic acid in water (solvent A) and acetonitrile (solvent B). Quantification was carried out using a Waters XEVO TQD triple quadrupole mass spectrometer with an electrospray ionization (ESI) source in positive ion mode. The multiple reaction monitoring (MRM) mode was employed to detect the following quantifier ion transitions: 717.95-99.97 (norvancomycin), 725.90-100.04 (vancomycin), 384.16-67.99 (meropenem). The method validation conformed to the guidelines of the FDA and the Chinese Pharmacopoeia. The method demonstrated good linearity within the range of 0.5-50 μg/ml for serum and 0.5-100 μg/ml for synovial fluid. Selectivity, intra-day and inter-day precision and accuracy, extraction recovery, matrix effect, and stability validation results all met the required standards. This method has been successfully applied in the pharmacokinetic/pharmacodynamic (PK/PD) studies of patients with PJI.

Phytochemical evaluation of Ziziphus mucronata and Xysmalobium undulutum towards the discovery and development of anti-malarial drugs

BackgroundThe development of resistance by Plasmodium falciparum is a burdening hazard that continues to undermine the strides made to alleviate malaria. As such, there is an increasing need to find new alternative strategies. This study evaluated and validated 2 medicinal plants used in traditional medicine to treat malaria.MethodsInspired by their ethnobotanical reputation of being effective against malaria, Ziziphus mucronata and Xysmalobium undulutum were collected and sequentially extracted using hexane (HEX), ethyl acetate (ETA), Dichloromethane (DCM) and methanol (MTL). The resulting crude extracts were screened for their anti-malarial and cytotoxic potential using the parasite lactate dehydrogenase (pLDH) and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, respectively. This was followed by isolating the active compounds from the DCM extract of Z. mucronata using silica gel chromatography and structural elucidation using spectroscopic techniques (NMR: 1H, 12C, and DEPT). The active compounds were then targeted against P. falciparum heat shock protein 70–1 (PfHsp70-1) using Autodock Vina, followed by in vitro validation assays using ultraviolet–visible (UV–VIS) spectroscopy and the malate dehydrogenase (MDH) chaperone activity assay.ResultsThe extracts except those of methanol displayed anti-malarial potential with varying IC50 values, Z. mucronata HEX (11.69 ± 3.84 µg/mL), ETA (7.25 ± 1.41 µg/mL), DCM (5.49 ± 0.03 µg/mL), and X. undulutum HEX (4.9 ± 0.037 µg/mL), ETA (17.46 ± 0.024 µg/mL) and DCM (19.27 ± 0.492 µg/mL). The extracts exhibited minimal cytotoxicity except for the ETA and DCM of Z. mucronata with CC50 values of 10.96 and 10.01 µg/mL, respectively. Isolation and structural characterization of the active compounds from the DCM extracts revealed that betulinic acid (19.95 ± 1.53 µg/mL) and lupeol (7.56 ± 2.03 µg/mL) were responsible for the anti-malarial activity and had no considerable cytotoxicity (CC50 > µg/mL). Molecular docking suggested strong binding between PfHsp70-1, betulinic acid (− 6.8 kcal/mol), and lupeol (− 6.9 kcal/mol). Meanwhile, the in vitro validation assays revealed the disruption of the protein structural elements and chaperone function.ConclusionThis study proves that X undulutum and Z. mucronata have anti-malarial potential and that betulinic acid and lupeol are responsible for the activity seen on Z. mucronata. They also make a case for guided purification of new phytochemicals in the other extracts and support the notion of considering medicinal plants to discover new anti-malarials.

Multidirectional research for the therapeutic potential of Phlomoides molucelloides (Bunge) Salmaki: LC-MS/MS, antioxidant, enzyme inhibition, and antiproliferative characteristics

Medicinal plants offer natural cures and inspire modern medicine's development. This study examined the antioxidant, enzyme-inhibitory, and antiproliferative activities of various extracts obtained from aerial and root fragments of Phlomoides molucelloides (Bunge) Salmaki. The extracts' overall phenolics, flavonoids, and compounds were defined using colorimetric and LC-MS/MS analyses. The highest total phenolic and flavonoid content was measured in the methanol and infusion extracts of the aerial fragments, with 102.21 mg RE/g and 51.33 mg GAE/g, respectively. Most compounds were defined as flavonoids, predominantly as apigenin and quercetin glycosides. Methanol, 70 % methanol, and infusion extracts from aerial parts had the highest antioxidant activity determined by DPPH, ABTS, CUPRAC, FRAP, metal chelation, and phosphomolybdenum analyses. Moreover, the methanol extract of the roots had the highest anti-acetylcholinesterase, anti-butyrylcholinesterase, and anti-glucosidase activities. The dichloromethane extracts of the roots displayed the highest anti-tyrosinase and anti-amylase activities. The antiproliferative activity of the extracts was investigated against MDA-MB-231, MCF-7, and HeLa cell lines. The lowest IC50 value (875.7 µg/mL) was computed for the methanol extract of the aerial part on the MCF-7 cell line at the 48th h. The findings showed that P. molucelloides extracts may offer a promising therapeutic approach due to their rich bioactive content.

Phyto-constituents of the Dichloromethane Extracts of the Bulbs of Selected Genera in the Family Amaryllidaceae

The analysis of phytoconstituents present in the dichloromethane extract of the bulb of Hippeastrum vittatum (L’Her.) Herb., Proiphys amboinensis (L.) Herb., Urceolina amazonica (Linden) Christenh. &amp; Byng., Hymenocallis littoralis (Jacq.) Salisb., Crinum jagus (J. Thomps.) Dandy and Zephyranthes carinata Herb. by Gas Chromatography-Mass Spectometry (GC-MS) analysis was carried out using standard methods. The Results of the GC-MS analysis of Hippeastrum vittatum, Proiphys amboinensis, Urceolina amazonica, Hymenocallis littoralis, Crinum jagus and Zephyranthes carinata revealed the presence of 50, 66, 61, 57, 56 and 61 peaks indicating the presence of the number of phytochemical constituents respectively. Phytol was present in Hymennocallis littoralis (0.41%) and Urceolina amazonica (0.79%) only. N-hexadecanoic acid, Di mevalonic acid lactone, Hexadecanoic acid methyl ester and Stigmasterol were present in all. Apiol and Xanthoxylin were absent in H. littoralis and P. amboniensis respectively. Oleic acid was present in Z. carinata (2.01%), P. amboniensis (1.85%) and U. amazonica (2.03%). Sakuranin was found in H. littoralis (3.42%), C. jagus (1.38%) and U. amazonica (4.43%). Linoleic acid ethyl ester was present in P. amboniensis (1.49%), U. amazonica (0.16%), H. littoralis (11.91%) and Z. carinata (0. 8 8%). The major components that delimited the species were as follows; In Hymenocallis littoralis was Liriodendromin (14.03%), Linoleic acid ethyl ester (11.91%) and Ethyl oleate (9.38%); in Zephranthes carinata; Phthalic acid, 4-methoxybenzyl methyl ester (15.34%) Gatanthamine, 3-O-acetyl-1, 2, dihydro (8.87%) Stigmasterol (5.87%); in Hippeastrum vittatum; N-benzyl-2-[1-(4-methoxyl-phenyl 1) – 1 H-tetrazo (14.94%), Benzaminde, 2-amino-N-(4-ethoxyphenyl) (12.65%) and 1-(5-methyl-2-hydroxyphenyl)-3-phenyl propane (10.49%); in Crinum jagus; 2H-1-Benzopyran-7-ol, 3,4-dihydro-3-(2-hyrdo) (19.87%), Benzamide, 2-amino-N- (4-ethoxyphenyl) (9.92%) and Stigmasterol (4.04%); in Proiphys amboniensis; Gamma-sitosterol (16.98%), Stigmasterol (11.49%) and N-Hexadecanoic acid(5.05%); in U. amazonica; 3-Furanacetic acid, 4-hexyl-2, 5-dihydro-2, 5 (12.73%), Benzamide, 2-amino-N- (4-ethoxyphenyl) (8.18%) and Phenyl, 2-(3,4-dihydro 2-methoxyl-2H-1-benzopy) (6.40%). The presence of various bioactive compounds may be responsible for the application of these species in the treatment and management of various ailments in folklore medicine. However, in vitro and in vivo studies, isolation of individual phytoconstituents and their mechanism of action may proceed to find a novel drug or lead compound for use as medicine.

Unlocking the functional potential of Nitraria schoberi extracts using chemical fingerprinting, biological efficiencies, in silico and network pharmacological approaches

The objective of this investigation was to assess the cytotoxic, antioxidant, and enzyme inhibitory properties of the aerial portions of Nitraria schoberi (family Nitrariaceae). Extracts were prepared by sequential maceration in hexane, dichloromethane (DCM), ethyl acetate and methanol (MeOH) and water extract was prepared by infusion. DCM and MeOH extracts accumulated the highest amount of metabolites where the former was characterized by the presence of octadecyl ferulate (16.96 mg/100 mg), methoxyluteolin (8.48 mg/100 mg) and isorhamnetin (5.35 mg/100 mg) and the alkaloids perlolyrine (5.03 mg/100 mg), (+)-5a-hydroxylemannine (2.43 mg/100 mg) and matrine (2.40 mg/100 mg). Results of antioxidant activity showed that the MeOH extract exerted the highest anti-2,2-diphenyl-1-picrylhydrazyl (DPPH) (28.13 mg Trolox equivalent (TE)/g) and Fe+++ (54.38 mg TE/g) reducing capacity. All extracts exerted significant acetylcholinesterase (3.71–4.37 mg galantamine equivalent (GALAE)/g) and tyrosinase (86.40–109.63 mg kojic acid equivalent (KAE)/g) inhibition activity. The best α-amylase and α-glucosidase inhibition was exhibited by the DCM (0.81 mmol ACAE/g) and MeOH (1.34 mmol ACAE/g) extracts respectively. The highest cytotoxic effect was exerted against the breast adenocarcinoma (MDA-MB-231) (IC50: 26.71 μg/mL) and cervix adenocarcinoma (HELA) (IC50: 29.10 μg/mL) cell lines by the MeOH and DCM extracts respectively. In addition, we performed molecular docking analysis to understand the interaction between chemical components and tested enzymes and cellular targets for cancer. Chrysoeriol-3-O-rutinoside bound strongly to AChE. Furthermore, a good interaction between vascular endothelial growth factor receptor 2 (VEGFR2) and isovitexin-2″-O-arabinoside was observed. We employed network pharmacology to understand the role of N. schoberi's compounds in neurological disorder like Alzheimer and multiple sclerosis. Therefore, the results of this study indicate that N. schoberi may serve as a viable starting point for the future creation of phytopharmaceuticals that target particular diseases associated with oxidative stress, such as diabetes and certain neurological disorders.

Correlation between intestinal toxicity and composition changes of toxic parts from Euphorbia ebracteolata before and after Terminalia chebula soup processing

This study aims to explore the correlation between intestinal toxicity and composition changes of Euphorbia ebracteolata before and after Terminalia chebula soup(TCS) processing. Intragastric administration was performed on the whole animal model. By using fecal water content, inflammatory causes, and pathological damage of different parts of the intestinal tract of mice as indexes, the differences in intestinal toxicity of dichloromethane extraction of raw E. ebracteolata(REDE), dichloromethane extraction of TCS, and dichloromethane extraction of E. ebracteolata after simulated TCS processing(STREDE) were compared, so as to investigate the effect of TCS processing on the intestinal toxicity of E. ebracteolata. At the same time, the component databases of E. ebracteolata and T. chebula were constructed, and the composition changes of diterpenoids, tannins, and phenolic acids in the three extracted parts were analyzed by HPLC-TOF-MS. HPLC was used to compare the content of four diterpenoids including ent-11α-hydroxyabicta-8(14), 13(15)-dien-16, 12-olide(HAO), jolkinolide B(JNB), fischeria A(FA), and jolkinolide E(JNE) in the E. ebracteolata before and after processing and the residue of container wall after processing, so as to investigate the effect of TCS processing on the content and structure of the diterpenoids. The results showed that the REDE group could significantly increase the fecal water content and the release levels of TNF-α and IL-1β from each intestinal segment, and intestinal tissue damage was accompanied by significant infiltration of inflammatory cells. However, compared with the REDE group, the intestinal tissue damage in the STREDE group was alleviated, and the infiltration of inflammatory cells decreased. The intestinal toxicity significantly decreased. Mass spectrometry analysis showed that there was no significant difference in the content of diterpenoids of REDE before and after simulated TCS processing, but a large number of tannins and phenolic acids were added. The results of HPLC showed that the content of four diterpenoids of E. ebracteo-lata decreased to varying degrees after TCS processing, ranging from-0.35% to-19.74%, and the decreased part mainly remained in the container wall, indicating that the structure of toxic diterpenoids of E. ebracteolata was not changed after TCS processing. The antagonistic effect of tannic and phenolic acids in the TCS may be the main reason for the reduced intestinal toxicity of E. ebracteolata after TCS processing. The TCS processing for E. ebracteolata is scientific.

Phytochemical Profiling Studies of Alkaloids and Coumarins from the Australian Plant Geijera parviflora Lindl. (Rutaceae) and Their Anthelmintic and Antimicrobial Assessment.

Phytochemical profiling followed by antimicrobial and anthelmintic activity evaluation of the Australian plant Geijera parviflora, known for its customary use in Indigenous Australian ceremonies and bush medicine, was performed. In the present study, seven previously reported compounds were isolated including auraptene, 6'-dehydromarmin, geiparvarin, marmin acetonide, flindersine, and two flindersine derivatives from the bark and leaves, together with a new compound, chlorogeiparvarin, formed as an artefact during the isolation procedure and isolated as a mixture with geiparvarin. Chemical profiling allowed for a qualitative and quantitative comparison of the compounds in the leaves, bark, flowers, and fruit of this plant. Subsequently, a subset of these compounds as well as crude extracts from the plant were evaluated for their antimicrobial and anthelmintic activities. Anthelmintic activity assays showed that two of the isolated compounds, auraptene and flindersine, as well as the dichloromethane and methanol crude extracts of G. parviflora, displayed significant activity against a parasitic nematode (Haemonchus contortus). This is the first report of the anthelmintic activity associated with these compounds and indicates the importance of such fundamental explorations for the discovery of bioactive phytochemicals for therapeutic application(s).

Phytochemical Constituents of Sap, Root and Leaf Extracts of Calotropis Procera from Select Regions in the Gambia

Medicinal plants serve as potential cure for animal and human diseases as they contain phytochemicals for therapeutic values. Most of the modern drugs produced are isolated from herbal plants. This research reports on the phytochemical constituents of the methanolic and dichloromethane (DCM) extracts of the sap, root and leaf of Calotropis procera in three select regions in The Gambia namely the West Coast Region, North Bank Region, and Lower River Region. The sap was collected in an air-tight test tube; the root and leaf were dried at room temperature for three weeks and one month, respectively and further ground into powder. Soxhlet extraction of the sap was done using both DCM for 30 minutes at 40oC to 50oC and methanol for 3 h at 60oC to 70oC. The root and leaf were extracted using cold maceration for 72 h. The methanolic extracts showed the presence of alkaloids, quinones, saponins, flavonoids, terpenoids, steroids, and carbohydrates in the sap and leaf. Quinones were present in the DCM extract of the sap and root, but absent in the leaf. While flavonoids and terpenoids were present in the sap and leaf extracts, they were absent in the root. Alkaloids, saponins, and steroids were absent in the sap and root extracts, but found in the leaf. Tannins and phenols were absent in both the methanolic and DCM extracts. The results of each of the samples collected at the three different regions were similar in their phytochemical constituents for the extracting solvents; but varied with the different solvent. The findings of this research allude to the fact that the sap, root and leaf of C. procera are good sources of therapeutic compounds that are responsible for the use of this plant in herbal medicine in The Gambia.

Phytochemical Profiling and Therapeutic Potential of Ficus benjamina L.: Insights into Anticancer and Anti-inflammatory Activities

Background: Ficus benjamina L., commonly known as the weeping fig, is a plant traditionally used for various medicinal purposes, particularly in Southeast Asia. Despite its widespread use, there is a scarcity of scientific data validating its therapeutic properties, especially its anti-inflammatory and anticancer potentials. Objective: This study aimed to investigate the phytochemical profile of Ficus benjamina L. and to evaluate its anticancer and anti-inflammatory activities to provide a scientific basis for its traditional uses. Methods: The plant materials were collected and subjected to extraction using methanol and dichloromethane. The extracts were analyzed for primary and secondary metabolites. The anticancer activity was tested using the MTT assay on HeLa cells, and anti-inflammatory activity was assessed using a luminol-enhanced chemiluminescence method. Data analysis was conducted using IBM SPSS Statistics Version 25, focusing on inferential statistics to compare the bioactivity of the extracts against standard drugs. Results: Phytochemical analysis confirmed the presence of proteins, lipids, carbohydrates, alkaloids, flavonoids, and tannins. The dichloromethane extract showed significant anti-inflammatory activity with 58.6% inhibition at a concentration of 50 µg/ml and an IC50 of 8.966±1.03. The methanol extract exhibited minimal anticancer activity with an 8.3% inhibition rate at 30 µg/ml, suggesting low efficacy against HeLa cells compared to the standard drug, Doxorubicin, which showed a 101.2% inhibition. Conclusion: The study confirms that Ficus benjamina L. contains bioactive compounds with potential anti-inflammatory benefits and limited anticancer activity. These findings support the traditional use of the plant in treating inflammatory conditions and highlight the need for further research to optimize extraction techniques and expand biological testing.

Cyclic peroxides and analogs: Antibacterial, antimalarial, and cytotoxic marine products from Xisha sponge Diacarnus sp.

A chemical investigation of the dichloromethane extract from the Xisha sponge Diacarnus sp. revealed seven undescribed norterpene cyclic peroxides, named diacarperoxides T–Z, and five unreported related norterpenes, named diacarnoids E–I, and eleven previously reported compounds. The structures of these isolated compounds, including their absolute configurations, were elucidated based on extensive spectroscopic analyses, electronic circular dichroism (ECD) calculations, Snatzke's method, [Rh2(OCOCF3)4]-induced ECD spectra, and modified Mosher's method. Bioassays were performed to assess the antibacterial activity against six pathogenic bacteria, cytotoxicities toward three cancer cell lines, and antimalarial activity against Plasmodium parasites. Most of the cyclic peroxides exhibited substantial antibacterial activity (MIC 1–8 μg/mL). Diacarperoxide W and nuapapuin A showed substantial antimalarial activity with IC50 values of 0.98 and 2.83 μM. Moreover, many compounds exhibited <50% cell survival rates, and IC50 values of 0.22–6.33 μM. The apoptosis assay showed that nuapapuin A induced cancer cell apoptosis in a dose-dependent manner.

Edible Medicinal Guava Fruit (Psidium guajava L.) Are a Source of Anti-Biofilm Compounds against Pseudomonas aeruginosa.

Psidium guajava is one of the most common edible medicinal plants frequently used in Malagasy traditional medicine to treat gastrointestinal infections. In order to evaluate their probable antibacterial activities, three organic extracts (successive extractions by hexane, dichloromethane, and ethanol) of ripe guava fruits were assessed for their bactericidal and anti-virulence properties against P. aeruginosa PAO1. Although these three extracts have shown no direct antibacterial activity (MIC of 1000 µg/mL) and, at the non-bactericidal concentration of 100 µg/mL, no impact on the production of major P. aeruginosa PAO1 virulence factors (pyocyanin and rhamnolipids), the hexane and dichloromethane extracts showed significant anti-biofilm properties and the dichloromethane extract disrupted the P. aeruginosa PAO1 swarming motility. Bioguided fractionation of the dichloromethane extract led to the isolation and identification of lycopene and β-sitosterol-β-D-glucoside as major anti-biofilm compounds. Interestingly, both compounds disrupt P. aeruginosa PAO1 biofilm formation and maintenance with IC50 of 1383 µM and 131 µM, respectively. More interestingly, both compounds displayed a synergistic effect with tobramycin with a two-fold increase in its effectiveness in killing biofilm-encapsulated P. aeruginosa PAO1. The present study validates the traditional uses of this edible medicinal plant, indicating the therapeutic effectiveness of guava fruits plausibly through the presence of these tri- and tetraterpenoids, which deserve to be tested against pathogens generally implicated in diarrhea.

Exploring nature's antidote: unveiling the inhibitory potential of selected medicinal plants from Kisumu, Kenya against venom from some snakes of medical significance in sub-Saharan Africa.

Background: The present study investigated the efficacy of Conyza bonariensis, Commiphora africana, Senna obtusifolia, Warburgia ugandensis, Vernonia glabra, and Zanthoxylum usambarense against Bitis arietans venom (BAV), Naja ashei venom (NAV), and Naja subfulva venom (NSV). Methods: 40 extracts and fractions were prepared using n-hexane, dichloromethane, ethyl acetate, and methanol. In vitro efficacy against snake venom phospholipase A2 (svPLA2) was determined in 96-well microtiter and agarose-egg yolk coagulation assays. in vivo efficacy against venom-induced cytotoxicity was determined using Artemia salina. Two commercial antivenoms were used for comparison. Results: The 96-well microtiter assay revealed poor svPLA2 inhibition of BAV by antivenom (range: 20.76% ± 13.29% to 51.29% ± 3.26%) but strong inhibition (>90%) by dichloromethane and hexane fractions of C. africana, hexane and ethyl acetate extracts and fraction of W. ugandensis, dichloromethane fraction of V. glabra, and the methanol extract of S. obtusifolia. The methanol extract and fraction of C. africana, and the hexane extract of Z. usambarense strongly inhibited (>90%) svPLA2 activity in NAV. The hexane and ethyl acetate fractions of V. glabra and the dichloromethane, ethyl acetate, and methanol extracts of C. africana strongly inhibited (>90%) svPLA2 in NSV. The agarose egg yolk coagulation assay showed significant inhibition of BAV by the dichloromethane fraction of C. africana (EC50 = 3.51 ± 2.58μg/mL), significant inhibition of NAV by the methanol fraction of C. africana (EC50 = 7.35 ± 1.800μg/mL), and significant inhibition of NSV by the hexane extract of V. glabra (EC50 = 7.94 ± 1.50μg/mL). All antivenoms were non-cytotoxic in A. salina but the methanol extract of C. africana and the hexane extracts of V. glabra and Z. usambarense were cytotoxic. The dichloromethane fraction of C. africana significantly neutralized BAV-induced cytotoxicity, the methanol fraction and extract of C. africana neutralized NAV-induced cytotoxicity, while the ethyl acetate extract of V. glabra significantly neutralized NSV-induced cytotoxicity. Glycosides, flavonoids, phenolics, and tannins were identified in the non-cytotoxic extracts/fractions. Conclusion: These findings validate the local use of C. africana and V. glabra in snakebite but not C. bonariensis, S. obtusifolia, W. ugandensis, and Z. usambarense. Further work is needed to isolate pure compounds from the effective plants and identify their mechanisms of action.

Evaluation of the Antiproliferative Potential of Yellow Jaboticaba (Myrciaria glazioviana) Extracts Against Human Cervical Cancer (HeLa cells line) and the Analysis of Their Chemical Composition by HPLC-HRESIMS.

Cervical cancer is a specific type of cancer that affects women around the world, with an incidence of 604 thousand new cases per year and 341 thousand deaths. There is a high demand for new effective antineoplastic drugs with few side effects. In this sense, recent research highlights the potential of compounds of natural origin in treating and preventing different types of cancer. Myrciaria glazioviana is a Brazilian native species belonging to the Myrtaceae family, which has previously described biological activities such as antimicrobial, anti-inflammatory, and antioxidant properties. This study aims to evaluate the anticancer activity of the dichloromethane extract (MGD) and ethyl acetate extract (MGA) of M. glazioviana leaves against human cervical cancer cell line (HeLa), as well as to identify their bioactive compounds. Using HPLC-HRESIMS technique, ten compounds were characterized in both samples: quinic acid, ellagic acid, Tri-O-methyl ellagic acid, two derivatives of Tetra-O-methyl flavellagic acid, quercetrin, Di-O-methyl ellagic acid, and three derivatives of pentamethyl coruleoellagic acid. Through MTT assays using HeLa cells and NIH/3T3 cells, it was observed that MGD and MGA were selective against tumor cells, with IC50 values of 24.31 and 12.62 μg/mL, respectively. The samples induced the tumor cell death by apoptosis, as evidenced by the activation of caspases 3/7, cell shrinkage, and pyknotic nuclei. Both samples were also able to inhibit the migration of HeLa cells after 24 hours of treatment, indicating a potential antimetastatic effect. Therefore, the present research highlights the antiproliferative and antimigratory potential of this species against HeLa cells.

Molecular networking-based mass spectral identification of Brucea javanica (L.) Merr. metabolites and their selective binding affinities for dengue virus enzymes

Brucea javanica, a valued traditional medicinal plant in Malaysia, known for its fever-treating properties yet remains underexplored for its potential antiviral properties against dengue. This study aims to simultaneously identify chemical classes and metabolites within B. javanica using molecular networking (MN), by Global Natural Product Social (GNPS), and SIRIUS in silico annotation. Liquid chromatography-mass spectrometry (LC-MS2)-based MN explores chemical diversity across four plant parts (leaves, roots, fruits, and stem bark), revealing diverse metabolites such as tryptophan-derived alkaloids, terpenoids, and octadecadenoids. Simultaneous LC-MS2 and MN analyses reveal a discriminative capacity for individual plant components, with roots accumulating tryptophan alkaloids, fruits concentrating quassinoids, leaves containing fusidanes, and stem bark primarily characterised by simple indoles. Subsequently, extracts were evaluated for dengue antiviral activity using adenosine triphosphate (ATP) and plaque assays, indicates potent efficacy in the dichloromethane (DCM) extract from roots (EC50 = 0.3 μg/mL, SI = 10). Molecular docking analysis of two major compounds; canthin-6-one (264) and 1-hydroxy-11-methoxycanthin-6-one (275) showed potential binding interactions with active sites of NS5 RNA-dependent RNA polymerase (RdRp) of dengue virus (DENV) protein. Subsequent in vitro evaluation revealed compounds 264 and 275 had a promising dengue antiviral activity with SI value of 63 and 1.85. These identified metabolites emerge as potential candidates for further evaluation in dengue antiviral activities.

Sucrose esters of aryldihydronaphthalene-type lignans, and antitumor activity of extracts of Moltkiopsis ciliata (Forssk.) aerial parts

One new compound (3f-[(7′R,8′R)-4,4′-dihydroxy-5-methoxy-2,7′-cycloligna-7-en-9-methoxycarbonyl, 9′-carbonyl-O-] -β- D-fructofuranosyl- (2→1)-α- D-glucopyranoside) (Moltkiopsin A) (2) was isolated and identified from the extract of aerial parts of the wild Egyptian plant Moltkiopsis ciliata (Frossk.), family Boraginaceae, for the first time, along with two aryldihydronaphthalene lignans 3f→9′:6f→9-[(7′R,8′R)-4,4′- dihydroxy-3,3′,5-trimethoxy-2,7′-cycloligna-7-en-9,9′-dicarbonyl]-6g-acetyl-α-D-gluco pyranosyl-(1→2) -β-D-fructofuranoside (Trigonotin A) (1) which was reported for the first time from this plant species and a known compound 3f→9′:6f→9-[(7′R,8′R)-4,4′- dihydroxy-3,3′,5-trimethoxy-2,7′-cycloligna-7-en-9,9′-dicarbonyl]-α-D-gluco pyranosyl - (1→2)- β-D- fructofuranoside (Trigonotin C) (3). These compounds were separated and purified using different chromatographic techniques and their structures were elucidated by extensive 1D (1H and 13C NMR), and 2D NMR (COSY, HSQC, and HMBC), besides ESI-MS spectral methods. Extracts were screened as antioxidant, antitumor and antibacterial. The different extracts showed moderate to strong antioxidant capacities in DPPH assays. Ethyl acetate, methylene chloride and crude methanol extracts exhibited the most significant free radicals scavenging activity when compared to the standard antioxidant vitamin C. Hexane and butanol fractions showed the highest cytotoxicity against the cancer cell lines HepG2 and MCF-7.