Activity Of Crude Extract Research Articles

Phytochemical and Biological Investigations of Crude Extracts of Astragalus pisidicus

Background/Objectives: Astragalus L. is a genus of the Fabaceae family, encompassing over 3000 species globally, with 380 species found in Turkey. This is the inaugural examination of the phytochemical, antioxidant, antibacterial, and cytotoxic properties of Astragalus pisidicus. Methods: The water and methanolic fractions of four parts (stems, flowers, leaves, root) as well as the whole plant were quantified and identified by Liquid Chromatography Electrospray Ionization Tandem Mass Spectrometry (LC–ESI–MS/MS) analysis. Cell death was assessed using the WST-1 assay, while apoptosis was identified by colorimetric protease assay for caspase 2, -3, -6, -8, and -9, as well as cellular DNA fragmentation assay. Antioxidant activity of A. pisidicus water and methanolic extracts was investigated with eight different assays. Antimicrobial activities of the extracts were evaluated against 16 bacterial strains by disc diffusion and broth microdilution methods. Results: A total of 13 phytochemicals were detected in the extracts at various concentrations. Hesperidin (147–40,174 µg/g extract) and hyperoside (363–2677 µg/g extract) comprised the principal constituents among the extracts. Fm (IC50 = 9.57 µg/mL), Rm (IC50 = 14.89 µg/mL), and Sm (IC50 = 9.57 µg/mL) were evaluated as active crude extracts on H1299, HT-29, and Panc-1 cells, while Rm (IC50 = 32.057 µg/mL) and Fm (IC50 = 64.25 µg/mL) were assessed as moderately active on MCF-7 and 22RV1 cells, respectively. The elevation of caspase 2, 3, 6, 8, and 9 enzyme activities, along with DNA fragmentation, signifies that the mode of cell death is apoptosis. According to the disc diffusion test results, Fm, Lm, Sm, and WPm extracts exhibited antimicrobial activity against gram (+) bacteria. Conclusions: A. pisidicus elicited apoptotic cell death in cancer cells selectively by the activation of caspases and subsequent DNA fragmentation and may serve as a novel source of an apoptosis-inducing anticancer drug.

Paradendryphiella arenariae an endophytic fungus of Centella asiatica inhibits the bacterial pathogens of fish and shellfish.

Aquaculture has been considered a major food-producing sector in the world during the last few decades. The foremost constraint in the development of aquaculture is bacterial disease control and management. Since various fish pathogens are resistant to conservative treatments, it is essential to screen new and effective alternative antibacterial agents. Endophytic fungi are microorganisms that live in the plant's internal tissues without harming its host. Endophytic fungi have proven themselves as reliable sources of novel bioactive compounds that can be used as antibacterial agents. In the present study, fifteen morphologically different endophytic fungi were isolated from the fresh and healthy stem section of Centella asiatica. The active endophytic fungal crude extracts were tested for agar well diffusion assay, Minimum Inhibitory Concentration, Minimum Bactericidal Concentration assays, Time-kill kinetic analysis, Brine shrimp lethality assay. Agar plug diffusion and agar well diffusion assays revealed that endophytic fungus CAS1 exhibits maximum antagonistic activity against bacterial fish pathogens. The ethyl acetate crude extract of CAS1 exhibited the maximum zone of inhibitions against Aeromonas hydrophila (21 ± 0.11 mm), Aeromonas caviae (18 ± 0.1 mm), Edwardsiella tarda (23 ± 0.11 mm), Vibrio anguillarum (19 ± 0.05 mm) and Vibrio harveyi (20 ± 0.27 mm). The MIC and MBC values extract varied reliant on the trial pathogens ranging between 12.5-100 μg/mL and 25-100μg/mL correspondingly. The morphological and molecular characterization of potential isolate CAS1 was confirmed as Paradendryphiella arenariae by 18S rRNA ITS gene sequencing with 99.18% identity. This is the foremost findings to study the antagonistic effect of Paradendryphiella arenariae isolated from the stem of Centella asiatica against bacterial fish pathogens which can be used as natural effective antibacterial agents in aquaculture.

Bioactivity Profiling and Phytochemical Analysis of Carissa carandas Extracts: Antioxidant, Anti-Inflammatory, and Anti-Urinary Tract Infection Properties.

Carissa carandas L. (Apocynaceae) is widely distributed in tropical and subtropical regions of Asia including Pakistan, India, Afghanistan, and Sri Lanka. C. carandas is considered as an integral component of traditional medicinal systems to combat several health ailments. The present study aimed to assess this plant's phytochemical contents and biological potential by performing sequential extraction, adopting a bioassay-guided approach. C. carandas powder was extracted with n-hexane to remove fatty substances and then residues were sequentially extracted with dichloromethane, methanol, and 50% methanol. All the sequential crude extracts were evaluated for phytochemical contents (total phenolics, flavonoids, and anthocyanins), in vitro antioxidant activity (FRAP, DPPH), in vitro anti-inflammatory activity (serum and egg albumin denaturation), in vivo anti-inflammatory activity (carrageenan- and formaldehyde-induced paw edema), and in vitro antimicrobial activity. Active crude extract was then partitioned using the liquid-liquid separation method followed by further separation of the active fraction by RP-HPLC. The active fraction was then subjected to LC-ESI-MS/MS analysis for tentative identification of bioactive metabolites responsible for its bioactive properties, followed by HPLC quantification. The analysis revealed methanol extract to have more phytochemical contents, radical scavenging properties, reduced inflammation in both models (in vitro and in vivo), and antimicrobial properties against urinary tract infection-causing agents as compared to dichloromethane and 50% methanol extracts. The ethyl acetate fraction obtained after liquid-liquid partitioning (LLP) of the active methanol extract exhibited more activity as compared to C. carandas methanol extract. RP-HPLC sub-fractionation yielded seven sub-fractions, but a slight decrease in biological potential was recorded. Therefore, LLP fraction B was subjected to further analysis. LC-ESI-MS/MS analysis led to the tentative identification of phenolic acids (chlorogenic acid, quinic acid), flavonoids (quercetin), and anthocyanins (peonidin-3-arabinoside, delphinidin-3-galactoside, delphinidin-3-rutinoside) in the active LLP ethyl acetate fraction. Chlorogenic acid, ellagic acid, and quinic acid were quantified as 17.6 µg/mg, 5.90 µg/mg, and 3.30 µg/mg, respectively, on a dry weight basis by HPLC. C. carandas may be considered a promising therapeutic plant, and the results of the current study provide more evidence to support the assertions made in ancient medical traditions. These findings highlight its promising applications in health, medicine, cosmetics, preservatives, and as a natural coloring agent.

Duddingtonia flagrans and its crude proteolytic extract: concomitant action in sheep coprocultures.

The presence of infective larvae (L3) of gastrointestinal nematode (GIN) parasites in pastures directly contributes to the constant recurrence of infections in ruminant herds. This study aimed to evaluate the nematophagous fungus Duddingtonia flagrans (AC001) (proteolytic crude extract and/or conidia) in the in vitro control of GIN L3 in coprocultures. To produce the proteolytic crude extract, a suspension (107 conidia/mL) of D. flagrans was inoculated into a liquid medium. After 6days, the medium was filtered, centrifuged, and its proteolytic activity was measured. For the experimental assay, fecal samples were collected directly from the rectal ampulla of naturally infected sheep, and egg counts per gram of feces (EPG) were performed. Coprocultures were prepared using 10g of fecal material with the groups defined as follows: control group G1 (1.0mL of denatured proteolytic crude extract); treated group G2 (1.0mL of active proteolytic crude extract); treated group G3 (1.0mL of active proteolytic crude extract + 1.0mL of AC001 conidia). The coprocultures were maintained at room temperature (25ºC), for 7days, and then the L3 larvae were recovered. The results demonstrated that AC001 successfully produced protease (56.34 U/mL). The treatments with active proteolytic crude extract (G2) and active proteolytic crude extract + AC001 conidia (G3) were significantly different (p < 0.01) from the control group with denatured proteolytic crude extract (G1). AC001 and its proteolytic crude extract acted concomitantly on helminths directly in the fecal environment, suggesting potential future applications in the field.

Sulphated Fucooligosaccharide from Sargassum Horneri: Structural Analysis and Anti-Alzheimer Activity.

In the present study, sulfated polysaccharides were obtained by digestion of Sargassum horneri and preparation with enzyme-assisted extraction using three food-grade enzymes, and their anti- Alzheimer's activities were investigated. The results demonstrated that the crude sulfated polysaccharides extracted using AMGSP, CSP and VSP dose-dependently (25-100µg·mL- 1) raised the spontaneous alternating manner (%) in the Y maze experiment of mice and reduced the escape latency time in Morris maze test. AMGSP, CSP and VSP also exhibited good anti-AChE and moderate anti-BuChE activities. CSP displayed the best inhibitory efficacy against AChE. with IC50 values of 9.77 µM. And, CSP also exhibited good inhibitory selectivity of AChE over BuChE. Next, CSP of the best active crude extract was separated by the preparation type high performance liquid phase to obtain the sulphated fucooligosaccharide section: SFcup (→3-α-L-fucp(2-SO3-)-1→4-α-L-fucp(2,3-SO3-)-1→section), SFcup showed a best inhibitory efficacy against AChE with IC50 values of 4.03 µM. The kinetic research showed that SFcup inhibited AChE through dual binding sites. Moreover, the molecular docking of SFcup at the AChE active site was in accordance with the acquired pharmacological results.

Isolation and characterization of cytotoxic and antioxidant biomarkers from the aerial parts of Suaedaaegyptica

Chronic disease is an irregular change inside or outside of the tissues and organs that results in accumulation, local damage, and inflammation or irritation. Suaeda aegyptiaca (S. aegyptiaca) is a plant that has been used for a long time for the treatment of human diseases. Therefore, the aim of this present research study is to prepare various plant extracts and screen their antioxidant activity spectroscopically, and later on to isolate antioxidant biomarkers from the significantly highest active crude extract of the aerial parts of S. aegyptiaca. To attain the present objectives, different crude extracts were prepared from the aerial parts of S. aegyptiaca by using a maceration method. The antioxidant and cytotoxic activities of the prepared aerial crude extracts of S. aegyptiaca were determined by 2,2-diphenyl-1-1-picrylhydrazyl (DPPH) and brine shrimp lethality (BSL) methods, respectively. All the prepared aerial crude extracts of the particular plant at six different concentrations showed significant antioxidant activity against the DPPH. The ethyl acetate crude extract showed the highest antioxidant activity, and the lowest activity was in the butanol extract. However, all the aerial crude extracts of S. aegyptiaca were prepared at different concentrations did not show any activity against the BSL method. Based on the antioxidant activity results, the ethyl acetate extract was selected for the isolation of antioxidant compounds. The extract was purified using column chromatography by using different solvent ratios. A series of test tubes were collected with a volume of 3 mL and depending on the similar retention mobility (Rf) behavior, a total of twelve fractions were prepared. Similarly, the antioxidant activity of the obtained twelve fractions from column chromatography was determined by the same DPPH method. All the fractions showed significant antioxidant activity. Among the fractions from the column, fraction 6 gave the highest antioxidant activity and the lowest was fraction 1. In conclusion, all the aerial extracts showed promising activities against DPPH and the fraction with the highest antioxidant activity could be used as natural antioxidant biomarkers to prevent cell damage.

Discovery of Anti-Coronavirus Cinnamoyl Triterpenoids Isolated from Hippophae rhamnoides during a Screening of Halophytes from the North Sea and Channel Coasts in Northern France

The limited availability of antiviral therapy for severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has spurred the search for novel antiviral drugs. Here, we investigated the potential antiviral properties of plants adapted to high-salt environments collected in the north of France. Twenty-five crude methanolic extracts obtained from twenty-two plant species were evaluated for their cytotoxicity and antiviral effectiveness against coronaviruses HCoV-229E and SARS-CoV-2. Then, a bioguided fractionation approach was employed. The most active crude methanolic extracts were partitioned into three different sub-extracts. Notably, the dichloromethane sub-extract of the whole plant Hippophae rhamnoides L. demonstrated the highest antiviral activity against both viruses. Its chemical composition was evaluated by ultra-high performance liquid chromatography (UHPLC) coupled with mass spectrometry (MS) and then it was fractionated by centrifugal partition chromatography (CPC). Six cinnamoyl triterpenoid compounds were isolated from the three most active fractions by preparative high-performance liquid chromatography (HPLC) and identified by high resolution MS (HR-MS) and mono- and bi-dimensional nuclear magnetic resonance (NMR). Specifically, these compounds were identified as 2-O-trans-p-coumaroyl-maslinic acid, 3β-hydroxy-2α-trans-p-coumaryloxy-urs-12-en-28-oic acid, 3β-hydroxy-2α-cis-p-coumaryloxy-urs-12-en-28-oic acid, 3-O-trans-caffeoyl oleanolic acid, a mixture of 3-O-trans-caffeoyl oleanolic acid/3-O-cis-caffeoyl oleanolic acid (70/30), and 3-O-trans-p-coumaroyl oleanolic acid. Infection tests demonstrated a dose-dependent inhibition of these triterpenes against HCoV-229E and SARS-CoV-2. Notably, cinnamoyl oleanolic acids displayed activity against both SARS-CoV-2 and HCoV-229E. Our findings suggest that Hippophae rhamnoides could represent a source of potential antiviral agents against coronaviruses.

Antimicrobial Activities of Some Constituents Isolated from a Kenyan Medicinal Plant, Capparis fascicularis DC

Background of the Study. Capparis fascicularis DC. is an indigenous medicinal plant belonging to the family Capparaceae found in Nyandarua County, Nairobi, Kenya, and many parts of Africa. It is a shrub whose roots are used traditionally to treat colds. Aim. The aim of the present study is to carry out antimicrobial activities of solvent extracts of different parts of Capparis fascicularis, characterize the phytochemical constituents of the most active extract, and identify the most active compounds. Place and Duration of the Study. All the experiments were carried out in the departments of Chemistry and Microbiology, Kenyatta University, Nairobi, Kenya. Methodology. Petroleum ether, ethyl acetate, methanol, and water extracts from the leaves, stem bark, and root bark of C. fascicularis were screened against selected strains of both Gram-positive (Staphylococcus aureus and Bacillus subtilis) and Gram-negative (Salmonella typhimurium and Escherichia coli) bacteria using disc diffusion and tube dilution methods. Fractionation of the most active crude extract was carried out by column chromatography, and the fractions together with the most active crude extract were screened against the selected bacterial strains. The most active fraction was further fractionated, and the subfractions were screened against the bacterial strains to test for possible synergistic effects between the subfractions and their constituents. The most active fraction was then analysed by GC-MS and LC-ESI-MS methods to identify the major constituents. Results. The ethyl acetate extract of C. fascicularis root bark (CFR2) showed a significant in vitro antibacterial activity. From the seven fractions of CFR2 obtained, fraction 2 (F2) had the lowest MIC value and was thus most active. Moreover, F2 was found to be more active compared to the four subfractions obtained from it. This suggested that constituents of F2 worked in synergy. Fraction 2 contained phenols, terpenes, and flavonoids. Two compounds were identified by GC-MS as 2,4-di-tert-butylphenol and (E,E)-2,4-decadienal, while three compounds were identified by LC-ESI-MS as tanshinone II A, cryptotanshinone, and danshensu. Conclusion. The study revealed that CFR2 is the most active extract on bacteria, suggesting that most antimicrobial compounds are concentrated in the roots of C. fascicularis. A follow-up study is directed towards chromatographic separations to obtain the other chemical constituents and screen them against various strains of bacteria.

Antibacterial Activities and Synergistic Effect of the Bioactive Compounds of Selected Medicinal Plants Against Diarrhoea-Causing Pathogens

In this study, the antimicrobial properties and toxicological effects of Anogeissus leiocarpus and Khaya senegalensis, two traditional medicinal plants from West Africa, were investigated against diarrhea-causing pathogens. Cold maceration was used to prepare extracts from the plants. Anogeissus leiocarpus yielded 22.87g of extract, while Khaya senegalensis yielded 13.94g. Both plant crude extracts exhibited varying degrees of antibacterial activity against Vibrio cholerae, Klebsiella pneumoniae, and Salmonella enterica serovar at different concentrations. A. leiocarpus and K. senegalensis showed the highest antibacterial activity, with significantly higher zones of inhibition at all concentrations against all test organisms. The Minimum Inhibitory Concentration (MIC) for A. leiocarpus ranged from 0.10 to 0.96 mg/mL, while the Minimum Bactericidal Concentration (MBC) ranged from 0.10 to 1.09 mg/mL. For K. senegalensis, MIC ranged from 0.96 to 1.80 mg/mL, and MBC ranged from 1.02 to 1.92 mg/mL. Fractionation of the most active crude extracts resulted in the highest yields in the n-Hexane fractions for both A. leiocarpus and K. senegalensis. Significant differences were observed in the antibacterial activity of these fractions. K. senegalensis fractions and A. leiocarpus n-Hexane fraction showed the highest activity against V. cholerae, while the ethyl acetate fraction of K. senegalensis exhibited significant activity against K. pneumoniae. The aqueous fraction of A. leiocarpus displayed the highest activity against Salmonella, whereas none of the K. senegalensis fractions were active against Salmonella. Antibacterial activity of K. senegalensis ethyl acetate and A. leiocarpus n-Hexane and aqueous column chromatography fractions against the test organisms was concentration-dependent, with the highest antimicrobial activity observed at 200 mg/mL concentration. Importantly, there were no significant differences in the body weights of experimental animals across all groups. In conclusion, A. leiocarpus and K. senegalensis extracts and their fractions demonstrated promising antimicrobial properties against diarrhea-causing pathogens. These findings support their traditional medicinal use in West Africa and suggest their potential as natural remedies for combating bacterial infections.

Compatibility study of Duddingtonia flagrans conidia and its crude proteolytic extract

This study aimed to evaluate the concomitant use of the nematophagous fungus Duddingtonia flagrans (AC001) and its protease-rich crude extract for the in vitro control of Panagrellus sp., Haemonchus spp., and Trichostrongylus spp. The nematicidal tests were carried out on larvae of the free-living nematode Panagrellus sp. and infective larvae of the gastrointestinal parasitic nematodes of domestic ruminants (Haemonchus spp. and Trichostrongylus spp). Five experimental groups were set: (1) one control group (G1) and (4) four treated groups –G2 – active crude extract; G3 – denatured crude extract; G4 – fungus, and G5 – fungus + active extract. Plates were incubated at 28 ºC for 24 h followed by the recovery of the larvae using the Baermann technique. The results showed a lower recovery of Panagrellus sp. larvae in the experimental groups compared to the control group, as follows: 52 % (G2), 16 % (G3), 46 % (G4), and 77 % (G5). An even greater reduction (77 ± 5 %) occurred in the group (G5). In addition, the authors observed lower averages of L3 of Haemonchus spp. and Trichostrongylus spp. in the experimental groups compared to the control group, as follows: 59 % (G2), 0 % (G3), 86 % (G4), and 76 % (G5). In turn, there was a difference (p < 0.01) between (G5) and (G2). The results this study indicate a positive effect from the compatible use of the D. flagrans fungus and its enzymatic crude extract (protease), which has been demonstrated here for the first time and with potential field applications for further designs.

Xylanase Production by Solid-State Fermentation for the Extraction of Xylooligosaccharides from Soybean Hulls§.

The development of a novel process for the production of xylooligosaccharides (XOS) based on the 4R concept is made possible by the integration of numerous techniques, especially enzymatic modification together with the physical pretreatment of renewable materials. This study aims to integrate the use of agricultural wastes for the production of xylanase by a new strain of Penicillium sp. and value-added products, XOS. For the production of xylanase, a solid-state fermentation was performed using wheat bran as substrate. To obtain the most active crude extract of xylanase, the time frame of cultivation was first adjusted. Then, the downstream process for xylanase purification was developed by combining different membrane separation units with size exclusion chromatography. Further characterisation included determination of the optimal pH and temperature, determination of the molecular mass of the purified xylanase and analysis of kinetic parameters. Subsequently, the hydrolytic ability of the partially purified xylanase in the hydrolysis of alkali-extracted hemicellulose from soybean hulls was investigated. Our results show that Penicillium rubens produced extracellular xylanase at a yield of 21 U/g during solid-state fermentation. Using two ultrafiltration membranes of 10 and 3 kDa in combination with size exclusion chromatography, a yield of 49 % and 13-fold purification of xylanase was achieved. The purified xylanase (35 kDa) cleaved linear bonds β-(1→4) in beechwood xylan at a maximum rate of 0.64 μmol/(min·mg) and a Michaelis constant of 44 mg/mL. At pH=6 and 45 °C, the purified xylanase showed its maximum activity. The xylanase produced showed a high ability to hydrolyse the hemicellulose fraction isolated from soybean hulls, as confirmed by thin-layer chromatography. In the hydrothermally pretreated hemicellulose hydrolysate, the content of XOS with different degrees of polymerisation was detected, while in the non-pretreated hemicellulose hydrolysate, the content of xylotriose and glucose was confirmed. Future research focusing on the creation of new enzymatic pathways for use in processes to convert renewable materials into value-added products can draw on our findings.

A moderately active crude methanol extract from the whole plant of Kalanchoe crenata (Andrews) Haw. (Crassulaceae) strongly potentiated the effect of antibiotics against multidrug-resistant Gram-negative bacteria

Background: Resistant bacteria develop a high level of resistance to multiple drugs, limiting treatment options and increasing morbidity and mortality. This work was planned to evaluate the antibacterial potential of the methanol extract from the whole plant of Kalanchoe crenata (KCW) against multidrug-resistant (MDR) Gram-negative bacteria. Methods: The minimal inhibitory concentrations (MIC) and the minimal bactericidal concentrations (MBC) of KCW alone, in the presence of an efflux pump inhibitor (EPI) phenylalanine-arginine β-naphthylamide (PAβN), or in the presence of antibiotics were assessed using the broth microdilution method combined with the rapid para-iodonitrotetrazolium chloride (INT) colorimetric technique. Results: KCW displayed weak antibacterial activities with MIC values ranging from 128 to 1024 μg/mL against 10 of the 15 tested bacterial strains. Moderate antibacterial activities with MIC values ranging from 128-625 μg/mL were recorded against some strains belonging to Klebsiella pneumoniae, Escherichia coli, and Providencia stuartii. PAβN does not significantly enhance the activity KCW. At MIC/2, KCW potentiated the activity of doxycycline (DOX), levofloxacin (LEV), imipenem (IMI), ciprofloxacin (CIP), ceftriaxone (CRO), and tetracycline (TET) against at least 80% of the MDR bacterial strains tested. Conclusion: The present study demonstrated that KCW is a moderately active antibacterial agent, but a good efflux pump inhibitor that could potentiate the activity of antibiotics against MDR bacteria over-expressing active efflux pumps. Keywords: Antibacterial; antibiotic-potentiation; Crassulaceae; efflux pumps; Kalanchoe crenata; multidrug resistance.

Metabolomics-guided identification of compounds with antibacterial and antioxidant activities from Polygonatum sibiricum-derived endophytic fungi

BackgroundInfections caused by multidrug resistant bacterial pathogens have been recognized as major global healthcare threat to medicinal, agricultural and pharmaceutical industries by World Health Organization. In this regard, the present study was aimed to isolate endophytes from medicinal plant Polygonatum sibiricum (P. sibiricum) and to investigate their antibacterial efficacy, radical scavenging ability and chemical fingerprinting using Gas Chromatography–Mass Spectrum (GC–MS) analysis.ResultsTwo endophytic fungi Talaromyces assiutensis HJ.14 (T. assiutensis) and Fusarium oxysporum HJ.15 (F. oxysporum) were isolated and identified from the rhizomes of P. sibiricum. Among the extracts screened, ethyl acetate extract of F. oxysporum HJ.15 showed maximum antibacterial activity with the zones of inhibition ranging from 10.98 ± 0.19 to 15.66 ± 1.49 mm and the MIC values ranging from 0.24 to 1.88 µg/mL against the tested bacterial pathogens. In addition, it showed significant antioxidant activity with EC50 values of 6.21–17.97 µg/mL. Further, GC–MS analysis revealed the presence of propanoic acid ethyl ester, hexadecanoic acid methyl ester, hexadecanoic acid ethyl ester, 9-Octadecenoic acid (Z)-methyl ester, 1-Octanol, 2-Undecenal, butanoic acid, 3-hydroxy- and hexanoic acid were the most abundant compounds in the active crude extract which was responsible for the significant antibacterial and antioxidant properties.ConclusionsIn summary, our results clearly suggest that the F. oxysporum HJ.15 will be a promising starting point for the isolation of active antibacterial compounds with antioxidant properties.

The Genus Dacryodes Vahl.: Ethnobotany, Phytochemistry and Biological Activities.

Dacryodes Vahl. species, belonging to the Burseraceae family, are widely used in traditional medicine in tropical regions to treat a range of ailments including malaria, wounds, tonsillitis, and ringworms. This review discusses the distribution, ethnobotanical uses, phytochemistry, and bioactivities of Dacryodes species. The intent is to spur future research into isolating and identifying key active principles, secondary metabolites, and crude extracts, and evaluating their pharmacological and toxicological effects, as well as the mechanism of actions to understand their medicinal benefits. A systematic review of scientific electronic databases from 1963 to 2022 including Scifinder, Scopus, Pubmed, Springer Link, ResearchGate, Ethnobotany Research and Applications, Google Scholar, and ScienceDirect was conducted with a focus on Dacryodes edulis (G.Don) H.J. Lam and Dacryodes rostrata (Blume) H.J. Lam. Pharmacological data revealed that D. edulis isolates contain secondary metabolites and other phytochemical groups belonging to the terpenoids class with anti-microbial, anticancer, antidiabetic, antiinflammatory and hepatoprotective activities, highlighting its pharmacological potential in the therapy or management of diverse cancers, cardiovascular, and neurological diseases. Thus, phytochemicals and standardized extracts from D. edulis could offer safer and cost-effective chemopreventive and chemotherapeutic health benefits/regimen, or as alternative therapeutic remedy for several human diseases. Nevertheless, the therapeutic potential of most of the plants in the genus have not been exhaustively explored with regard to phytochemistry and pharmacology, but mostly complementary approaches lacking rigorous, scientific research-based knowledge. Therefore, the therapeutic potentials of the Dacryodes genus remain largely untapped, and comprehensive research is necessary to fully harness their medicinal properties.

Relationship between pyroptosis and cardiovascular diseases and traditional Chinese medicine prevention and treatment research

Pyroptosis is a programmed cell death initiated by the activation of caspases, which is involved in the development and progression of several cardiovascular diseases. The gasdermins, a protein family, are key executive proteins in the development of pyroptosis, which increase cell membrane permeability, mediate the release of inflammatory factors, and aggravate the inflammatory injury. Traditional Chinese medicine(TCM)has shown unique therapeutic advantages in cardiovascular diseases with multi-component and multi-target characteristics. Currently, the effective prevention and treatment of cardiovascular diseases based on the theory of pyroptosis become a new research hotspot in this field. Based on the theories of TCM and modern medicine, this study summarized the role of pyroptosis in cardiovascular diseases such as atherosclerosis, myocardial infarction, diabetic cardiomyopathy, hypertension, and myocarditis. The role of TCM, including active monomers, crude extracts, and compound preparations, in cardiovascular protection through the regulation of pyroptosis was also summarized, providing a theoretical basis for the clinical prevention and treatment of cardiovascular diseases by TCM.

Promising antioxidant activity of crude extract from Calliandra tweedii Benth

The interest in medicinal plants encourages new research studies on plant extracts, as they are sources for treatments in medicine, agriculture, and veterinary. Calliandra tweedii is a native Brazilian species with broad use in folk medicine. This study aimed to examine the leaf crude extract (CE) of C. tweedii and its methanolic (MP) and hexane (HP) phases concerning total phenolic compounds (TPC), proanthocyanidins (PRO), and flavonoid profile, and correlate it to their antioxidant activity (DPPH and FRAP). CE and MP revealed high contents of TPC, PRO and high antioxidant activity (DPPH and FRAP) in relation to HP. Contrarily, HP showed reduced antioxidant activity, according to the scarce phenolic constituents obtained from the partition. Five flavonols were detected by HPLC-UV-DAD, being quercitrin the major constituent. Also, one kaempferol derivate and a series of three quercetin derivates were detected. Strong positive correlations were observed between DPPH, FRAP, and phenolic compounds. These discoveries are important to highlight the promising antioxidant activity of CE of C. tweedii, which could contribute to the expansion of popular herbal medicines and new drug discovery.

Identification of Novel Sphydrofuran-Derived Derivatives with Lipid-Lowering Activity from the Active Crude Extracts of Nocardiopsis sp. ZHD001.

Lipid-lowering is one of the most effective methods of prevention and treatment for cardiovascular diseases. However, most clinical lipid-lowering drugs have adverse effects and cannot achieve the desired efficacy in some complex hyperlipidemia patients, so it is of great significance to develop safe and effective novel lipid-lowering drugs. In the course of our project aimed at discovering the chemical novelty and bioactive natural products of marine-derived actinomycetes, we found that the organic crude extracts (OCEs) of Nocardiopsis sp. ZHD001 exhibited strong in vivo efficacies in reducing weight gain, lowering LDL-C, TC, and TG levels, and improving HDL-C levels in high-fat-diet-fed mice models. Chemical investigations of the active OCEs led to identifying two new sphydrofuran-derived compounds (1-2) and one known 2-methyl-4-(1-glycerol)-furan (3). Their structures were elucidated by the analysis of HRESIMS, 1D and 2D NMR spectroscopic data, and ECD calculations. Among these compounds, compound 1 represents a novel rearranged sphydrofuran-derived derivative. Bioactivity evaluations of these pure compounds showed that all the compounds exhibited significant lipid-lowering activity with lower cytotoxicity in vitro compared to simvastatin. Our results demonstrate that sphydrofuran-derived derivatives might be promising candidates for lipid-lowering drugs.

Staphylococcus aureus antibiofilm agents from Combretum species (Combretaceae) by metabolomics profiling

About 80 % of all chronic bacterial infections are related to biofilms. Among several bacteria capable of developing biofilms, Staphylococcus aureus and Pseudomonas aeruginosa are recognized as two major opportunistic pathogens associated with biofilm infections, especially those related to medical devices. In light of the exciting progress of metabolomics within the field of natural products, and given the pressing need for new alternatives to control bacterial pathogens, this study applied metabolomic profiling and statistical analyses to identify S. aureus or P. aeruginosa biofilm inhibitors from three Brazilian Combretum species. The extracts were obtained from leaves and bark of C. leprosum, C. laxum, and C. lanceolatum, by solvent extraction with hexane (Hx), dichloromethane (Dcm), and hydromethanolic (Me70). Me70 extracts from leaves of all tested species were active against S. aureus biofilm formation (inhibition rate of 92 % for C. lanceolatum, 80 % for C. leprosum, and 65 % for C. laxum), but they did not inhibit bacterial growth. Other extracts from C. leprosum also presented similar results, decreasing S. aureus biofilm formation without affecting cell growth (inhibition of 90 % for bark Me70 extract, 72 % for bark Dcm extract, and 69 % for leaf Hx extract). Dcm extract from C. leprosum leaves decreased biofilm formation in 69 % while having antibacterial activity (85 % inhibition of bacterial growth). None of the extracts were active against P. aeruginosa. Metabolomic analysis by LC-MS followed by statistical evaluation clearly evidenced chemical differences associated with the activity level of the extracts. Univariate analysis by Pearson's r correlation suggested thirty-five metabolites with positive correlation with S. aureus antibiofilm activity, including alkaloids, tannins, phenolic acids, sugars, and glycosylated and non-glycosylated flavonoids. We obtained in vitro confirmation that ellagic acid is a key component for antibiofilm activity by Combretum extracts against S. aureus, showing circa 70% inhibition. It is likely that ellagic acid prevents bacterial-material surfaces interaction, since it led to increased hydrophobicity in S. aureus surface at the same concentrations that affected biofilm formation (up to 0.1563 µM). Importantly, ellagic acid, and the 4 most active Combretum crude extracts, are not toxic as determined using Galleria mellonella larvae model. The lower selective pressure toward bacterial resistance is an attractive feature of antibiofilm agents compared with antibiotics. Their identification will contribute to the development of novel anti-infective strategies, including less prone adherent surfaces, with a direct impact on the reduction of infections associated with medical devices.

In vitro antiplasmodial, molecular docking and pharmacokinetics studies of specialized metabolites from Tetrapleura tetraptera (Fabaceae)

Tetrapleura tetraptera is a well-known plant widely used in Cameroon as spices in cooking and in preparations prescribed in folk medicine for the treatment of malaria. The main purpose of this study was to provide relevant chemical and pharmacological insights that can support the effectiveness of T. tetraptera against malaria by identifying the lead compounds that may be responsible for its therapeutic potential. The stem bark and root methanolic crude extracts of this plant displayed a good inhibition of P. falciparum 3D7 with rates of 83.6% and 76.3%, respectively. A total of sixteen distinct compounds (1‒16) have been isolated during the chemical investigations of the two active crude extracts. Their structures were established with the aid of their NMR data. Thriteen compounds (2‒9, 11‒13, 15 and 16) were screened for antiplasmodial activity using P. falciparum 3D7. Results showed that seven tested compounds displayed good activity (IC50 < 7 μM) and the most effective were compounds 5, 9, 7, 2 and 6 with IC50 values of (1.8 ± 0.4 μM), (1.9 ± 0.8 μM), (2.1 ± 0.5 μM), (2.3 ± 0.7 μM), (2.4 ± 0.6 μM), respectively. The in silico evaluation of the isolated compounds for their ability to inhibit the P. falciparum dihydroorotate dehydrogenase 5TBO and their ADMET studies revealed that up to fifteen isolated compounds displayed a greater affinity to the binding site of the 5TBO receptor compared to the reference drug chloroquine. More especially, compounds 1, 2, 4, 8 and 14 demonstrated a good drug-likeness. These findings support the use of T. tetraptera for the management of malaria and further qualify it as an important source of good candidates in new antiplasmodial drug development.

Structural Elucidation and Antibacterial Activity Studies of Leaf Extracts of &lt;i&gt;Withania somnifera&lt;/i&gt;

Withania somnifera (W. somnifera), a small, woody shrub in the Solanaceae family, has been studied using a phytochemical test, antibacterial activity and partial characterizations. Air-dried and powdered leaves of the plant were extracted with maceration over an electrical shaker using the solvent chloroform and methanol. After crude extracts of the plant were concentrated, the diffusion antibacterial susceptibility test was carried out on 25, 50, 75, and 100 mg/mL of chloroform and methanol crude extract. The bacteria used were S. aureus, S. pneumonia, E. coli, and S. typhi. Each antibacterial activity test was carried out three times. The most active crude extract of the plant was subjected to a phytochemical test and fractionation with column chromatography. Chloroform and methanol extract of the plant inhibits all cultures of four bacteria. Both chloroform and methanol extract of W. Somnifera inhibits both gram-positive and negative bacterium with a comparable inhibition zone with the standard antibiotics, amoxicillin, gentamicin, and cefoxitine. In addition, it gives a maximum inhibition zone than that of amoxicillin, starting from 25 to 100 mg/mL. Methanol extract of W. somnifera contains phenolic, alkaloids, flavonoids, tannins, and phytosteroids. Partial characterization of pure fractions by using 1H-NMR, 13C-NMR, Dept-135 NMR, and IR spectroscopy, the compound WS-1 affords withaferin A. Withaferine A shows antibacterial activity with an inhibition zone of 11, 10.5, 11, and 9 mm against the bacterium S. aureus, S. pneumoniae, E. coli, and S. typhi respectively.