Active Ethyl Acetate Research Articles

Anti- psoriatic effect and phytochemical evaluation of Iraqi Scabiosa palaestina ethyl acetate extract

The purpose of this study was to confirm the antipsoriasis activity of Scabiosa palaestina (S. palaestina) ariel component extract and identify the active compound(s) responsible for this activity using a developed RP-HPLC technology. The active ethyl acetate extract of S. palaestina was extracted and fractionated by the hot continuous Soxhlet apparatus method. Psoriasis was induced in experimental animals after 4 days of imiquimod (IMQ) cream application on dorsal skin rats of 3 treated groups (6 rats for each) and the normal group (6 rats) left without treatment. Two of the psoriatic-induced groups were treated with ethyl acetate (EA) extract or methotrexate (MTX) for 12 days, starting from day 4 of the IMQ application. Assessment of psoriatic lesions was done during the experiment, depending on the psoriasis area severity index (PASI). At the end of the study (day 15), animals were sacrificed and 2 skin specimens were collected for histopathological examination and cytokine measurement. Compared with the positive control group, ethyl acetate extract shows significant improvement in PASI (p-value < 0.05) and histopathological changes exerted by IMQ. On the other hand, no significant reduction has been seen in the psoriatic and angiogenic mediator (IL-17 and VEGF) with a P-value > 0.05 compared with the positive control group, which may be attributed to other cytokines that could be affected by the ethyl acetate extract of S. palaestina. These results suggest that the antipsoriasis properties of ethyl acetate extract may possibly be due to the presence of flavonoid compounds (luteolin, apigenin, quercetin, vitexin and kaempferol).

Preliminary Study to Assess the Antioxidant and Antibacterial Activity of Extracts from the Leaves of Morelia Senegalensis (A Rich)

frican populations rely heavily on traditional medicine, which uses plants to treat human and animal diseases. However, scientific validation of this empirical knowledge concerning the efficacy, toxicity and dosage of the proposed treatments is urgently needed. The aim of this study was to evaluate the antioxidant and antibacterial activity of Morelia senegalensis leaf extracts on the 2,2-diphenyl-1-picrylhydrawyl (DPPH) radical and the (2,2’-azino-bis-(3-ethylbenzothiazoline-6-sulfonic) acid) ABTS cation radical and on four reference bacterial strains (E. coli 25922, E. coli 35218, E. faecalis 29212 and S. aureus 29213) using protocols already described in the literature. The phytochemical screening test revealed the presence of flavonoids, alkaloids, tannins, saponins, reducing compounds and sterols in Morelia senegalensis leaves. All the extracts showed antioxidant activity to varying degrees. The most active ethyl acetate (AE) extract had half-maximum inhibition concentration (IC50 )of 0.33 and 0.62 mg/mL for the ABTS and DPPH tests respectively, followed by DCM and EB extracts with IC50 of 0.86 and 0.88 mg/mL for the ABTS test respectively, while the vitamin C used as a reference was more active with IC50 of 0.04 and 0.06 mg/mL. Antibacterial activity showed inhibition diameters ranging from 7 to 16 mm depending on the concentration and strain considered. The ethyl acetate fraction was the most active on S aureus 29213 with an inhibition diameter of 16 mm at 50 mg/mL. These interesting results were confirmed by the Minimal Inhibitory Concentration inhibitory (MIC) and Minimal Bacterial Concentration (MBC) studies, which showed that all the extracts had a bactericidal effect on all the studied strains. Morelia senegalensis plant has shown promising preliminary results in the treatment of bacterial infections. Further studies are needed to isolate and characterize the secondary metabolites contained in the leaves of this plant.

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.

Further Polycyclic Quinones of Micromonospora sp.

The crude acetone extract of a marine Micromonospora sp. strain associated with Eudistoma vannnamei was fractioned with hexane and ethyl acetate. The crude extract and both soluble fractions were assayed against several bacteria strains. The new polycyclic quinones 12-hydroxy-9-propyltetracene-6,1-dione (1), 5,12-dihydroxy-4-methoxy-9-propyltetracene-5,12-dione (2), and 4,6-dihydroxy-3-methoxycarbonyl- methyl-6a-(oxobutyl)-5,12-anthraquinone (3), along with the known 4,6-dihydroxy-3-methoxycarbonyl-methyl-6a-(oxo-3-methyl-butyl)-5,12-anthraquinone (4) and 4,6-dihydroxy-3-methoxycarbonyl-methyl-6a-(oxopentyl)-5,12-anthraquinone (5) were isolated from the hexane-soluble fraction, while from the active ethyl acetate fraction were isolated the known 4,6,11-trihydroxy-9-propyltetracene-5,12-dione (6), 4-methoxy-9-propyltetracene-6,11-dione (7), 7,8,9,10-tetrahydro-9-hydroxy-4-methoxy-9-propyltetracene-6,11-dione (8), and 10β-carbomethoxy-7,8,9,10-tetrahydro-4,6,7α,9α,11-pentahydroxy-9-propyltetracene-5,12-dione (9). The structures of the new compounds were established by interpretation of HRMS and NMR techniques. A study of molecular docking was performed with the compounds from the active ethyl acetate fraction to correlate tentatively with the antimicrobial activity. Molecular docking, RMSD, RMSF, and MM-GBSA evaluations were performed to investigate the inhibitory activity of 6-8 against the protein PDB-codex 1MWT, being considered a promising target for studying drug development responsible for inhibiting replication of Staphylococcus aureus. Penicillin G was used as the standard inhibitory. Anthracyclinones 6-8 were the best hydrolase inhibitor with affinity energy -8.1 to -7.9 kcal/mol compared to penicillin G, which presented -6.9 kcal/mol. Both 8 and 7 present potent inhibitory effects against hydrolase through molecular dynamics simulation and exhibit favorable drug-like properties, promising new hydrolase blockers to fight bacterial infections from Staphylococcus aureus.

Aaptamine-rich Fraction from the Indonesian Marine Sponge, Aaptos suberitoides, Exhibits a Cytotoxic Effect on DLD-1 Colorectal Cancer Cells.

This study aimed to investigate the cytotoxicity effect of the ethyl acetate extract of Aaptos suberitoides on colorectal cancer cells (DLD-1) and murine fibroblast cells (NIH-3T3). A. suberitoides was collected from Putus Island, Bunaken National Park, North Sulawesi, Indonesia, and was processed with maceration and ethyl acetate extraction. The sponge extract was characterized based on Thin Layer Chromatography (TLC) and then identified by using LCMS/MS analysis. DLD-1 and NIH-3T3 cells were treated with the ethyl acetate extract and then followed by 3- [4, 5-dimethylthiazol-2-yl] -2.5 diphenyl tetrazolium bromide (MTT) assay to assess their cytotoxicity effect. LCMS/MS analysis showed that the most abundant compounds in this extract were identified as aaptamine (1). Furthermore, this study revealed that the active ethyl acetate fraction of A. suberitoides has cytotoxic effects in colorectal cancer DLD-1 cells with an IC50 value of 9.597 µg/mL, higher than NIH-3T3 cells with an IC50 value of 12.23 µg/mL Thus, the active ethyl acetate fraction of A. suberitoides is considered more toxic to cancer cells than normal cells. This study provides the first evidence to support the role of the ethyl acetate extract of A. suberitoides sponge extracts to be developed as a colorectal anticancer agent.

Miliutine C methyl ester, a new drimane sesquiterpene and bioactive alkaloids from the stems of Miliusa velutina

Previous results from the our research group have isolated numerous compounds, including novel ones, but the anticancer activity of Miliusa velutina has not been demonstrated. In this study, from the most active ethyl acetate extract of the stems of Miliusa velutina, seven compounds were isolated and determined structures, including a new drimane sesquiterpenoid compound named miliutine C methyl ester (1) and three bioactive alkaloids (5-7). These three alkaloids (5-7) exhibited strong anticancer activities against various cancer cell lines such as MCF-7, HepG2, HeLa, NCI H460 and normal fibroblasts. Especially, on MCF-7 and normal fibroblasts with values of IC50 (μM) in order for compounds 5 (3.38, 31.15), 6 (21.96, 102.00), 7 (7.90, greater than 300), to compare with positive control camptothecin (0.020, 4.51); which is highly noteworthy. These results contribute to elucidating and confirming the value of Miliusa velutina, similar to other published and folkloric findings.

Free radical scavenging polyphenols isolated from Phyllanthus niruri L. ameliorates hyperglycemia via SIRT1 induction and GLUT4 translocation in in vitro and in vivo models

Type 2 diabetes milletus (T2DM) is a complex multifaceted disorder characterized by insulin resistance in skeletal muscle. Phyllanthus niruri L. is well reported sub-tropical therapeutically beneficial ayurvedic medicinal plant from Euphorbiaceae family used in various body ailments such as metabolic disorder including diabetes. The present study emphasizes on the therapeutic potential of Phyllanthus niruri L. and its phytochemical(s) against insulin resistance conditions and impaired antioxidant activity thereby aiding as an anti-hyperglycemic agent in targeting T2DM. Three compounds were isolated from the most active ethyl acetate fraction namely compound 1 as 1-O-galloyl-6-O-luteoyl-β-D-glucoside, compound 2 as brevifolincarboxylic acid and compound 3 as ricinoleic acid. Compounds 1 and 2, the two polyphenols enhanced the uptake of glucose and inhibited ROS levels in palmitate induced C2C12 myotubes. PNEAF showed the potent enhancement of glucose uptake in palmitate-induced insulin resistance condition in C2C12 myotubes and significant ROS inhibition was observed in skeletal muscle cell line. PNEAF treated IR C2C12 myotubes and STZ induced Wistar rats elevated SIRT1, PGC1-α signaling cascade through phosphorylation of AMPK and GLUT4 translocation resulting in insulin sensitization. Our study revealed an insight into the efficacy of marker compounds isolated from P. niruri and its enriched ethyl acetate fraction as ROS scavenging agent and helps in attenuating insulin resistance condition in C2C12 myotubes as well as in STZ induced Wistar rat by restoring glucose metabolism. Overall, this study can provide prospects for the marker-assisted development of P. niruri as a phytopharmaceutical drug for the insulin resistance related diabetic complications.

Isolation of Biomolecules from the Leaves of Lecaniodiscus cupanoides (Sapindaceae), a Plant used in Traditional Medicine in Benin

The aim of the present study was to identify the structure of the bioactive molecules in the active ethyl acetate fraction of the hydroethanolic extract of Lecaniodiscus cupanoides (Sapindaceae), a Beninese plant used in the treatment of microbial infections. We prepared the hydroethanolic extract from powdered dried leaves. We fractionated the hydroethanol extract using the liquid-liquid extraction method with solvents of increasing polarity. The active ethyl acetate fraction obtained after bioguided fractionation of the hydroethanol extract on bacterial strains was purified by a series of atmospheric pressure column chromatographic methods coupled with thin layer chromatography. At the end of this purification process, three compounds, including a flavonoid and two fatty acids, were isolated and identified by interpretation of 1H NMR, 13C NMR and mass spectrometry spectra. These were: 2-(3,4-dihydroxyphenyl)-3,5,7-trihydroxy-2,3-dihydrochromen-4-one;(E)-3-(3,4-dihydroxyphenyl)-2-(3-(3,4-dihydroxyphenyl) acryloyloxy) propanoic acid and (E)octadec -9- enoic acid (oleic acid).
 The added value of this work lies in the fact that these three molecules have never before been identified in this plant, and therefore represent a potential avenue for the development of a therapeutic arsenal to combat microbial infections.

Limosilactobacillus reuterias sustainable biological control agent against toxigenic Fusarium verticillioides.

Corn contamination with Fusarium verticillioides (Sacc.) Nirenberg is a worldwide problem that affects yield and grain quality resulting in severe economic losses and implications for food safety. Control of F. verticillioides is a challenge, but lactic acid bacteria (LAB) has high potential as a biological control agent. In this study, the antifungal effect of Limosilactobacillus reuteri (formerly Lactobacillus reuteri) LR-92 against F. verticillioides 97L was investigated. Cell-free supernatant (CFS) from L. reuteri showed concentration-dependent fungicidal and fungistatic activity against F. verticillioides 97L. The antifungal compounds from CFS showed heat stability and pH dependence, and antifungal activity was not affected by treatment with proteolytic enzymes. High-performance liquid chromatography analysis indicated that L. reuteri LR-92 produces lactic and acetic acids. After liquid-liquid extraction, electrospray ionization mass spectrometry analysis of the active ethyl acetate fraction containing antifungal compounds revealed the production of 3-phenyllactic acid, cyclo-(L-Pro-L-Leu), cyclo-(L-Pro-L-Phe), and cyclo-(L-Phe-trans-4-OH-L-Pro). L. reuteri LR-92 has potential as a biocontrol agent for F. verticillioides and contributes to food safety.

A potent bioactive fraction against colon cancer from Plectranthus vettiveroides.

This study was designed to investigate the anticancer efficacy of the organic leaf extracts of the plant, Plectranthus vettiveroides (P. vettiveroides), and to analyze the molecular mechanism of the anticancer activity. The leaf extracts were prepared by polarity-graded serial extraction of the dried leaf powder. The cytotoxic effect of the extracts was analyzed by the 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay. The most active ethyl acetate extract was subjected to bioactivity-guided fractionation by column chromatography, which yielded a cytotoxic fraction designated as the P. vettiveroides fraction (PVF). The anticancer property of PVF was confirmed further by clonogenic assay. The mechanism of PVF-induced cell death was analyzed by flow cytometry and fluorescence microscopy. Additionally, the effects of PVF on apoptotic and cell survival pathways were analyzed using western immunoblot analysis. A bioactive fraction PVF, was isolated from the ethyl acetate leaf extract. PVF showed significant anticancer activity against colon cancer cells, whilst normal cells were comparatively less affected. PVF induced strong apoptotic stimuli in colorectal carcinoma cell line HCT116, involving both extrinsic and intrinsic pathways. Investigation into the molecular mechanism of anticancer activity of PVF in HCT116 cells revealed that the fraction activates the pro-apoptotic pathway via tumor suppressor protein 53 (p53) and inhibits the anti-apoptotic pathway by regulating phosphatidylinositol 3-kinase (PI3K) signaling. The findings of this study demonstrate, with mechanism-based evidence, the chemotherapeutic potential of a bioactive fraction PVF, derived from the leaves of the medicinal plant P. vettiveroides against colon cancer.

EVALUATION OF DOPAMINERGIC ACTIVITY OF BIOLOGICALLY ACTIVE SUBSTANCES OF VERBENA HERB (VERBENA OFFICINALIS L.)

Relevance. The development of herbal medicines remains relevant today. Verbena officinalis L. has a spectrum of pharmacological activity, but our interest is manifested in its ability to treat amenorrhea and anovulation in hyperprolactinemia. The purpose of the work was to study the dopaminergic activity of the extract, fractions and dominant substances of the verbena officinalis herb. Materials and methods. The object of the study is the verbena officinalis herb, harvested experimentally in the field of the Botanical Garden of the Federal State Budgetary Scientific Institution VILAR in 2019. Results. The dopaminergic activity of fractions of different polarity of herb verbena officinalis was assessed. The most active absorb ethyl acetate fraction, which includes: verbenalin and verbascoside. Verbenalin has been found to have a dopaminergic effect. Dopaminergic activity of the total ex-tract, ethyl acetate fraction and inflammation verbenalin. Conclusions. It is expedient to develop drugs for the treatment of amenorrhea and anovulation based on a total extract standardized for verbenalin.

PHYTOCHEMICAL INVESTIGATION, FT-IR PROFILING AND ANTIBACTERIAL ACTIVITY OF PAPAYA (VAR. RED LADY) PEEL- A RICH SOURCE OF BIOACTIVE CHEMICALS

Fruit wastes are produced in huge quantities which constitute a source of pesterer in the environment due to their highbiodegradability. To explore the potential of fruit waste as natural resources of bioactive compounds the present studyinvestigate the qualitative and quantitative analysis of phytochemicals, FT- IR fingerprinting and antimicrobial activity ofpetroleum ether, ethyl acetate, ethanol and water extracts of papaya peel collected from variety red lady. The qualitativephytochemical investigation of papaya peel extracts showed the presence of phenols, flavonoids, alkaloids, tannins,saponins, terpenoids and steroids, whereas in the estimation, total amount of phenols was high when compared toflavonoids. The FT-IR spectroscopic investigation showed the presence of characteristic peak values with different usefulmixtures of functional groups such as hydroxy group, aliphatic, carbonyl, alcohols, phenols, alkanes, ketones, carboxylicacids, amine and aromatics. Among the four extracts evaluated, ethyl acetate fraction showed more numbers offunctional groups. The ethyl acetate and ethanol extract displayed increased antibacterial activity in all tested bacterialstrains and found as better solvents for the isolation of the bioactive compounds from papaya peel. Highest zone ofinhibition (20mm) was showed by Gram negative bacterium Proteus mirabilis against synthetic antibiotic tetracycline(24mm).

Ciliatoside A, isolated from Peristrophe japonica, inhibits HBsAg expression and cccDNA transcription by inducing autophagy

Hepatitis B surface antigen (HBsAg) loss and seroconversion are considered as an end point of a functional cure. Therefore, it is crucial to find new agents which could efficiently decrease HBsAg. Traditional herbal plants have been considered as an important source of new hepatitis B drugs development for their extensive use in antimicrobial and anti-inflammation. In this study, Peristrophe japonica, which could remarkably reduce HBsAg in the supernatant of HepG2.2.15 cells, was screened out for further extraction. Here, an active ethyl acetate fraction of Peristrophe japonica containing 34 sub-fractions was extracted. Subsequently, the monomeric compound Ciliatoside A was isolated and identified as a potential antiviral reagent with low cytotoxicity from Fraction 30. Ciliatoside A exhibited strong inhibition on intracellular and circulating HBsAg and HBV RNAs in HBV-infected cells and an HBV recombinant-cccDNA mouse model. The mechanistic study revealed that Ciliatoside A exhibited a potent anti-HBV effect through inducing autophagy-lysosomal pathway to autophagic degradation of HBc by activating AMPK-ULK1 axis and inhibiting mTOR activation. In summary, we have identified a novel antiviral compound Ciliatoside A isolated from Peristrophe japonica. This study may provide important direction and new ideas for the discovery of hepatitis B cure drugs.

Bronchodilator Secondary Metabolites from Rhazya stricta Decne Aerial Parts

The plant kingdom comprises medicinally useful plants that have provided many new drugs used to treat various diseases. In our search for bronchodilator secondary metabolites from plants growing in Saudi Arabia, the total extract of Rhazya stricta showed activity against carbamylcholine- (CCh) induced bronchoconstriction in guinea pig tracheal muscles used as an ex vivo model. The fractions obtained from liquid–liquid extraction process were tested for bronchodilator effects. The most active ethyl acetate fraction (RS-E) and aqueous fraction (RS-H) were subjected to biologically guided phytochemical study using different stationary phases and chromatographic techniques to isolate the pure secondary metabolites. Five known compounds were isolated from the active fractions. Three alkaloids namely; (-)-quebrachamine (1), (+)-eburenine (2), (+)-stemmadenine (3) as well as the two iridoid glycosides loganic acid (4) and loganine (5) were identified by various spectroscopic methods. Among the isolated compounds 1 and 5 were the only active as bronchodilators in the plant. It is worth to mention that iridoid glycosides are isolated for the first time from R. stricta.

Biological evaluation, molecular modeling and dynamics simulation of phenanthrenes isolated from Bletillastriata as butyrylcholinesterase inhibitors

As part of our continuous studies on natural cholinesterase inhibitors from plant kingdom, the 95% ethanol extract from tubers of Bletillastriata showed promising butyrylcholinesterase (BChE) inhibition (IC50 = 8.6 μg/mL). The extracts with different polarities (petroleum ether, ethyl acetate, n-butanol, and water) were prepared and evaluated for their inhibition of cholinesterases. The most active ethyl acetate extract was subjected to a bioassay-guided isolation and afforded twenty-two bibenzyls and phenanthrenes (1–22). All isolates were further evaluated for their BChE inhibition activity, and five phenanthrenes presented promising capacity (IC50 < 10 μM). Further kinetic studies indicated their modes of inhibition. Compounds 6, 8, and 14 were found to be mixed-type inhibitors, while compounds 10 and 12 could be classified as non-competitive inhibitors. The potential interaction mechanism of them with BChE was demonstrated by molecular docking and molecular dynamics simulation, showing that they could interact with catalytic active site and peripheral anionic site of BChE. These natural phenanthrenes provide new scaffold for the further design and optimization, with the aim to discover new selective BChE inhibitors for the treatment of AD.

Melissa officinalis L. nanoethosomal formulation: evaluation of antioxidant, enzyme inhibitory activities and in vitro toxicity

ABSTRACT This work aimed to create an extract of Melissa officinalis L. with strong antiradical efficacy, characterize it, and enhance its long-term efficacy by developing an ethosomal formulation. DPPH and ABTS assays were used to test the antiradical activity of extracts with different ethanol ratios obtained from the aerial part. Phytochemical characterization of the extract with the highest activity, ethyl acetate fraction of 60% ethanol extract, was analyzed by HPLC. The active ethyl acetate fraction was loaded into ethosomes, and characterization and release studies of the formulation were performed. The released extract from the formulation exhibited substantial antiradical action as well as inhibition of collagenase (71.5%) and elastase (75.5%) enzymes. The toxicity of the active extract and the formulation was determined in the mouse fibroblast cell line. This study successfully developed a long-term antioxidant and enzyme inhibitor formulation containing M. officinalis, which stands out for its medicinal properties.

Isolation and characterization of β-sitosterol, oleanolic, 19- dehyroursolic and yarumic acids, from Plectranthus esculentus leaves and tubers

Plectranthus esculentus N.E.Br. (family Lamiaceae) also known as Livingstone potato (vat or rizga in Nigeria), is a dicotyledonous perennial shrub growing up to 2 m tall. While it is cultivated mainly for its edible tubers, the plant is potentially valuable as phytomedicine. Three varieties (vat-long’at, vat-riyom and vat-bebot) are well known among the Berom of Plateau State, Nigeria. The vat-bebot variety (which showed good promise in bioactivity studies) was used in this study. The leaves and tubers were extracted successively with hexane, ethyl acetate, methanol and water. Fractionation of the active ethyl acetate extracts was carried out using open column and preparative High Performance Liquid Chromatography (prep HPLC). This led to the isolation of β-sitosterol and oleanolic acid from the leaves; while 19-dehydroursolic acid and yarumic acid, as well as β-sitosterol were isolated from the tubers. Nuclear Magnetic Resonance (NMR) and Electron Impact Mass Spectroscopy (EIMS) were used to characterize isolated compounds. Comparing acquired spectral data of isolated compounds with those from literature helped to confirm the identity of the compounds. The isolation and characterisation of these compounds, from Plecthranthus esculentus, have not been hitherto reported in literature.

Antibacterial metabolites from an unexplored strain of marine fungi Emericellopsis minima and determination of the probable mode of action against Staphylococcus aureus and methicillin-resistant S. aureus.

Increasing prevalence of drug resistance has led researchers to focus on discovering new antibacterial agents derived from the marine biome. Although ample studies have investigated marine fungi for their bioactive metabolites with hopeful prospects in drug discovery. The present study was aimed to isolate/ identify potential antimethicillin-resistant Staphylococcus aureus compounds producing marine fungal strain from the Indian marine environment. The effective anti-MRSA compound was produced by a marine fungal strain designated as D6. The D6 strain exhibited 99% similarity to Emericellopsis minima based on 18S rRNA gene analysis. The culture conditions of E. minima D6 were optimized using nutritional and environmental parameters for enhanced anti-MRSA compound production. The agar well diffusion assay was used to determine the inhibition zone diameter of the crude extract against S. aureus and methicillin-resistant S. aureus, whereas the broth microdilution method was used to determine their minimum inhibitory concentration (MIC) active fraction. MIC values of the ethyl acetate fraction ranged from 0.8 to 1 mg/mL. SEM analysis revealed that the ethyl acetate fraction induces deep craters in methicillin-resistant S. aureus. Further, GC-MS analysis confirmed the occurrence of a total of 15 major compounds in active ethyl acetate fraction. Some of the major antibacterial compounds included cyclopentanol, isothiazole, benzoic acid, pyrrolo[1,2-a] pyrazine-1,4-dione, and hexahydro. These findings suggest that the marine fungi of E. minima can be a valuable candidate for prospecting antibiotics and an alternative complementary strategy for drug-resistant bacterial infections.

Anthelmintic and antimycobacterial activity of fractions and compounds isolated from Cissampelos mucronata

Ethnopharmacological relevanceCissampelos mucronata A. Rich., a perennial climber belonging to the family Menispermaceae, has been used traditionally to treat parasites and tuberculosis-related symptoms. Co-infection of helminth parasites and tuberculosis-causing pathogens heightens the risk of developing active tuberculosis. Aim of the studyThe aim was to isolate and characterize antimycobacterial compounds from Cissampelos mucronata and to investigate their antibiofilm and anthelmintic efficacy as well as cytotoxicity. Materials and methodsThe acetone extract of C. mucronata leaves and stems was fractionated by vacuum liquid chromatography using hexane, ethyl acetate, acetone and methanol:chloroform (3:7). Separation of the active ethyl acetate fraction by column and preparative thin layer chromatography led to the isolation and identification of five compounds using NMR and LC-MS, as well as GC-MS for non-polar compounds. The anthelmintic, antimycobacterial, antibiofilm, antioxidant and anti-inflammatory effects as well as cytotoxicity of the fractions and compounds were determined. ResultsThe ethyl acetate fraction had the best antimycobacterial activity (MIC = 0.015–0.08 mg/ml). The fractions were relatively non-toxic to Vero cells (0.03–0.79 mg/ml) and had good anti-inflammatory and antibiofilm effects. Five compounds were identified as stigmasterol, hentriacontane, simiarenol, nonacosene and carbonic acid. Nonacosene had moderate anthelmintic effects but poor antimycobacterial activity (MIC = 0.375 mg/ml). Nonacosene and hentriacontane had good biofilm inhibitory effect (90–100%). ConclusionsThis study reveals that C. mucronata is a potential source of promising compounds with a range of useful bioactivities that support its use in traditional medicine. Development of plant-based remedies may assist in reducing the impact of co-infections with helminth parasites and tuberculosis-causing mycobacteria.

Antibacterial Activity of Ethyl Acetate and Cream Formulation of Coleus atropurpureus leaves Against Staphylococcus aureus

Infectious diseases caused by Staphylococcus aureus (Sa) bacteria reaching 70% of cases in Asia and can attack and survive in epithelial cells including endothelial cells. Attempts to overcome the infection caused by Sa by giving antibiotics, which work as antibacterial. Myana (Coleus atropurpureus L. Benth) leaves contain several active compounds that might act as antibacterial agents. This study aimed to analyze the antibacterial activity of Coleus Extract in vitro and to evaluate the formulation of the extract cream against the bacteria causing infection, Sa. Coleus leaves ethyl acetate extract contains alkaloids and tannins, the absorbance of Sa at the 3rd hour was getting smaller, from 0.668 to 0.552, this showed that the longer the incubation time of the extract against bacterial inoculation, the more bacteria died. Our cream formulation with criteria: the pH value, homogeneity, spreadability, adhesion, and protection power. Our cream formulation results were then evaluated based on the standard, with criteria: the pH value, homogeneity, spreadability, adhesion, and protection power. It seems that our cream is per the cream standards. It is semi-solid, brownish-white in color, smells typical of Coleus, and pH 6. Moreover, the cream is homogeneous with 5 cm of spreadability, 7 seconds for adhesion, and colorless. Moreover, we found that Coleus extract cream has better antibacterial activity than positive control with a wound closure time of 7-14 days for extract while more than 14 days for positive control.