Activity Of Ethyl Acetate Extracts Research Articles

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.

Phenolic compounds and antifungal activity of ethyl acetate extract and methanolic extract from Capsicum chinense Jacq. ripe fruit.

Food loss due to contamination caused by fungi has much impact on agriculture and leads to significant economic losses. Synthetic and natural fungicides have been used for avoiding losses of several food products due to fungal contamination. As a result, species of the genus Capsicum have been used for preserving food because of their chemical compounds with antifungal activity. Therefore, this study aimed at identifying some phenolic compounds found in both ethyl acetate extract (EAE) and methanolic extract (ME) from habanero pepper (C. chinense) ripe fruit by liquid chromatography tandem mass spectrometry with electrospray ionization (LC-ESI-MS/MS) and at evaluating their antifungal activities against fungi Sclerotinia sclerotiorum, Rhizopus stolonifer and Colletotrichum gloeosporioides. Extracts resulted from a sequential process of maceration. Antifungal activity was evaluated by the disk diffusion method (DDM) at the following doses of both diluted extracts: 25 µL, 50 µL, 100 µL and 200 µL. The chemical analysis showed that there were protocatechuic acid, gentisic acid, vanillic acid, kaempferol-3-O-robinobiosideo and naringenin in both extracts. EAE showed high inhibition of mycelial growth at both doses 100µL and 200µL against the three fungi while methanolic exhibited weak activity even at the highest dose under investigation. However, further in-depth studies are needed to reinforce their uses and practical applications to the agricultural field.

Uji Aktivitas Sel Kanker Payudara T47D Ekstrak Etil Asetat Daun Glodokan Tiang (Polyalthia longifolia L.) Secara In Vitro

Cancer is one of the main causes of death throughout the world. Breast cancer is a non-communicable disease and a type of cancer that is often suffered by women. Breast cancer is a reproductive health problem, both in the world and in Indonesia, which is now a serious concern. Medical treatment of cancer is usually carried out with chemotherapy, surgery and radiotherapy, but the Indonesian people are familiar with and use efficacious plants as an effort to cure various diseases, including cancer. One of them is by using glodokan mast leaves or Polyalthia longifolia L. as natural chemotherapy from biological ingredients. This plant is reported to be high in antioxidant content, so it can be used as an anticancer agent, especially T47D breast cancer. The aim of this research is to examine the compound content and activity of T47D breast cancer cells from P. longifolia leaf extract. This research is basic experimental research, namely by comparing the IC50 value of ethyl acetate extract on young and old leaves. Based on the research results, it is known that the ethyl acetate extract in young and old leaves contains alkaloids, flavonoids, tannins and terpenoids which are useful as anticancer compounds. Cytotoxic activity of ethyl acetate extract of P. longifolia leaves against T47D breast cancer cells with an IC50 value of 253.76 μg/mL on old leaves and young leaves of 220.54 μg/mL with moderate cytotoxicity.

Cytotoxic activity of ethyl acetate extract of Chromolaena odorata on MCF7 and T47D breast cancer cells.

One of the most cancers in women that can be fatal is breast cancer. Radiation therapy, chemotherapy, or a combination of the two are often used to treat cancer, and these treatments tend to modify the immune system and weaken defences. Using natural compounds from plants has become a research interest to prevent cancer cell development. The aim of this study was to determine the anticancer activities of ethyl acetate extract of Chromolaena odorata (EACO) against breast cancer cells (MCF-7 and T47D). The viability of the cells was determined by the MTT colorimetry assays. The apoptosis test was performed by using flow cytometry. The IC50 value for MCF-7 cells was 218.78 µg/mL and 307.61 µg/mL for T47D. The extract acted selectively against breast cancer cells, with selectivity indexes against MCF-7 and T47D were 12.77 and 9.08, respectively. The viable cells of T47D cells were decreased from 85±36.5% (24 hours) to 54±34% (48 hours) after treatment with IC50 of EACO. Significant decrease of the MCF-7's viable cells were observed between 48 and 72 hours after treatment with IC50 (68.5±17.7% to 51.01±12.1%, respectively). Apoptosis assay showed that T47D and MCF-7 cells were mainly in the necrosis stage (83.35±0.49% and 95.15±1.76%, respectively). This study suggested that ethyl acetate extract of C. odorata is promising to be developed as an anticancer agent.

In vitro screening of icacinaceous plants indigenous to kerala

This project work was focused on “in vitro screening of Icacinaceous plants indigenous to Kerala”. From phytochemical analysis of ethyl acetate extract of leaves of Sarcostigma kleinii it was found that carbohydrates, alkaloids, flavonoids,tannins, phenols, glycosides are present and saponins,proteins & amino acids are absent. From phytochemical analysis of ethyl acetate extract of leaves of Pyrenacantha volubilis it was found that carbohydrates, proteins and amino acids, flavonoids,alkaloids, glycosides, tannins and phenolic compounds are present. Sarcostigma kleinii leaves are used to treat helminthiasis, ulcers, leprosy and skin conditions traditionally. Pyrenacantha volubilisleaves are mainly used to treat cancer. The present study deals with the anti-inflammatory activity and antibacterial activity of ethyl acetate extracts of leaves of Sarcostigma kleinii and Pyrenacantha volubilis of Icacinaceae family. The results suggest that ethyl acetate extract of leaves of these two Icacinaceous plants may serve as a anti - inflammatory and antibacterial agents which may be due to the chemical constituents like alkaloids, phenols, tannins or flavonoids present in these plants.

Anti-cancer potential of Lactiplantibacillus plantarum NG28 through the induction of intrinsic apoptosis

Introduction: Probiotics and fermented foods have become the focal point of research across different scientific disciplines, with recent findings indicating that Lactiplantibacillus plantarum (L. plantarum) isolated from various origins, holds significant promise in combating numerous diseases, including cancer. Hence, our current study seeks to explore how the L. plantarum NG28 strain might counteract the growth of HT-29 colorectal adenocarcinoma cells, potentially contributing to anti-cancer strategies.
 
 Methods: The effect of the ethyl acetate extract of L. plantarum NG28 strain on HT-29 cells was evaluated in several ways. First, the cytotoxicity of HT-29 cells was determined by MTT assay. Additionally, the changes in cell morphology of HT-29 cells through DAPI staining and the induction of apoptosis using Annexin V-FITC/PI staining followed by flow cytometry were investigated. By using the RT-PCR and western blot techniques the expression of pro-apoptotic genes and proteins such as Bax, Caspase-9, and Caspase-3, as well as the anti-apoptotic gene Bcl-2 was examined.
 
 Results: The findings revealed that the ethyl acetate extract of L. plantarum NG28 strain had a significant impact on the viability of HT-29 colon cancer cells in a dose-dependent manner, in contrast to its minimal effect on HUVEC cells. DAPI staining revealed the noticeable DNA damage and condensation of treated HT-29 cells and the flow cytometry strengthened the occurrence of apoptosis in the treated HT-29 cells. RT-PCR and western blot techniques investigated the intrinsic apoptosis of HT-29 cells through the increased expression levels of pro-apoptotic genes / proteins and decreased expression levels of anti-apoptotic gene.
 
 Conclusion: The study demonstrated the anti-cancer activity of ethyl acetate extract of the L. plantarum NG28 strain against HT-29 colon cancer cells, primarily through the intrinsic apoptotic pathway. This suggests that L. plantarum NG28 strain could be used as a therapeutic tool in the inhibition and medication of colorectal cancer.

Evaluation of Antioxidant and Anticancer Activities of Memecylon umbellatum in Breast Carcinoma and Lupeol and Beta-sitosterol Quantified by HPTLC

Introduction: Memecylon umbellatum is a perennial plant of the Melastomataceae family that grows in abundance in the Western Ghats and has been used traditionally to treat cancer and inflammatory conditions. background: Memecylon umbellatum is a perennial plant of the Melastomataceae family grows in abundance in the Western Ghats and has been used traditionally to treat cancer and inflammatory conditions. Methods: From the literature survey, it was found that no substantial work has been carried out to identify the bioactive compounds by HPTLC method and to screen the antioxidant and anticancer activity of M. umbellatum. Hence, an effort has been made to carry out the phytochemical investigation by HPTLC method and to screen the antioxidant activity by ABTS assay, DPPH assay, Nitric oxide antioxidant assay, Iron chelating activity and Total antioxidant activity. objective: From the literature survey it was found that no substantial work has been carried out to identify the bioactive compounds by HPTLC method and to screen the antioxidant and anticancer activity of M. umbellatum. Hence an effort has been made to carry out the phytochemical investigation by HPTLC method and to screen the antioxidant activity and anticancer activity Results: Total phenolics and flavonoids were carried out by using suitable methods. MCF-7 as well as MDA-MB-231 cells were used to test anticancer activities in vitro. Cell cycle analysis demonstrated that ethyl acetate extract caused G0/G1 phase arrest in MCF-7 cells. HPTLC analysis led to the identification of Lupeol from ethyl acetate extract. Conclusion: The anticancer activity of ethyl acetate extract of M. umbellatum was significant. The antioxidant and anticancer activity may attributed to Lupeol, Phenolic compounds and Flavonoids. conclusion: The antioxidant and anticancer activity may attributed to Lupeol, Phenolic compounds and Flavonoids.

Determination of In-vitro antioxidant activity of Ougeinia oojeinensis leaves

In this investigation, the In-vitro antioxidant Activity of extracts of leaves of Ougeinia oojeinensis was evaluated. The antioxidant activity in vitro was measured by means DPPH, Reducing power and hydroxyl radical scavenging activity. DPPH radical scavenging activity of ethyl acetate extract of Ougeinia oojeinensis exhibited percent inhibition 66.774% and its IC50 value was found to be 43.503μg/ml. DPPH radical scavenging activity of methanol extract of Ougeinia oojeinensis exhibited percent inhibition 76.267% and its IC50 value was found to be 25.722μg/ml. Ascorbic acid was used as a reference compound which exhibited percent inhibition 89.428% and showed IC50 value of 15.615 μg/ml. Similarly hydroxyl radical scavenging activity of ethyl acetate extract of Ougeinia oojeinensis exhibited percent inhibition 62.183% and its IC50 value was found to be 69.341 μg/ml. Similary, hydroxyl radical scavenging activity of methanol extract of Ougeinia oojeinensis exhibited percent inhibition 75.84% and its IC50 value was found to be 33.360μg/ml. Ascorbic acid was used as a reference compound which exhibited percent inhibition 87.749% and showed IC50 value of 9.904 μg/ml. The methanolic extract showed strong reducing capacity as compared to ethyl acetate extract of Ougeinia oojeinensis.

In-vitro antioxidant and cytotoxic activities of ethyl acetate extract of Holigarna ferruginea

Higher plants have long been used as traditional medicines to treat human ailments. Approximately 80% of people worldwide utilize plants as safe sources of medicines to heal human diseases via a totally new medicinal system. Holigarna ferruginea is an indigenous medicinal tree plant in the Anacardiaceae family. The plant has a wide range of physiologically active chemicals. GC-MS was used to screen phytochemical substances, while FTIR was used to identify functional groups. GC-MS study revealed 10 major bioactive phytochemical substances that belong to functional groups such as secondary amines, alcohols, ethers, esters, carboxylic acids, and anhydrides. These diverse active phytochemicals have been discovered to have a wide range of actions that may aid in the prevention of illnesses. Higher quantities of phytochemical substances were found in ethyl acetate extracts of leaves. As a result, the extract possesses anticancer and antioxidant activities against Humans Breast cell lines (MCF-7). The viability was reduced when the concentrations of the ethyl acetate extract of H. ferruginea leaves were increased and it may help in the discovery of an ideal therapeutic agent in novel drugs as well as nutritional supplements.

Insecticidal potential of a Consolida ajacis extract and its major compound (ethyl linoleate) against the diamondback moth, Plutella xylostella

The diamondback moth (Plutella xylostella) is one of the most destructive lepidopteran pests of cruciferous vegetables. However, DBM has developed resistance to current chemical and biological insecticides used for its control, indicating the necessity for finding new insecticides against it. Bio-insecticides derived from plant extracts are eco-friendly alternatives to synthetic pesticides. The aims of this study were to evaluate the insecticidal activity of Consolida ajacis seed extracts against DBM, the underlying mechanism of the control effect of promising extracts, and the identification of the main insecticidal compounds of these extracts. The results showed that ethyl acetate extract of C. ajacis seed exhibited strong contact toxicity (LC50: 5.05 mg/mL), ingestion toxicity, antifeedant, and oviposition deterrent activities against DBM, among the extracts evaluated. At 72 h, glutathiase, acetylcholinesterase, carboxylesterase, peroxidase, and superoxide dismutase activities were inhibited, but catalase activity was activated. The main compound identified from the extract was ethyl linoleate, which had the most significant insecticidal activity on the diamondback moths. This study's findings provide a better understanding of the insecticidal activity of ethyl acetate extract obtained from C. ajacis and its main component (ethyl linoleate). This will help in the development of new insecticides to control DBM.

Exploration of in vitro cytotoxic and in ovo antiangiogenic activity of ethyl acetate extract of Penicillium oxalicum.

Fungal endophytes have established new paradigms in the area of biomedicine due to their ability to produce metabolites of pharmacological importance. The present study reports the in vitro cytotoxic and in ovo antiangiogenic activity of the ethyl acetate (EA) extract of Penicillium oxalicum and their chemical profiling through Gas Chromatography-Mass Spectrometry analysis. Treatment of the EA extract of P. oxalicum to the selected human breast cancer cell lines (MDA-MB-231 and MCF-7) leads to the reduced glucose uptake and increased nitric oxide production suggesting the cytotoxic activity of EA extract of P. oxalicum. Our results further show thattreatment of EA extract of P. oxalicum attenuates the colony number, cell migration ability and alters nuclear morphology in both the human breast cancer cell lines. Furthermore, the treatment of EA extract of P. oxalicum mediates apoptosis by increasing theexpression of BAX, P21, FADD, and CASPASE-8 genes, with increased Caspase-3 activity. Additionally, in ovo chorioallantoic membrane (CAM) assay showed that the treatment of EA extract of P. oxalicum leads to antiangiogenic activity with perturbed formation of blood vessels. Overall, our findings suggest that the EA extract of P. oxalicum show in vitro cytotoxic and antiproliferative activity against human breast cancer cell lines, and in ovo antiangiogenic activity in CAM model.

Antidiabetic and Immunoregulatory Activities of Extract of Phyllanthus emblica L. in NOD with Spontaneous and Cyclophosphamide-Accelerated Diabetic Mice.

Oil-Gan, also known as emblica, is the fruit of the genus Phyllanthus emblica L. The fruits are high in nutrients and display excellent health care functions and development values. The primary aim of this study was to investigate the activities of ethyl acetate extract from Phyllanthus emblica L. (EPE) on type 1 diabetes mellitus (T1D) and immunoregulatory activities in non-obese diabetes (NOD) mice with spontaneous and cyclophosphamide (Cyp)-accelerated diabetes. EPE was vehicle-administered to spontaneous NOD (S-NOD) mice or Cyp-accelerated NOD (Cyp-NOD) mice once daily at a dose of 400 mg/kg body weight for 15 or 4 weeks, respectively. At the end, blood samples were collected for biological analyses, organ tissues were dissected for analyses of histology and immunofluorescence (IF) staining (including expressions of Bcl and Bax), the expression levels of targeted genes by Western blotting and forkhead box P3 (Foxp3), and helper T lymphocyte 1 (Th1)/Th2/Th17/Treg regulatory T cell (Treg) cell distribution by flow cytometry. Our results showed that EPE-treated NOD mice or Cyp-accelerated NOD mice display a decrease in levels of blood glucose and HbA1c, but an increase in blood insulin levels. EPE treatment decreased blood levels of IFN-γ and tumor necrosis α (TNF-α) by Th1 cells, and reduced interleukin (IL)-1β and IL-6 by Th17 cells, but increased IL-4, IL-10, and transforming growth factor-β1 (TGF-β1) by Th2 cells in both of the two mice models by enzyme-linked immunosorbent assay (ELISA) analysis. Flow cytometric data showed that EPE-treated Cyp-NOD mice had decreased the CD4+ subsets T cell distribution of CD4+IL-17 and CD4+ interferon gamma (IFN-γ), but increased the CD4+ subsets T cell distribution of CD4+IL-4 and CD4+Foxp3. Furthermore, EPE-treated Cyp-NOD mice had decreased the percentage per 10,000 cells of CD4+IL-17 and CD4+IFNγ, and increased CD4+IL-4 and CD4+Foxp3 compared with the Cyp-NOD Con group (p < 0.001, p < 0.05, p < 0.05, and p < 0.05, respectively). For target gene expression levels in the pancreas, EPE-treated mice had reduced expression levels of inflammatory cytokines, including IFN-γ and TNF-α by Th1 cells, but increased expression levels of IL-4, IL-10, and TGF-1β by Th2 cells in both two mice models. Histological examination of the pancreas revealed that EPE-treated mice had not only increased pancreatic insulin-expressing β cells (brown), and but also enhanced the percentage of Bcl-2 (green)/Bax (red) by IF staining analyses of islets compared with the S-NOD Con and the Cyp-NOD Con mice, implying that EPE displayed the protective effects of pancreas β cells. EPE-treated mice showed an increase in the average immunoreactive system (IRS) score on insulin within the pancreas, and an enhancement in the numbers of the pancreatic islets. EPE displayed an improvement in the pancreas IRS scores and a decrease in proinflammatory cytokines. Moreover, EPE exerted blood-glucose-lowering effects by regulating IL-17 expressions. Collectively, these results implied that EPE inhibits the development of autoimmune diabetes by regulating cytokine expression. Our results demonstrated that EPE has a therapeutic potential in the preventive effects of T1D and immunoregulation as a supplementary.

Antioxidant activities of medang lendir (Litsea glutinosa) stem bark

Background: Medang lendir (Litsea glutinosa), a member of the Lauraceae family, is typically found in the Kampar Regency area of Riau Province, Indonesia. This plant is frequently used in traditional medicine to treat rheumatism, diarrhea, and dysentery. Objective: To evaluate the antioxidant activities of L. glutinosa stem bark extracts. Method: L. glutinosa stem bark was macerated in methanol to obtain methanol extract, followed by partitioning with ethyl acetate to obtain ethyl acetate extract. The antioxidant activities of these extracts were determined using the NO radical scavenging and the DPPH radical scavenging methods. The Folin-Ciocalteu method was also used in this study to determine total phenolic content (TPC). Result: The antioxidant activities of ethyl acetate and methanol extracts of L. glutinosa stem bark against NO radicals resulted in a small percentage of inhibition (%I &lt; 0). Meanwhile, for DPPH radical scavenging, the antioxidant activity of the ethyl acetate extract (IC50 = 222.03 ug/mL) was greater than the methanol extract (IC50 = 232.81 ug/mL), and the TPC value of the ethyl acetate extract (23.88 mgGAE/g) was greater than the methanol extract (23.16 mgGAE/g). Conclusion: These results show that the antioxidant activity based on scavenging DPPH radicals for both extracts was active; however, it was inactive on NO radicals. The ethyl acetate extract possessed a higher TPC value compared to the methanol extract.

Gamma irradiation effect on physicochemical properties of Guazuma ulmifolia leaves and their antiproliferative activities against human cancer cell lines

Guazuma ulmifolia leaves (GUL) has a long been used in traditional medicine, including anticancer. To preserve the simplicia, many companies utilize gamma irradiation techniques. The research aimed to study the irradiation effect on GUL simplicia that preserved using gamma irradiation based on its physicochemical properties and antiproliferative activities against human cancer cell lines. GUL was irradiated at 7.5 kGy, then the irradiated sample (IRGUL) and un-irradiated sample (GUL) as a control were gradually macerated using n-hexane, ethyl acetate, and ethanol. The obtained ethyl acetate extracts from control sample (EAE-GUL) and irradiated samples (EAE-IRGUL) were then fractionated by silica gel column chromatograph using combination of n-hexane/ethyl acetate/methanol. The EAE-GUL, EAE-IRGUL, and its active fraction (fraction 4) were then evaluated their total phenolic and total flavonoid contents (TPC, TFC), thin layer chromatograph-densitometry (TLC-densitometry), LC/MS/MS, as well as in vitro bioassay against human cancer cells (THP1 leukemia, MCF7 breast cancer, and K562 erythroleukemia). The results showed that the n-hexane, ethyl acetate, and ethanol extracts of EAE-IRGUL were lower than these extracts of EAE-GUL. Analysis of TPC, TFC showed that their TPC and TFC of EAE-IRGUL decreased by 15.8% and 4.9%, respectively, compared to EAE-GUL. In vitro bioassay showed that the irradiation dose of 7.5 kGy could decrease their antiproliferative activity of ethyl acetate extracts and their fraction 4 against THP1, MCF7, and K562 cancer cells, however, the decrease did not eliminate their bioactivity. Therefore, good manufacturing practices to obtain low bioburden is important, so the irradiation dose can be kept as low as possible. In addition, increasing the active ingredient dosage may be applied with regard to the decrease in physicochemical and biological properties of GUL simplicia due to irradiation exposure. TLC-densitometry and LC/MS/MS analysis showed that some main spots on TLC and main peaks at total ion chromatogram (TIC) of F4 of EAE-IRGUL decreased, while other spots on TLC and peaks in TIC increased compared to control. More studies are needed to evaluate the effect of gamma radiation on individual compounds using chromatographic techniques and NMR as well.

Bioinsecticide activity of ethyl acetate extract of Nothaphoebe coriacea Kosterm bark against Spodoptera exigua larvae in a laboratory

Spodoptera exigua is a cosmopolitan and polyphagous pest. Botanical pesticides are an alternative technique to control S. exigua. This study aimed to evaluate the effect of an ethyl acetate extract of Nothaphoebe coriacea Kosterm bark (EEN) on the biological activity of S. exigua larvae and to determine the most effective concentration to manage S. exigua. This experiment was arranged on a single factor completely randomized design with the concentration level as a factor. Botanical pesticide formulated from ethyl acetate solvent in maceration extraction. The test was carried out by dipping the leaf mustard into the treatment solution and then feeding it to 10 S. exigua larvae. The result showed the EEN had an 0.5% extract content with bioactive from the alkaloids and tannins groups. Mortality and feeding inhibition showed good responses to the biological activity test. However, the mortality rate test revealed different responses the most effective concentration of EEN was 0.5%. This concentration has a mortality of 92% and kill 3.6 individuals per hour, but has a low feeding inhibition of 72.82%. A botanical pesticide from EEN can be developed to control S. exigua. The LC50 obtained from the application of the EEN to S. exigua larvae was 0.062%. EEN has the potential to be developed as a botanical pesticide.

Preliminary study on the effective site and mechanism of action of Meconopsis quintuplinervia Regel in alleviating acute alcoholic liver injury in mice.

Meconopsis quintuplinervia Regel (MQR) belongs to the opium poppy tree plant species, and it has heat purging, detoxification, diuretic, anti-inflammatory, and analgesic effects. MQR has liver-protective properties and can alleviate liver heat. Therefore, this study aimed to observe the effect of MQR extract on acute alcoholic liver injury in mice and explore the mechanism of action of ethyl acetate extract of MQR (MQR-E) on alcohol-induced liver injury in combination with the network pharmacology. To induce acute alcoholic liver injury, 52% of edible wine was administered at 12mL/kg for 14 days. The pharmacodynamic results were used to screen the active site. MQR-E composition was analyzed based on UPLC-Q-TOF-MS, and relevant MQR-E and alcoholic liver disease (ALD) targets were screened using an online database. Then, Venn analysis of drug and disease-related targets was performed to obtain cross-targets. We investigated the protein-protein interaction network (PPI) of overlapping targets, the core targets were screened using the STRING database, and the DAVID database was chosen for GO and KEGG enrichment analysis of the central targets. Each of the four MQR extracts ameliorated alcoholic liver injury to varying degrees; the best results were achieved with MQR-E. MQR-E reduces liver index, serum transaminases, and fat accumulation, and attenuates ethanol-induced histopathological changes. The activities of hepatic superoxide dismutase (SOD) and glutathione peroxidase (GSH-PX) were increased, the content of malondialdehyde (MDA) was significantly reduced compared to the EtOH group, and MQR-E effectively mitigated the oxidative stress induced by ethanol in the liver. Thirty-six compounds were identified, and flavonoids were the most abundant. PPI network topology analysis was employed to assess 32 core targets: IL-6, TNF, STAT3, PPARA, and other inflammation and lipid metabolism related genes. Pathway analysis of GO and KEGG enrichment showed that the regulation of inflammatory factors and lipid metabolism were primarily involved. We concluded that MQR-E had protective effects against acute alcohol-induced liver injury in mice, and the mechanism could be linked to the inhibition of lipid peroxidation and oxidative stress. The mechanism by which MQR-E ameliorated ALD primarily involved regulating inflammatory factors and lipid metabolism based on the prediction of the network pharmacology.

Ultraperformance liquid chromatography-based metabolite profiling and cytotoxic activity of the ethyl acetate extract of two endophytic Penicillium sp.

The present study evaluated the mycochemical abundance, and the cytotoxic and hemolytic activities of ethyl acetate extract (EAE) of endophytic Penicillium camponotum (PC) and Penicillium fuscoglaucum (PF). Higher yield was noted in EAE-PF with total phenols (26.59 ± 1.52 mg of GAE/g DW) and flavonoids (3.12 ± 1.83 mg of QE/g DW). The EAE-PF inhibited the proliferation of two breast cancer cells (BT-474 and MDA-MB-231) with the half-maximal inhibitory concentration (IC50) of 0.112 and 0.120 mg/mL, respectively, while the IC50 values against HEK-293 and NIH3T3 cells were not found up to 1 mg/mL dose of EAE-PF. Moreover, EAE-PF (1 mg/mL) demonstrated its trivial toxicity in erythrocytes with ∼4.6% of hemolysis. The metabolic profiling of EAE-PF revealed the presence of mycochemicals including penicitide B (C18H34O5), p-hydroxyphenethyl anisate (C16H16O4), and dihydroxystearic acid (C18H36O4). Furthermore, these compounds exhibited substantial interactions with human cancer-related proteins such as epidermal growth factor receptor (EGFR), N-myristoyltransferase isoform 2 (NMT-2), cyclin-dependent kinase 2 (CDK-2), and c-mesenchymal epithelial transition factor kinase (c-Met K) evidenced by in-silico molecular docking analysis. Overall, this report suggests further studies on the isolation and purification of novel anti-cancer compounds from endophytic PF.

GC-MS Based Characterization, Antibacterial, Antifungal and Anti-Oncogenic Activity of Ethyl Acetate Extract of Aspergillus niger Strain AK-6 Isolated from Rhizospheric Soil.

Rhizospheric soil is the richest niche of different microbes that produce biologically active metabolites. The current study investigated the antimicrobial, antifungal and anticancer activities of ethyl acetate extract of the potent rhizospheric fungus Aspergillus niger AK6 (AK-6). A total of six fungal isolates were isolated, and isolate AK-6 was selected based on primary screening. Further, it exhibited moderate antimicrobial activity against pathogens such as Klebsiella pneumonia, Candida albicans, Escherichia coli, Shigella flexneri, Bacillus subtilis and Staphylococcus aureus. The morphological and molecular characterization (18S rRNA) confirmed that the isolate AK-6 belonged to Aspergillus niger. Further, AK-6 showed potent antifungal activity with 47.2%, 59.4% and 64.1% of inhibition against Sclerotium rolfsii, Cercospora canescens and Fusarium sambucinum phytopathogens. FT-IR analysis displayed different biological functional groups. Consequently, the GC-MS analysis displayed bioactive compounds, namely, n-didehydrohexacarboxyl-2,4,5-trimethylpiperazine (23.82%), dibutyl phthalate (14.65%), e-5-heptadecanol (8.98%), and 2,4-ditert-butylphenol (8.60%), among the total of 15 compounds isolated. Further, the anticancer activity of AK-6 was exhibited against the MCF-7 cell line of human breast adenocarcinoma with an IC50 value of 102.01 μg/mL. Furthermore, flow cytometry depicted 17.3%, 26.43%, and 3.16% of early and late apoptosis and necrosis in the AK-6 extarct treated MCF-7 cell line, respectively. The results of the present analysis suggest that the isolated Aspergillus niger strain AK-6 extract has the potential to be explored as a promising antimicrobial, antifungal and anticancer drug for medical and agricultural applications.

Screening of medicinal mushroom strains with antimicrobial activity and polysaccharides production

AbstractObjectivesThis study aimed to determine the antimicrobial activity of culture fluid and mycelial mass of selectedHericiumstrains from the IBK Mushroom Culture Collection (Kyiv, Ukraine) against bacteria and fungi, as well as to evaluate the potential of these mushrooms for biomass and extracellular polysaccharides production.MethodsThe antimicrobial activity of ethyl acetate extracts of culture fluid and aqueous-ethyl extracts of mycelial mass for threeHericiumspecies:Hericium cirrhatumIBK 2393,Hericium coralloidesIBK 2332, andHericium erinaceusIBK 2530 against Gram-positiveBacillus subtilis,Staphylococcus aureus, and Gram-negativeEscherichia coli,Klebsiella pneumoniae,Pseudomonas aureginosabacteria as well asAspergillus niger,Penicillium polonicum, andMucor globosusfungi by the disk diffusion method was conducted. Analysis of the minimum inhibitory concentration was carried out according to the broth dilution method.ResultsHigh antimicrobial activity of culture fluid extracts ofHericiummushroom species againstS. aureuswas established after 14–21 days of cultivation. No effects ofHericiumextracts againstA. niger,P. polonicum, andM. globosuswere observed. On the 7th day of submerged cultivation, the studied strains produced the maximum yield of extracellular polysaccharides. The most promising extracellular polysaccharide (EPS) producers were strains ofH. coralloidesIBK 2332 (1.89 g/L) andH. erinaceusIBK 2530 (1.90 g/L). The maximal value of biomass was produced byH. cirrhatumIBK 2393 on the 21st day of submerged cultivation (17.45 g/L).ConclusionsHericiummushrooms have significant potential for the development of new drugs with health benefits properties.

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.