Inhibitory Effect Of Extracts Research Articles

Inhibitory effect of extracts from edible parts of nuts on α-amylase activity: a systematic review.

Elevated blood glucose concentration is a risk factor for developing metabolic dysfunction and insulin resistance, leading to type 2 diabetes and cardiovascular diseases. Nuts have the potential to inhibit α-amylase activity, and so lower postprandial glucose, due to their content of polyphenols and other bioactive compounds. We conducted a systematic literature review to assess the ability of extracts from commonly consumed edible parts of nuts to inhibit α-amylase. Among the 31 included papers, only four utilised human α-amylases. These papers indicated that polyphenol-rich chestnut skin extracts exhibited strong inhibition of both human salivary and pancreatic α-amylases, and that a polyphenol-rich almond skin extract was a potent inhibitor of human salivary α-amylase. The majority of the reviewed studies utilised porcine pancreatic α-amylase, which has ∼86% sequence homology with the corresponding human enzyme but with some key amino acid variations located within the active site. Polyphenol-rich extracts from chestnut, almond, kola nut, pecan and walnut, and peptides isolated from cashew, inhibited porcine pancreatic α-amylase. Some studies used α-amylases sourced from fungi or bacteria, outcomes from which are entirely irrelevant to human health, as they have no sequence homology with the human enzyme. Given the limited research involving human α-amylases, and the differences in inhibition compared to porcine enzymes and especially enzymes from microorganisms, it is recommended that future in vitro experiments place greater emphasis on utilising enzymes sourced from humans to facilitate a reliable prediction of effects in intervention studies.

Chemical Analysis of the Antihyperglycemic, and Pancreatic α-Amylase, Lipase, and Intestinal α-Glucosidase Inhibitory Activities of Cannabis sativa L. Seed Extracts.

Cannabis is considered (Cannabis sativa L.) a sacred herb in many countries and is vastly employed in traditional medicine to remedy numerous diseases, such as diabetes. This research investigates the chemical composition of the aqueous extracts from Cannabis sativa L. seeds. Furthermore, the impact of these extracts on pancreatic α-amylase and lipase, and intestinal α-glucosidase enzymes is evaluated, as well as their antihyperglycemic effect. Analysis of the chemical composition of the aqueous extract was conducted using high-performance liquid chromatography with a photodiode array detector (HPLC-DAD). In contrast, the ethanol, hexanic, dichloromethane, and aqueous extract compositions have been established. Additionally, the inhibitory effects of ethanolic, dichloromethane, and aqueous extracts on pancreatic α-amylase and lipase, and intestinal α-glucosidase activities were evaluated in vitro and in vivo. The results of HPLC analysis indicate that the most abundant phenolic compound in the aqueous cannabis seed extract is 3-hydroxycinnamic acid, followed by 4-hydroxybenzoic acid and rutin acid. Moreover, administration of ethanolic and aqueous extracts at a dose of 150 mg/Kg significantly suppressed postprandial hyperglycemia compared to the control group; the ethanolic, dichloromethane, and aqueous extracts significantly inhibit pancreatic α-amylase and lipase, and intestinal α-glucosidase in vitro. The pancreatic α-amylase test exhibited an inhibition with IC50 values of 16.36 ± 1.24 µg/mL, 19.33 ± 1.40 µg/mL, 23.53 ± 1.70 µg/mL, and 17.06 ± 9.91 µg/mL for EAq, EDm, EET, and EHx, respectively. EET has the highest inhibitory capacity for intestinal α-glucosidase activity, with an IC50 of 32.23 ± 3.26 µg/mL. The extracts inhibit porcine pancreatic lipase activity, demonstrating their potential as lipase inhibitors. Specifically, at a concentration of 1 mg/mL, the highest inhibition rate (77%) was observed for EDm. To confirm these results, the inhibitory effect of these extracts on enzymes was tested in vivo. The oral intake of aqueous extract markedly reduced starch- and sucrose-induced hyperglycemia in healthy rats. Administration of the ethanolic extract at a specific dose of 150 mg/kg significantly reduced postprandial glycemia compared with the control group. It is, therefore, undeniable that cannabis extracts represent a promising option as a potentially effective treatment for type 2 diabetes.

Potential Biopesticides from Seed Extracts: A Sustainable Way to Protect Cotton Crops from Bollworm Damage

In the current study, the inhibitory effect of extracts from Gramineae (wheat, barley, and corn) and Leguminosae (sophora, bean, and pea) seeds was studied on the digestive alpha-amylase activity in cotton bollworm (Helicoverpa armigera Hubner). The insect was bred on artificial food based on Vigna unguiculata in the greenhouse condition (26 ± 2 °C, 60 ± 10% (Relative Humidity), R.H., 16:8 (Light: Darkness), L: D). The extracts of wheat (95.2%), barley (84.6%), corn (73.8%), sophora (77%), Vigna unguiculata (52%), and pea (56.7%) significantly inhibited the alpha-amylase activity in H. armigera. Studying the impact of different fractions (obtained via deposition at various concentrations of ammonium sulfate salt) on the alpha-amylase enzyme activity demonstrated that in 0–30% fractions, wheat, barley, and sophora have the highest effect (95.26%, 94.65%, and 94.73%, respectively) compared to the other fractions. The inhibitory activities of 0–30% fractions of corn, bean, and pea were 83.3, 56.94, and 50.92%, respectively. In 30–50% fractions, the most effective ones were those of wheat and barley with the inhibitory activity of 79.7% and 82.9%, respectively. In addition, bean and pea fractions inhibited 25.2% and 27.5%, in that order. No significant inhibitory impact was detected in 50–70% or higher fractions. The investigation of the impact of pH values (i.e., 2, 4, 8, and 10) on the inhibition of the alpha-amylase enzyme activity introduced 8–10 as the optimum pH in H. armigera. Nanotechnology offers several ways to enhance plant-based pesticides, which are a solution for making plant extract usage more efficient. The exploration of plant-based pesticides, in conjunction with the incorporation of nanotechnology and other scientific fields, offers a wide range of prospects for further investigation.

Selective Cytotoxicity of Ficus Benjamina Leaf Extract Against Lung Cancer Cells

This study examines the inhibitory effects of chloroform extract (samples A, B, C, D and E) from Ficus benjamina leaves as a cancer treatment by comparing them to the anticancer medicine, Bortezomib (BTZ), and evaluating their effects on lung cancer cell lines. Sample A is the crude chloroform extract from Ficus benjamina leaf; samples B to E are different fractions derived through flash chromatography of the crude chloroform extract. Positive control was Bortezomib and negative control was Dimethyl sulfoxide (DMSO). The test samples were used at two concentrations of 10 µg/ML and 50 µg/ML. BTZ was tested at 1 µM and DMSO at 1 %. According to the findings, sample C showed significant (p<0.05) inhibition of cancer cell lines at 50 µg/ML. The extract's inhibitory activity, however, was shown to be less than that of BTZ. Increased concentrations of the extract showed increased inhibitory activity, supporting the finding that the inhibitory effect of the extract is concentration dependent. At a concentration of 10 µg/ML, extracts A, C, D, and E significantly inhibited lung cancer cell lines as compared to extract B that did not. At both concentrations of 10 µg/ML and µ50 g/ML, the inhibition displayed by bortezomib was noticeably higher than that of all the samples of the chloroform extract of Ficus benjamina leaves. At a concentration of 50 µg/ML, extract C showed a much greater percentage of inhibition against the lung cancer cell lines. Overall, the study shows that Ficus benjamina leaves may be used as an anticancer drug. Sample C showed selective cytotoxicity against the cancer cells while sparing healthy human embryonic kidney (HEK) cells. The extract also exhibits a better therapeutic index than Bortezomib, indicating the possibility of a targeted cancer medication with fewer side effects. To clarify the underlying mechanisms and determine clinical feasibility, more study is required. These results highlight the promise of Ficus benjamina leaf extract in the treatment of cancer, but they also highlight the need for further research to fully comprehend its potential.

Momordica charantia phytoconstituents can inhibit human T-lymphotropic virus type-1 (HTLV-1) infectivity in vitro and in vivo.

There is an urgent need to find an effective therapy for life-threatening HTLV-1-associated diseases. Bitter melon (Momordica charantia) is considered a traditional herb with antiviral and anticancer properties and was tested in this study on HTLV-1 infectivity. GC-MS analyzed the alcoholic extract. In vitro assay was carried out using transfection of HUVEC cells by HTLV-1-MT2 cell line. The cells were exposed to alcoholic and aqueous extracts at 5,10, and 20µg/mL concentrations. In vivo, mice were divided into four groups. Three groups were treated with HTLV-1-MT-2 cells as test groups and positive control, and PBS as the negative control group in the presence and absence of M. charantia extracts. Peripheral blood mononuclear cells (PBMCs), mesenteric lymph nodes (MLNs), and splenocytes were collected for HTLV-1-proviral load (PVL) assessment, TaqMan-qPCR. The GC-MS analysis revealed 36 components in M. charantia. The studies showed significant reductions in HTLV-1-PVL in the presence of extract in the HUVEC-treated groups (P = 0.001). Furthermore, the inhibitory effects of extracts on HTLV-1 infected mice showed significant differences in HTLV-1-PVL among M. charantia treated groups with untreated (P = 0.001). The T-cells in MLNs were significantly more susceptible to HTLV-1 than others (P = 0.001). There were significant differences among HTLV-1-infected cells in MLNs and splenocytes (P = 0.001 and 0.046, respectively). Also, aqueous and alcoholic extract-treated groups significantly affected HTLV-1-infected PBMCs (P = 0.002 and 0.009, respectively). M. charantia may have effective antiviral properties. The substantial compound of M. charantia could have inhibitory effects on the proliferation and transmission of HTLV-1 oncovirus.

СРАВНИТЕЛЬНАЯ ОЦЕНКА АНТИОКСИДАНТНОЙ АКТИВНОСТИ ТРАВЫ И КОРНЕЙ ЦИКОРИЯ ОБЫКНОВЕННОГО, ПРОИЗРАСТАЮЩЕГО НА ТЕРРИТОРИИ ОРЕНБУРГСКОЙ ОБЛАСТИ

The purpose of the work: to study the effect of water extracts of herb and roots of Cichorium intybus L., growing in the Orenburg region, on the processes of free radical oxidation in in vitro systems. Materials and methods. The objects of the study were samples of C. intybus L. raw materials collected in 2020 in the Adamovsky, Belyaevsky, Buzuluksky and Tulgansky districts of the Orenburg region. The antioxidant activity of aqueous extracts from raw materials was determined by the method of registration of chemiluminescence on the device "Chemiluminomer KhLM-003" in systems simulating the processes of production of reactive oxygen species in the Central Research Laboratory of the Federal State Budgetary Educational Institution of Higher Education "Bashkir State Medical University" of the Ministry of Health of the Russian Federation . Statistica 10.0 for Windows (StatSoft, Inc.) was used for statistical processing. Results. The analysis of the obtained results established that the samples of the roots of C. intybus L. growing in the Adamovsky district of the Orenburg region, as well as all the studied samples of the herb of C. intybus L., have antioxidant properties. It was found that the most pronounced antioxidant activity, expressed in the inhibitory effect of extracts from raw materials samples on chemiluminescence in model systems, is shown by the herb of C. intybus L., growing in the Buzuluksky district of the Orenburg region, and the roots of C. intybus L., collected in the Adamovsky district of the Orenburg region. Conclusion. The herb of of Cichorium intybus L., growing in the Orenburg region, and the roots of Cichorium intybus L., collected in the Adamovsky district, can be considered as potential promising sources of natural antioxidants of plant origin.

Effects of herb (mint, ginger, and cinnamon) addition on the formation of 3‐monochloropropanediol esters in the refined olive oil

The inhibitory effects of using extracts and leaf powders from mint (Mentha spicata), ginger (Zingiber officinale), and cinnamon (Cinnamomum verum) were investigated on the formation of 3-monochloropropanediol esters (3-MCPD esters) in the refined olive oil at temperatures 100–200°C using Taguchi's experimental design. The initial concentration of 3-MCPD esters in the refined olive oil before the treatment was 0.33 mg/100 g of oil. The greatest reducing effect was found for mint powder (0.16 mg/100 g of oil). The inhibitory effects of extracts and powders were similar. Based on the Taguchi's approach for the analysis of the data, the best level for the extract and/or the powder of mint or ginger was 0.04 mg for 100 g refined olive oil. During the storage of refined olive oil for 1 and 2 months, mint and ginger as both dry extract and plant powder reduced the formation of 3-MCPD esters. Practical applications In the current study, during 1 and 2 months of storage of refined olive oil, decreases in the production of 3-monochloropropanediol esters were observed in samples containing mint and ginger (as a powder or in their extract forms). Therefore, to avoid the production of this toxic chemical in olive oil after it is packaged, mint and ginger can be combined with the oil immediately after its refining stage. Results from the current study can encourage manufacturers to use these natural antioxidants for inhibiting the formation of 3-monochloropropanediol esters.

Ayurvedic, herbal extracts suppress Candidal biofilms in vitro

Plant derivatives have been used for centuries to treat various human afflictions including microbial infections. A vast majority of these infections are initiated and perpetuated by community dwelling, surface-attached organisms living in micro-econiches known as biofilms. We investigated the biofilm suppressant effect of phytomedicinal preparations used widely in traditional Ayurvedic medicine, Triphala, a mixture of Terminalia bellirica , Terminalia chebula and Emblica officinalis , and Mimusops elengi bark extract. Inhibitory effect of extracts were first investigated against the planktonic C. albicans and C. tropicalis using the well diffusion. Minimum biofilm inhibitory concentration for in-vitro biofilms was determined by MTT assay. The biofilm suppressant effect was determined by measuring biofilm viability at different time intervals, post-exposure to the two herbal extracts, and using MTT. Scanning electron microscopy was performed to assess the post-exposure biofilm architecture. Triphala inhibited both species of the planktonic yeasts, and only the biofilm phase C. tropicalis and mixed species , and not C. albicans. M. elengi had no inhibitory effect on either the planktonic or the biofilms of either Candida species. Ultrastructural microscopy revealed increased cell density of C. albicans biofilm, but not that of C. tropicalis which was significantly reduced in size after Triphala exposure. Triphala, but not M. elengi, extracts exhibit selective and differential biofilm inhibitory activity against Candida . C. albicans biofilms are more resistant to the anti-biofilm activity of Triphala.

The Effects of Ethanol and Methanol Extracts of Ziziphus Spina-christi, Peganum Harmala, Salvia Officinalis, and Querqus Brantii on the Growth and Biofilm Formation by Staphylococcus Aureus in Vitro

Background and Objectives: Medicinal plants are one of the most important natural resources in each country. The aim of this study was to evaluate the anti-biofilm effect of ethanol and methanol extracts of Ziziphus spina-christi leaves, Peganum harmala, Salvia officinalis, and Querqus brantii on the growth and formation of biofilm by Staphylococcus aureus. Methods: Following evaluation of the susceptibility of the studied Staphylococcus aureus strain to various antibiotics, the growth inhibitory effect of extracts on the bacterium was investigated by disc diffusion method and then the inhibitory effect of the extracts on biofilm formation was evaluated in 96 well micro-titer plates. The means were compared with ANOVA test. Results: The results from antibacterial effect of the extracts showed that the methanol extract of Peganum harmala and Querqus brantii seeds at 350 and 450 mg/ml concentrations had a greater inhibitory effect on the growth of Staphylococcus aureus than other extracts as well as synthetic antibiotics. The results from anti-biofilm formation effect of the extracts showed that methanol extract of Salvia officinalis leaves and Querqus brantii seeds at 350 mg/ml concentration, and ethanol extract of Salvia officinalis leaves at 350 mg/ml concentration were the lowest concentrations that showed the greatest inhibitory effect on biofilm formation by Staphylococcus aureus. Other extracts inhibited biofilm formation by this bacterium in higher concentrations. The lowest anti-biofilm effect on Staphylococcus aureus was observed by ethanolic and methanolic extracts of Ziziphus spina-christi leaf. Conclusion: The studied extracts in this study, especially the methanol extracts of Salvia officinalis leaves and Peganum harmala seeds, and ethanol extract of Salvia officinalis leaves are good solutions for S. aureus infection and biofilms formation control and are suggested that be evaluated in In vivo experiments and clinical applications.

Bulbine natalensis (currently Bulbine latifolia) and select bulbine knipholones modulate the activity of AhR, CYP1A2, CYP2B6, and P-gp.

Bulbine natalensis, an emerging medicinal herb on the global market with androgenic properties, is often formulated in dietary supplements that promote perceived sexual enhancement. However, to date, comprehensive safety studies of B. natalensis are lacking, particularly those related to its herb-drug interaction potential. The purpose of this study was to assess the inductive and inhibitory effects of extracts and pure compounds of B. natalensis on human cytochrome P-450 isozymes in vitro. Our findings demonstrated that both water and methanolic extracts of B. natalensis as well as knipholone, bulbine-knipholone, and 6'-O-methylknipholone dose-dependently increased mRNA expression encoded by CYP2B6, CYP1A2, and ABCB1 genes. Functional analyses showed that water (60 to 2.20 µg/mL) and methanolic (30 to 3.75 µg/mL) extracts and knipholones (10 to 0.33 µM) increased CYP2B6 and CYP1A2 activity in a dose-dependent manner. Additionally, water extract (60 µg/mL), methanolic extract (30 µg/mL), and knipholone (10 µM) caused activation of the aryl hydrocarbon receptor up to 11.1 ± 0.7, 8.9 ± 0.6, and 7.1 ± 2.0-fold, respectively. Furthermore, inhibition studies revealed that methanolic extract attenuated the activity of metabolically active CYP1A2 (IC50, 22.6 ± 0.4 µg/mL) and CYP2B6 (IC50, 34.2 ± 6.6 µg/mL) proteins, whereas water extracts had no inhibitory effect on either isoform. These findings suggest that chronic consumption of B. natalensis may affect normal homeostasis of select CYPs with subsequent risks for HDIs when concomitantly ingested with conventional medications that are substrates of CYP2B6 and CYP1A2. However, more in-depth translational studies are required to validate our current findings and their clinical relevance.

Comparative Evaluation of the Antibacterial Effects of Nigella sativa and Moringa oleifera on some Clinical Bacteria Isolates

Aim: In this study, the antibacterial effect of the n-hexane, methanol, and ethanol extracts of two traditional medicinal plants, Nigella sativa and Moringa oleifera was carried out to comparatively assess the antibacterial efficacy of these plants against some selected multi-drug resistant diarrheagenic bacterial isolates such as Escherichia coli, Salmonella typhi, Shigella spp, Enterobacter aerogenes, Klebsiella pneumonia, and Pseudomonas aeruginosa.
 Methodology: The inhibitory effects of extracts were assessed using disk diffusion method at six different concentrations i.e. 12.5 mg/ml, 25 mg/ml, 50 mg/ml, 100 mg/ml, 200 mg/ml, and 400 mg/ml. The minimum inhibitory concentrations and minimum bactericidal concentrations of the plant seed extracts were determined by the micro-broth dilution technique. Synergism and antagonism studies were similarly done to determine the combined effects of both N. sativa and M. oleifera seed oil. Further, resistant bacteria were subjected to sodium dodecyl sulphate treatment for plasmid curing and continued with the antibiotic susceptibility test.
 Results: The oil extracts of N. sativa were found to be more effective than that of M. oleifera (at MIC and MCC of 50 mg/ml and 100 mg/ml respectively). It was observed that the plasmids were cured in all the E. coli isolates. Among the pathogens, E. coli was highly susceptible to both seed oils.
 Conclusion: Higher antibacterial activity was observed when the extracts were used in combination, showing a strong synergistic effect against all the pathogens tested.

Synthesis and Evaluation of Lipid-based Nanoparticle Containing Ginger Extract against Aspergillus Species

Introduction: Loading the active ingredients of medicinal plants in lipid nanoparticles reduces the reaction of the active substance with the surrounding environment, such as water and oxygen, and reduces the intensity of transmission or evaporation to the external environment. In this study, intended to enhance efficacy of ginger extract, encapsulation in nanoliponiosome synthesized by thin-film hydration method were done and their antifungal effect on the growth of Aspergillus flavus and Aspergillus parasiticus were studied.
 Methods: In this experimental laboratory study, derivation was done using Soxhlet extractor method. Antifungal activity of ginger extract was specific by disc diffusion and microplate dilution methods. The inhibitory effect of extract was investigated. Physiochemical characteristics and structural characterization of nanoparticle were evaluated from the perspective of in vitro efficiency, drug release, nanoparticle size, zeta potential, surface morphology and FTIR (Fourier-transform infrared spectroscopy), DLS (Dynamic light scattering) and finally SEM (Scanning electron microscope) spectra.
 Results: FTIR investigations showed ginger extract and nanoliponiosome had no chemical interaction leading to change the functional groups. SEM microscope showed the spherical mprphology of particles and average particles size of 73nm. Ginger extract was loaded into the nanoliponiosome with a yield of 71%. It was also found out that ginger extract had a stronger antifungal effect against Aspergillus flavus fungus compared to the Aspergillus parasiticus fungus. At both 37°C and 42°C, the release of ginger extract was higher at pH of 4.5 compared to neutral pH (7.4).
 Conclusion: Nanoliponiosomes containing ginger extract with good physicochemical properties, increased drug stability and good release control can be promising antifungal agents with high antifungal effects and low side effects.

In vitro antioxidant properties and inhibitory effect of extracts and fractions of Plectranthus glandulosus leaves on copper sulfate (CuSO4)-induced oxidation in human low-density lipoprotein

Oxidation of LDL has been suggested to be an initial step in the development of atherosclerosis. This research work deals with the evaluation of antioxidant potential of Plectranthus glandulosus leaves extracts and fractions as well as its protective effects against human LDL oxidation. A preliminary quantitative phytochemical screening was carried out. Antioxidant potential was evaluated employing in vitro hydrogen peroxide, nitric oxide scavenging assays and TAOC test. The human LDL oxidation induced by CuSO4 inhibition test was also performed. Plectranthus glandulosus leaves exhibited the presence of 18.3% of saponines, 25.6% of terpenoids and 36.2% of flavonoids. EAF exhibited highest hydrogen peroxide and nitric oxide scavenger activity (IC50 13.63µg/ml and 24.59 µg/ml respectively). Ascorbic acid exhibited an IC50 value of 15.39µg/ml in hydrogen peroxide assay and 22.96 µg/ml in nitric oxide scavenging activity. EAF exhibited a higher TAOC (optical density 0.186±0.00) than that of ascorbic acid (0.162±0.001) at the concentration of 25µg/ml while at 200µg/ml N-BUTF exhibited a higher optical density (1.261±0.001) than that of ascorbic acid (1.065±0.001). EAF lengthened the lag time of the CD formation up to 150mins at the concentration 1mg/ml. TBARS formation inhibition at the concentration 0.5mg/ml, were no significant different between n-butanol (68.55%) ethyl acetate fraction (68.21%) and quercetin 67.69%). Plectranthus glandulosus is a promising prospect as an anti-atherosclerotic agent and needs a detailed study to establish the same.
 Key words: Plecthrantus glandulosus; oxidation; LDL; atherosclerosis, antioxidant.

In vitro anti-aging activities of ginkgo biloba leaf extract and its chemical constituents

Abstract To determine in vitro anti-aging activity and identify the active chemical constituents in Ginkgo leaf extracts. The antioxidant properties of Ginkgo biloba leaves extracts were evaluated using 1,1-diphenyl-2-picrylhydrazyl radical (DPPH) scavenging and 2,2’-azino-bis (3-ethylbenzothiazoline)-6 sulfonic acid radical (ABTS) scavenging assays. The inhibitory effects of extracts and chemical constituents on reactive oxygen species, matrix metalloproteinase-1 (MMP-1) and collagen tpye I level were tested using human dermal fibroblasts (HDFs). Reverse-phase liquid chromatography (RPLC) and ultra-performance liquid chromatography tandem mass spectroscopy (UPLC/MS/MS) were used to quantitatively analyze flavonoids and terpene trilactones in the extraction. The established quantitative analysis method was validated according to the regulatory guidelines. The extraction and compounds kaempferol 3-O-β-D-glucopyranoside, isorhamnetin-3-O-glucoside, myricetin, ginkgolide A and bilobalide could have potential anti-aging activities of G. biloba. The results suggest that G. biloba could be used as anti-aging products and as a cosmetic and medicinal raw material.

Ligand fishing and identification of acetylcholinesterase inhibitors in Mahonia bealei (Fort.) Carr. using high performance liquid chromatography-mass spectrometry

A fishing platform was developed using immobilized capillary enzyme reactors in combination with liquid chromatography-mass spectrometry (LC-MS) to fish acetylcholinesterase inhibitor (AChEI) from Mahonia bealei (Fort.) Carr. (M. bealei) extract. Four potential AChEIs (columbamine, jatrorrhizine, berberine, and palmatine) were successfully screened out and identified. Their AChE inhibitory activities were further verified by an in vitro assay with IC50 values of 0.93 ± 0.12 μg/mL (columbamine), 3.50 ± 0.15 μg/mL (jatrorrhizine), 2.51 ± 0.12 μg/mL (berberine), and 1.52 ± 0.13 μg/mL (palmatine). A synergy study of these AChEIs was subsequently investigated. In comparison with the IC50 value of M. bealei extract (IC50=0.83 ± 0.21 μg/mL), it can be stated that M. bealei extract is much more active than any single AChEI. Thereafter, the determination of these four alkaloids were investigated and AChE inhibitory effect were compared in terms of the extract and corresponding contents of these four alkaloids. The inhibitory effects of extract at each concentration were stronger than four alkaloids mixture. The results demonstrated that not the four AChEI mixture cause the synergistic effect but rather than the concentrations or ratios of these AChEIs play a vital role in their synergy study.

A strong inhibitory effect of heather honey, propolis and medicinal plant extracts on biofilm formation by pathogenic bacteria

Introduction: P. aeruginosa and S. aureus are opportunistic pathogens that cause a wide range of infections. Their increasing resistance to antibiotics is a serious concern and making them susceptible to treatments is now more essential than ever. There is a need to discover new biofilm inhibitors to increase the susceptibility of these bacteria to antibiotics. Hypothesis and aims: To evaluate the antibiofilm activity of heather honey, propolis and medicinal plant extracts against P. aeruginosa and S. aureus. Methodology: Determination of optimum biofilm growth was carried out using a time-course assay over 24 h intervals, using P. aeruginosa PA14 and S. aureus NCTC 4135 strains. The inhibitory effects of all extracts were determined by biofilm inhibition assay in 24-well plates, with biofilms stained with crystal violet and de-stained with ethanol:acetone; OD were measured at 550 nm. Planktonic growth was measured at 600 nm and samples from the wells were streaked to determine bactericidal effects. Results: Heather honey extracts inhibited both P. aeruginosa and S. aureus by 68%. At 60 μg/mL, one of the propolis extracts promoted biofilm growth of both pathogens. Two other propolis extracts also promoted growth in P. aeruginosa but inhibited biofilm formation in S. aureus by 76.5% and 13.8%, respectively. Three plant extracts inhibited S. aureus biofilm by 7.5%, 10.2% and 87.6% and inhibited P. aeruginosa by −34.9%, 34.7% and 19.4%, respectively. Conclusion: All samples showed varying biofilm inhibition capabilities, but biofilm formation seemed to be more easily inhibited in S. aureus than in P. aeruginosa.

Synthesis, Characterization and Evaluation of Liponiosome Containing Ginger Extract as a New Strategy for Potent Antifungal Formulation

Aflatoxins are natural fungous toxins made by Aspergillus species. The toxins can cause tissue necrosis. In this study, nanoliponiosomes containing ginger extract were synthetized and their antifungal effect on the growth and Aflatoxin production of Aspergillus flavus and Aspergillus parasiticus fungi was studied. Physiochemical characteristics of the sample were determined using XRD, FTIR, AFM, DLS and SEM. The resultant nanostructure can operation as an angiogenesis promoter and provide antifungal nanocarrier for improving the wound healing process. Antifungal activity of ginger extract was determined by disc diffusion and microplate dilution methods. The inhibitory effect of extract on Aflatoxin-B1 production was investigated using MIC method. Ginger concentration, cholesterol%, SPAN-60 and DPPC% were optimized by response surface method. FTIR analysis showed that ginger extract and nanoliponiosome had no chemical interaction resulting in the change of functional groups. SEM observation showed the spherical morphology of particles and the average size of 95 nm. It was also found out that ginger extract had a stronger antifungal effect against Aspergillus flavus fungus compared to Aspergillus parasiticus fungus. The results of this study showed that the ginger extract loaded nanoliponiosomes can be promising antifungal agents for improving wound healing process with high antifungal effects and low side effects.

Allelopathically inhibitory effects of eucalyptus extracts on the growth of Microcystis aeruginosa

Microcystis aeruginosa (M. aeruginosa), as the dominant algae in eutrophic water bodies, has caused a serious harm to the local eco-environment. A biological tool, employing allelopathic inhibitory of eucalyptus to control M. aeruginosa, has been receiving tremendous attention. This work presents the results of the allelopathic inhibitory effects of eucalyptus (Eucalyptus grandis × E.urophylla ‘GLGU9’) extracts of roots (ERE), stems (ESE), and leaves (ELE) on culture solutions of M. aeruginosa and its eco-physiological mechanism. The inhibitory effects of the extracts on the growth of M. aeruginosa varied greatly with ELE exhibiting the highest level of potency. Modes of action by which ELE inhibited M. aeruginosa growth were established. They involved reduction in photosynthesis, disruption of the cell membrane integrity, and inhibition of esterase activities of the cyanobacterial cells. However, ELE did not exhibit any gradients of toxicity towards zebrafish nor Washington grass plant. Species abundance and diversity in the systems remained likewise unaffected by ELE. The synergistic interaction between ELE and single-component allelochemicals (e.g., gallic acid and berberine) was ascribed to the increase in efficacy of allelochemicals in the various systems. The results of this study provide an underlying, novel, and attractive approach for controlling the growth of M. aeruginosa in aquatic environments.

Inhibition of Dipeptidyl Peptidase 4 (DPP IV) Activity by Some Indonesia Edible Plants

Background: Some edible plants are promising to control blood sugar level. These plants contained phenolic substances that suggested to be able to inhibit dipeptidyl peptidase 4 (DPP IV). Objective: The objective of this study was to investigate the inhibitory effect of several selected Indonesia plants on inhibiting of DPP IV activity and to determine the total phenolic content of the most active extract. Methods: Twelve Indonesia edible plants were macerated using 80% ethanol at room temperature. DPP IV activity was evaluated by using glycyl-prolyl-7-amino-4-methyl coumarin (Gly-Pro-AMC) substrate and the inhibitory effect of extracts were determined based on the level of free AMC group by measuring its fluorescence on excitation wavelength 350-360 nm and an emission wavelength 450-465 nm using a microplate reader. Total phenolic contents of the active extracts were determined with Folin-Ciocalteu 1:4 on 765 nm using microplate reader. Total anthocyanins from extract were determined using the pH differential method. Results: Among the tested samples, the extract of Ipomoea batatas roots at a concentration of 10 μg/mL showed the highest inhibition, followed by Cajanus cajan leaves and Gnetum gnemon rind, with percentage inhibition of 28.8, 24.9 and 24.1, respectively. I. batatas extract have an IC50 value of 65.53 μg/mL, while the IC50 value of the positive control Sitagliptin 9.37 μg/mL. Total phenolic content from the extracts of I. batatas, C. cajan and G. gnemon rind extract were 279.3; 152.8; and 141.3 mg GAE/gram, respectively. Total anthocyanin from I. batatas extract was 462.14 mg cyanidin- 3-glucoside/L. Conclusion: The extract of I. batatas showed the highest inhibition on DPP IV among other plants investigated and showed high content of phenolic compound and anthocyanin that correlated with activity as inhibitor DPP IV.

Eduscho Coffee Extract Effectively Inhibits the Formation of Amyloid-like Fibrils by Trypsin in Aqueous Ethanol

In this work we used an in vitro trypsin aggregation model to show that certain commercial coffee extracts can inhibit protein aggregation. Aggregation experiments were performed using several spectroscopic methods and a dye binding assay, such as turbidity, Congo red (CR) and electronic circular dichroism (ECD), that was further supported by transmission electron microscopy (TEM). A correlation was found between the anti-aggregation properties and the total phenolic content of the coffee extracts. The results revealed that the greatest effect was exerted by the Eduscho coffee extract. It was found that the inhibitory effect of this extract was concentration dependent. Using size exclusion chromatography, we demonstrated that the inhibitory effect of the Eduscho coffee extract on the formation of amyloid-like fibrils was due to its capacity to stabilize the oligomeric form of the protein.