LC-MS/MS, GC-MS and molecular docking analysis for phytochemical fingerprint and bioactivity of Beta vulgaris L.

The plants that we consume in our daily diet and use as a risk preventer against many diseases have many biological and pharmacological activities. In this study, the phytochemical fingerprint and biological activities of Beta vulgaris L. leaf extract, which are widely consumed in the Black Sea region, were investigated. The leaf parts of the plant were dried in an oven at 35 °C and then ground into powder. The main constituents in B. vulgaris were identified by LC-MS/MS and GC-MS analyses. Phenolic content, betaxanthin and betacyanin levels were investigated in the extracts obtained using three different solvents. The biological activity of the extract was investigated by anti-microbial, anti-mutagenic, anti-proliferative and anti-diabetic activity tests. Anti-diabetic activity was investigated by in vitro enzyme inhibition and in-silico molecular docking was performed to confirm this activity. In the LC-MS analysis of B. vulgaris extract, a major proportion of p_coumaric acid, vannilin, protecatechuic aldehyde and sesamol were detected, while the major essential oils determined by GC-MS analysis were hexahydrofarnesyl acetone and phytol. Among the solvents used, the highest extraction efficiency of 2.4% was obtained in methanol extraction, and 36.2 mg of GAE/g phenolic substance, 5.1 mg/L betacyanin and 4.05 mg/L betaxanthin were determined in the methanol extract. Beta vulgaris, which exhibited broad-spectrum anti-microbial activity by forming a zone of inhibition against all tested bacteria, exhibited anti-mutagenic activity in the range of 35.9-61.8% against various chromosomal abnormalities. Beta vulgaris extract, which did not exhibit mutagenic, sub-lethal or lethal effects, exhibited anti-proliferative activity by reducing proliferation in Allium root tip cells by 21.7%. 50 mg/mL B. vulgaris extract caused 58.9% and 55.9% inhibition of α-amylase and α-glucosidase activity, respectively. The interactions of coumaric acid, vanniline, hexahydrofarnesyl acetone and phytol, which are major compounds in phytochemical content, with α-amylase and α-glucosidase were investigated by in silico molecular docking and interactions between molecules via various amino acids were determined. Binding energies between the tested compounds and α-amylase were obtained in the range of - 4.3 kcal/mol and - 6.1 kcal/mol, while for α-glucosidase it was obtained in the range of - 3.7 kcal/mol and - 5.7 kcal/mol. The biological activities of B. vulgaris are closely related to the active compounds it contains, and therefore studies investigating the phytochemical contents of plants are very important. Safe and non-toxic plant extracts can help reduce the risk of various diseases, such as diabetes, and serve as an alternative or complement to current pharmaceutical practices.

Selective Removal of Chlorophyll and Isolation of Lutein from Plant Extracts Using Magnetic Solid Phase Extraction with Iron Oxide Nanoparticles.

In recent years, there has been a growing interest in plant pigments as readily available nutraceuticals. Photosynthetic pigments, specifically chlorophylls and carotenoids, renowned for their non-toxic antioxidant properties, are increasingly finding applications beyond their health-promoting attributes. Consequently, there is an ongoing need for cost-effective methods of isolation. This study employs a co-precipitation method to synthesize magnetic iron oxide nanoparticles. Scanning electron microscopy (SEM) coupled with energy dispersive spectrometry (EDS) confirms that an aqueous environment and oxidizing conditions yield nanosized iron oxide with particle sizes ranging from 80 to 140 nm. X-ray photoelectron spectroscopy (XPS) spectra indicate the presence of hydrous iron oxide FeO(OH) on the surface of the nanosized iron oxide. The Brunauer-Emmett-Teller (BET) surface area of obtained nanomaterial was 151.4 m2 g-1, with total pore volumes of pores 0.25 cm3 g-1 STP. The material, designated as iron oxide nanoparticles (IONPs), serves as an adsorbent for magnetic solid phase extraction (MSPE) and isolation of photosynthetic pigments (chlorophyll a, lutein) from extracts of higher green plants (Mentha piperita L., Urtica dioica L.). Sorption of chlorophyll a onto the nanoparticles is confirmed using UV-vis spectroscopy, Fourier transform infrared photoacoustic spectroscopy (FT-IR/PAS), and high-performance liquid chromatography (HPLC). Selective sorption of chlorophyll a requires a minimum of 3 g of IONPs per 12 mg of chlorophyll a, with acetone as the solvent, and is dependent on a storage time of 48 h. Extended contact time of IONPs with the acetone extract, i.e., 72 h, ensures the elimination of remaining components except lutein, with a spectral purity of 98%, recovered with over 90% efficiency. The mechanism of chlorophyll removal using IONPs relies on the interaction of the pigment's carbonyl (C=O) groups with the adsorbent surface hydroxyl (-OH) groups. Based on molecular dynamics (MD) simulations, it has been proven that the selective adsorption of pigments is also influenced by more favorable dispersion interactions between acetone and chlorophyll in comparison with other solutes. An aqueous environment significantly promotes the removal of pigments; however, it results in a complete loss of selectivity.

Extracts of Jamun seeds inhibited the growth of human (Hep-2) cancer cells.

INTRODUCTION: In the last century, the human laryngeal epithelioma has become a life-threatening disease leading to a high rate of mortality worldwide. The current investigation is focusing on the antiproliferative effect of Eugenia jambolana seed extracts against Hep-2 cancer cells. METHODS: The active compounds from the seeds of E. jambolana were extracted by the decoction extraction method using acetone, ethanol, and methanol. The filtrates from the different solvents were subjected to liquid-liquid separation before drying by a rotary evaporator. In various doses, the crude extracts and carcinoma were subjected to a methylthiazolyl diphenyl tetrazolium bromide assay. Cell viability was determined under ultraviolet visualization at an absorbance of 540 nm. The data of the viable cells were subjected to analysis of variance at P ≤ .01. RESULTS: Crude compounds of E. jambolana seeds extracted by acetone, methanol, and methanol extract had an anticarcinoma effect. Among the extracts, methanol extract possessed a recommendable anti-carcinoma effect compared to acetone and ethanol crude extracts. At a concentration of 125 µg/mL, the crude extracts of methanol, acetone, and ethanol destroyed 49.57, 35.01, and 27.67 carcinomas, respectively. The concentration of 31.25 µg/mL of acetone extract and 125 µg/mL of ethanolic extract affected 28.11 and 27.67 carcinomas, respectively. CONCLUSIONS: E.jambolana seeds possess anticarcinoma potency and thus can be administered in the reduction of proliferative carcinoma. The study recommended further studies which will involve the elution of pure compounds from the methanol extract of E. jambolana that possess antitumour and antiproliferative activity against Hep-2 cell lines.

Analyzing the Antioxidant Activity and Fatty Acid Composition of Monofloral Mullein (Verbascum sp.) Pollen Oil obtained via Various Extraction Techniques.

This study focused on characterizing fatty acids and evaluating the antioxidant properties in oils extracted from mullein (Verbascum sp.) bee-collected pollen, utilizing soxhlet and ultrasound-assisted methods with acetone and hexane solvents. Soxhlet extraction demonstrated high efficiency in mullein bee pollen oil extraction. The highest levels of total phenolic content (TPC), total flavonoid content (TFC), DPPH⋅, and ABTS⋅+ activities (41.07±1.43 mg GAE/g extract; 1.86±0.01 mg QE/g extract; 16.23±0.68 mg TE/g extract; 56.88±0.43 mg TE/g extract, respectively) were observed in oil extracted using the soxhlet method with acetone solvent. Conversely, ultrasound-assisted extraction with hexane yielded oils rich in saturated fatty acids, while acetone extraction contained higher monounsaturated fatty acids. Palmitic, linoleic, and oleic acids were predominant in the extracted oils. This study introduces, for the first time, the identification of fatty acids found in mullein bee pollen oil, along with an examination of their antioxidant properties. The choice of solvent was found to significantly influence compound extraction compared to the extraction method.

Solanum pseudocapsicum vs Capsicum annum; comparative phenolics profiling using green ultrasonic extraction and UHPLC analysis.

BACKGROUND: Solanum pseudocapsicum (PC) and Capsicum annum (CA) belongs to the family of Solanaceae. CA have been reported a rich source of phenolics whereas, the phenolics content of GA (gallic acid), SC (scopoletin), RA (rosmarinic acid), and RV (resveratrol) are yet to be reported for the PC-fruit. This study comparatively evaluates the phenolics profile for different parts (seeds and skin) and colors (green and red) of the PC- and CA-fruits using the green solvents of ethanol (ET), acetone (AC), water (H2O), and different combinations of these solvents. METHODOLOGY: Ultrasonics extraction (US) and UHPLC analysis were employed for phenolics evaluation. RESULTS: The USMD (method development) revealed the highest extract yield of 62 mg/100 mg for the PC-skin in ET:AC (70:30) solvent whereas, more phenolics (ppm) were observed for PC-seeds in ET:AC (50:50) solvent, particularly the SC (29.46) and GA (16.92). The UHPLCMDMV exhibited significant accuracies (100.70-114.14 %) with r2-values (0.9993-0.9997) in the linearity range of 1-200 ppm. The USMV (method validation) in PC- and CA-fruit parts and colors revealed more extract yields for the red skin part of the PC- (180.5 mg) and CA-fruit (126.2 mg). The phenolics were seen more in the green seeds of the PC-fruit (ppm); SC (276), GA (147.36), RV (28.54), and RA (23.87) followed by the green PC-skin, and red/green CA-seeds. The statistical models of mean differences, ANOVA, and Pearson's correlation showed significant differences for the PC-fruit parts (seeds and skin) and colors (red and green) vs extract yield and phenolics content (P = 0.05). CONCLUSION: PC-and CA-fruits were successfully evaluated where the seeds for the green fruits exhibited more phenolics amount.

Low levels of Cd2+ combined with procymidone may cause ovarian damage in mice via unfolded protein response.

As no study about the combined effect of low levels of Cd2+ with procymidone (PCM) on organs and organisms, we investigated their actions on mouse-ovary in vivo and in vitro. Four-week mice were treated with corn oil for the control group, corn oil + 0.0045 mg/L Cd2+ (CdCl2 was dissolved in ultrapure water and freely consumed by mice) for Cd2+ group, 50 mg/kg/d PCM (suspended in corn oil and administered orally to mice) for PCM group, and 50 mg/kg/d PCM + 0.0015 (0.0045 and 0.0135) mg/L Cd2+ for L+ (M+ and H+) PCM group for 21 days. For in vitro experiment, the cultured ovaries were treated with acetone for the control group, 0.1% acetone + 8.4 µg/L Cd2+ for the Cd2+ group, 0.63 mg/L PCM (dissolved in acetone) for the PCM-group, and 0.63 mg/L PCM + 2.8 (8.4 and 25.2) µg/L Cd2+ for L+ (M+ and H+) PCM group for 7 days. Mouse body weight in each treatment group, the weight and volume of ovaries in all PCM groups were lower than the control. Both in vivo and in vitro, all-stage follicle numbers were lower in M+PCM and H+PCM groups, whereas the atretic follicles and CASPASE3/8 were higher; meanwhile, lower estradiol and progesterone and higher unfolded protein response (UPR) members in all PCM groups. L+, M+, and H+PCM groups had further ovarian damage and stronger UPR than PCM groups, as did M+PCM groups over Cd2+ groups. It is hypothesized low-level PCM and Cd2+ may mutually promote each other's triggered UPR and exacerbate ovarian damage.

Oviposition Deterrent Activity of Some Wild Plants for Adult Females of Chrysomya albiceps with Medical and Veterinary Importance.

<b>Background and Objective:</b> <i>Chrysomya albiceps</i> is widely spread worldwide, causing myiasis in both humans and animals and playing a mechanical role in the spreading of helminths, viruses and bacteria. Searching for new and safe alternative control methods is very important to eliminate the transmission of pathogens. This study aims to determine the oviposition-deterrent activity of <i>Juniperus procera</i>, <i>Artemisia absinthium</i>, <i>Rosmarinus officinalis</i> and <i>Hypoestes forskaolii</i> wild plants against adult <i>Chrysomya albiceps</i>. <b>Materials and Methods:</b> The effect of plant extracts from <i>Juniperus procera</i>, <i>Artemisia absinthium</i>, <i>Rosmarinus officinalis</i> and <i>Hypoestes forskaolii</i> plants were tested against adult females of <i>Chrysomya albiceps</i> for oviposition deterrent or repellency. These extracts resulted in oviposition deterrent efficacy for adult females of <i>C. albiceps</i> based on the plant type, plant part (leaves or stems), extract type (methanol, acetone and petroleum ether) and tested dose. <b>Results:</b> The highest anti-oviposition activity against <i>C. albiceps</i> females presented from <i>A. absinthium</i> stems acetone extract at a dose of 1 mg cm² by 100 %, while at 0.5 mg cm² recorded remarkable repellency by 86.7% as compared with the control treatment. According to the dose-response relationship, <i>A. absinthium</i> methanol and acetone extracts were ED₅₀ values of 0.85, 0.319 mg cm² (leaves) and 1.88, 0.576 mg cm² (stems), followed by <i>J. procera</i> methanol extract by 0.983 mg cm² (leaves) and 0.98 mg cm² (stems), respectively achieved highest oviposition deterrent efficiency as compared with other extracts. <b>Conclusion:</b> The high repellency activities of these extracts can be utilized to stop <i>C. albiceps</i> flies from laying eggs on wounds and transmitting myiasis diseases to humans and animals and could potentially replace pesticides used in the future control programs of flies.

Bioactivities and Medicinal Value of the Fruiting Body Extracts of Laetiporus sulphureus and Meripilus giganteus Polypore Mushrooms (Agaricomycetes).

In the present investigation methanol and acetone extracts of basidiocarps of mushrooms Laetiporus sulphureus and Meripilus giganteus were evaluated for their antimicrobial, cytotoxic and antioxidant/prooxidant effects. The antimicrobial potential was determined by the microdilution method against ten microorganisms. Cytotoxic effects were evaluated by MTT test, while changes of the redox status parameters (superoxide anion radical, nitrites and reduced glutathione) were determined spectrophotometrically on a human colorectal cancer cell line and human health fibroblasts cells. The results were measured 24 and 72 h after the treatment. Tested extracts exhibited moderate antimicrobial activity with MIC values from 0.004 to 20 mg/mL. The maximum antimicrobial activity was found in the methanol extracts of the M. giganteus against Bacillus subtilis, which was better than positive control. The acetone extract of M. giganteus with IC5072h = 13.36 µg/mL showed significant cytotoxic effect with strong cell selectivity (selectivity index = 37.42) against cancer human colorectal cancer cells. The tested extracts, especially M. giganteus acetone extract, induced an increase in oxidative stress parameters in tested cell lines, but significantly heightened it in human colorectal cancer cells. The obtained results suggest that these extracts, especially M. giganteus acetone extract, can be proposed as a novel source of nutraceuticals and pharmaceuticals.

Assessment of antimicrobial, antidiabetic, and anti-inflammatory properties of acetone extract of Aerva lanata (L.) by in-vitro approach and bioactive compounds characterization.

The antimicrobial, antidiabetic, and anti-inflammatory activities efficiency of Aerva lanata plant extracts (aqueous (Aqu-E), acetone (Ace-E), and ethanol (Eth-E)) were investigated in this study. Furthermore, the active molecules exist in the crude extract were characterized by UV-Visible spectrophotometer, Fourier transform infrared (FTIR), High-performance liquid chromatography (HPLC), and Gas Chromatography-Mass Spectrometry (GC-MS) analyses. The preliminary phytochemical study revealed that the Ace-E restrain more phytochemicals like alkaloids, saponins, anthraquinone, tannins, phenolics, flavonoids, glycosides, terpenoids, amino acid, steroids, protein, coumarin, as well as quinine than Aqu-E and Eth-E. Accordingly to this Ace-E showed considerable antimicrobial activity as the follows: for bacteria S. aureus > E. coli > K. pneumoniae > P. aeruginosa > B. subtilis and for fungi T. viride > A.flavus > C. albicans > A.niger at 30 mg ml concentration. Similarly, Ace-E showed considerable antidiabetic (α-amylase: 71.7 % and α-glucosidase: 70.1 %) and moderate anti-inflammatory (59 % and 49.8 %) activities. The spectral and chromatogram studies confirmed that the Ace-E have pharmaceutically valuable bioactive molecules such as (Nbutyl)-octadecane, propynoic acid, neophytadiene, and 5,14-di (N-butyl)-octadecane. These findings suggest that Ace-E from A. lanata can be used to purify additional bioactive substances and conduct individual compound-based biomedical application research.

Casearia tomentosa fruit extracts exposed larvicidal activity and morphological alterations in Culex quinquefasciatus and Aedes albopictus under in vitro and semi field conditions.

Mosquitoes are notorious insects that transmit a wide range of infectious diseases, including zika, malaria, chikungunya, filariasis, and dengue. The overuse and incorrect application of synthetic pesticides to control mosquitoes has resulted in resistance development and environmental contamination, both of which have had a negative impact on human health. To address this issue, the larvicidal and pupicidal potential of acetone extract from Casearia tomentosa fruits was investigated. The extract was evaluated in a lab setting against all larval instars and pupa of Culex quinquefasciatus and Aedes albopictus, as well as against third instar larvae in a semi-field condition. Purified compounds through TLC were also tested against 3rd instar larvae of both mosquito and non-target organisms. The FT-IR and GC-MS analyses were used to characterise the extract. Morphological aberration caused by the acetone extract was observed using FESEM. The anal gills and respiratory siphon of both mosquitoes showed significant deformation from their normal state. 100 ppm was found to cause 100% larval mortality at 24 h of exposure in case of Cx. quinquefasciatus and at 72 h of exposure in Ae. albopictus larvae. After 72 h of exposure under in vitro conditions, the extract demonstrated considerable larvicidal activity with LC50 values of 38.33 and 47.56 against 3rd instar larvae of Culex quinquefasciatus and Aedes albopictus, respectively. The acetone extract can be considered as a highly effective mosquito larvicidal agent that is safe for the environment.

The Valorisation of Melissa officinalis Distillation By-Products for the Production of Polyphenol-Rich Formulations.

Lemon balm (Melissa officinalis) is an aromatic and medicinal plant, rich in bioactive ingredients and with superior antioxidant activity. The essential oil of this plant is an expensive product, so the use of the by-products of the essential oil industry is particularly useful. The aim of this research was to process Melissa officinalis distillation by-products to develop a series of polyphenol-rich formulations. In the present research, lemon balm was distilled in a laboratory-scale distiller, and the recovered by-product was used for further successive extractions with acetone and water, using a fixed-bed semi-batch extractor. Acetone extract exhibited relatively poor results as far as yield, phenolic composition and antiradical activity are concerned. However, the aqueous extract presented high yield in both total phenolic content (i.e., 111 mg gallic acid equivalents (GAE)/g, on a dry herb basis (dw)), and anti-radical capacity (205 mg trolox equivalents (TE)/g dw). On a dried extract basis, the results were also impressive, with total phenols reaching 322 mg GAE/g dry extract and antiradical capacity at 593 mg TE/g dry extract. The phenolic components of the extract were identified and quantified by HPLC-DAD. Rosmarinic acid was the major component and amounted to 73.5 mg/g dry extract, while the total identified compounds were quantified at 165.9 mg/g dry extract. Finally, formulations with two different wall materials (gum arabic-maltodextrin and maltodextrin) and two different drying methods (spray-drying and freeze-drying) were applied and evaluated to assess their performance, yield, efficiency and shelf-life of total phenolic content and rosmarinic acid concentration. From the present investigation, it is concluded that after one year of storage, rosmarinic acid does not decrease significantly, while total phenolic content shows a similar decrease for all powders. According to the yield and efficiency of microencapsulation, maltodextrin alone was chosen as the wall material and freeze-drying as the preferred drying method.

Phytochemical, bactericidal, antioxidant and anti-inflammatory properties of various extracts from Pongamia pinnata and functional groups characterization by FTIR and HPLC analyses.

The present research looked into possible biomedical applications of Pongamia pinnata leaf extract. The first screening of the phytochemical profile showed that the acetone extract had more phytochemicals than the other solvent extracts. These included more saponins, proteins, phenolic compounds, tannins, glycosides, flavonoids, steroids, and sugar. The P. pinnata acetone extract exhibited highest antibacterial activity against C. diphtheriae. The bactericidal activity was found in the following order: C. diphtheria (14 mm) > P. aeruginosa (10 mm) > S. flexneri (9 mm) > S. marcescens (7 mm) > S. typhi (7 mm) > S. epidermidis (7 mm) > S. boydii (6 mm) > S. aureus (3 mm) at 10 mg mL-1 concentration. MIC value of 240 mg mL-1 and MBC is 300 mg mL-1 of concentration with 7 colonies against C. diphtheriae was noticed in acetone extract. Acetone extract of P. pinnata was showed highest percentage of inhibition (87.5 %) at 625 mg mL-1 concentrations by DPPH method. Furthermore, the anti-inflammatory activity showed the fine albumin denaturation as 76% as well as anti-lipoxygenase was found as 61% at 900 mg mL-1 concentrations correspondingly. FT-IR analysis was used to determine the functional groups of compounds with bioactive properties. The qualitative examination of selected plants through HPLC yielded significant peak values determined by intervals through the peak value. In an acetone extract of P. pinnata, 9 functional groups were identified. These findings concluded that the acetone extract has high pharmaceutical value, but more in-vivo research is needed to assess its potential.

Flours from Spondias mombin and Spondias tuberosa seeds: Physicochemical characterization, technological properties, and antioxidant, antibacterial, and antidiabetic activities.

Yellow mombin (Spondias mombin) and Brazil plum (Spondias tuberosa) seeds are byproducts of exploiting their pulp and currently have no relevant food or industrial applications. Thus, the present study aimed to evaluate the physicochemical, technological, and functional characteristics of flours obtained from yellow mombin (YMF) and Brazil plum (BPF) residues. The flours presented a high percentage of insoluble fiber (68.8-70.2 g/100 g) and low carbohydrate (2.7-4.0 g/100 g) and caloric (91.9-95.3 kcal) values. The flours showed potential for technological application. In addition, the highest concentration of total phenolic content (31.1-50.2 mg GAE/g) was obtained with 70% acetone, which provided excellent results for antioxidant capacity evaluated by 2,2'-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) (81.0%-89.7%) and 2,2-diphenyl-1-picrylhydrazyl (60.6%-69.1%) radical scavenging capacity assays. Flour extracts in 70% acetone also exhibited inhibition of α-amylase (63.3%-78.8%) and amyloglucosidase (63.5%-71.0%). The antibacterial study revealed that extracts inhibited the growth of Escherichia coli, Burkholderia cepacia, and Burkholderia multivorans. Therefore, this study suggests the use of yellow mombin and Brazil plum residues for different food or industrial applications. PRACTICAL APPLICATION: The knowledge gained from this study will open a new approach to add value to yellow mombin and Brazil plum fruit seeds as sources of fiber and bioactive compounds, with promising application in the formulation of functional and nutraceutical products, benefiting both a sustainable environment and a sustainable industry.

Salazinic Acid and Norlobaridone from the Lichen Hypotrachyna cirrhata: Antioxidant Activity, α-Glucosidase Inhibitory and Molecular Docking Studies.

The present study was intended for the identification of secondary metabolites in acetone extract of the lichen Hypotrachyna cirrhata using UPLC-ESI-QToF-MS/MS and the detection of bioactive compounds. This study led to the identification of 22 metabolites based on their MS/MS spectra, accurate molecular masses, molecular formula from a comparison of the literature database (DNP), and fragmentation patterns. In addition, potent antioxidant and α-glucosidase inhibitory potentials of acetone extract of H. cirrhata motivated us to isolate 10 metabolites, which were characterized as salazinic acid (11), norlobaridone (12), atranorin (13), lecanoric acid (14), lichesterinic acid (15), protolichesterinic acid (16), methyl hematommate (17), iso-rhizonic acid (18), atranol (19), and methylatratate (20) based on their spectral data. All these isolates were assessed for their free radicals scavenging, radical-induced DNA damage, and intestinal α-glucosidase inhibitory activities. The results indicated that norlobaridone (12), lecanoric acid (14), methyl hematommate (17), and atranol (19) showed potent antioxidant activity, while depsidones (salazinic acid (11), norlobaridone (12)) and a monophenolic compound (iso-rhizonic acid, (18)) displayed significant intestinal α-glucosidase inhibitory activities (p < 0.001), which is comparable to standard acarbose. These results were further correlated with molecular docking studies, which indicated that the alkyl chain of norlobaridione (12) is hooked into the finger-like cavity of the allosteric pocket; moreover, it also established Van der Waals interactions with hydrophobic residues of the allosteric pocket. Thus, the potency of norlobaridone to inhibit α-glucosidase enzyme might be associated with its allosteric binding. Also, MM-GBSA (Molecular Mechanics-Generalized Born Surface Area) binding free energies of salazinic acid (11) and norlobaridone (12) were superior to acarbose and may have contributed to their high activity compared to acarbose.

Antimicrobial, antioxidant and cytotoxic activities of the leaf and stem extracts of Carissa bispinosa used for dental health care.

BACKGROUND: Carissa bispinosa (L.) Desf. ex Brenan is one of the plants used traditionally to treat oral infections. However, there is limited data validating its therapeutic properties and photochemistry. The aim of this study was to investigate the protective efficacy of the leaf and stem extracts of C. bispinosa against oral infections. METHODS: The phenolic and tannin contents were measured using Folin-Ciocalteau method after extracting with different solvents. The minimum inhibitory concentrations (MIC) of the extracts were assessed using the microdilution method against fungal (Candida albicans and Candida glabrata) and bacterial (Streptococcus pyogenes, Staphylococcus aureus and Enterococcus faecalis) strains. The 2-diphenyl-1-picrylhydrazyl (DPPH) and ferric reducing power (FRP) models were utilised to assess the antioxidant potential of the extracts. Cytotoxicity of the leaf acetone extract was evaluated using the methylthiazol tetrazolium assay. RESULTS: The methanol leaf extract had the highest phenolic content (113.20 mg TAE/g), whereas hexane extract displayed the highest tannin composition of 22.98 mg GAE/g. The acetone stem extract had the highest phenolic content (338 mg TAE/g) and the stem extract yielded the highest total tannin content (49.87 mg GAE/g). The methanol leaf extract demonstrated the lowest MIC value (0.31 mg/mL), whereas the stem ethanol extract had the least MIC value of 0.31 mg/mL. The stem methanol extract had the best DPPH free radical scavenging activity (IC50, 72 µg/mL) whereas the stem ethanol extract displayed maximum FRP with absorbance of 1.916. The leaf acetone extract had minimum cytotoxicity with the lethal concentration (LC50) of 0.63 mg/mL. CONCLUSIONS: The results obtained in this study validated the protective effect of C. bispinosa against oral infections.

Anti-microbial and anti-cancer efficacy of acetone extract of Rosa chinensis against resistant strain and lung cancer cell line.

BACKGROUND: Screening of herbal plants for various therapeutic properties is the hour as it shows promising activity. Scientific evidence of the pharmacological activity of the plant strengthens the traditional application of plants. METHODS: Rose flowers (Rosa chinensis) were procured and grounded into a coarse powder. The DNA was isolated from rose flower and molecular identification was performed by rbcL-BF and rbcL-724R primers. Antibacterial activity was evaluated by using disc and agar diffusion methods and the anti-cancer effect of the rose flower extract (RE) was examined using MTT assay in lung cancer cell line. The mechanism of cell death induced by RE was qualitatively measured using Acridine orange/Ethidium bromide staining and Hoechst staining. GC-MS analysis was performed using GC-MS-5975C. RESULT: The RE showed potent antimicrobial activity against various ATCC cultures. The rose extract strongly inhibits the growth of ESBL resistant organism along with inhibition of biofilm formation in the ESBL resistant organism. The extract caused apoptotic and necrotic cell death in lung cancer cells. GC-MS analysis demonstrated the presence of several biologically active compounds such as Clindamycin, Phytol, Octanoic acid, and Stigmasterol which might be the reason for the therapeutic properties of the plant. CONCLUSION: This study shows the antimicrobial and biofilm inhibition activity against the clinical isolates of Klebsiella pneumonia. The study shows the cytotoxic and apoptotic activity in A549 cancer cell line. Thus, the plant may act as a potent antimicrobial drug against resistant strains.

Preliminary Study on the Antibacterial Activities and Antibacterial Guided Fractionation of Some Common Medicinal Plants Practices in Itum Bahal, Kathmandu Valley of Nepal.

The aim of this study was to evaluate the antibacterial activities of selected medicinal plant practices by a traditional healer of the Newar community in Itum Bahal, Kathmandu, Nepal. The antibacterial activities of the methanolic extract (1 mg/disc) of fifteen medicinal plants were screened against two Gram-positive bacteria (Staphylococcus aureus ATCC 25923 and Bacillus subtilis ATCC 6633) and two Gram-negative bacteria (Escherichia coli ATCC 25922 and Salmonella typhi CCM 5445) using the disc diffusion method. Minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) were calculated for the different fractions (hexane, chloroform, ethyl acetate, acetonitrile, and acetone) of the plants having a significant antimicrobial effect. Only Quercus infectoria G. Olivier (galls) and Mallotus repandus (Willd.) Müll.Arg. (seeds) exhibited prominent antibacterial effects. The acetone fraction from Q. infectoria had the strongest antibacterial effect, with a 41.00 mm inhibition zone against S. aureus. In contrast, the ethyl acetate fraction in M. repandus exhibited the highest efficacy, producing a 29.00 mm inhibition zone against S. typhi. In a similar manner, in the case of Q. infectoria, the acetoe fraction depicted the lowest MIC (0.19 mg/mL) and MBC (0.98 mg/mL) values against S. aureus, whereas the ethyl acetate fraction of M. repandus was most significant, showing the lowest MIC and MBC of 0.25 and 0.53 mg/mL, respectively, against S. typhi. This study suggested that the acetone extract of Q. infectoria galls can be used as a potential source against Gram-positive bacteria, whereas the ethyl acetate extract of M. repandus seeds could serve as a useful source to inhibit Gram-negative bacteria. Furthermore, extensive scientific investigation is mandatory to ensure the proper use of folk medicines.

Cytotoxic, anti-proliferative, and apoptotic evaluation of Ramalina sinensis (Ascomycota, Lecanoromycetes), lichenized fungus on oral squamous cell carcinoma cell line; in-vitro study.

BACKGROUND: Scientists and medical professionals are actively striving to improve the efficacy of treatment methods for oral squamous cell carcinoma (OSCC), the most frequently occurring cancer within the oral cavity, by exploring the potential of natural products. The active pharmacological compounds found in lichenized fungi have shown potential for aiding in cancer treatment. Recent research aims to evaluate the impact of the lichenized fungus Ramalina sinensis (R. sinensis) on the cell viability and apoptosis of OSCC cell lines, considering the anti-inflammatory and anti-cancer capabilities of lichens. METHODS: Ramalina sinensis (Ascomycota, Lecanoromycetes) was selected for investigation of its effects on a human oral squamous cell carcinoma cell line. Acetone and methanol extracts of R. sinensis on an OSCC cell line (KB cell line, NCBI Code: C152) were investigated. Viability was assessed by MTT assay analysis, and apoptotic cells were measured using flow cytometry analysis. Scratch assay was used to assess cell migration. The chemical composition and metabolic profiling of R. sinensis were investigated. RESULTS: The growth and multiplication of KB cells were observed to undergo a gradual but remarkable inhibition when exposed to various concentrations. Specifically, concentrations of 6.25, 12.5, 25, 50, 100, and 200 µg/mL exhibited a significant suppressive effect on the proliferation of KB cells. The inhibition of cell proliferation exhibited a statistically significant difference between the extracts obtained from acetone and methanol. Flow cytometry results show an increase in apoptosis of OSCC cells by acetone extract. R. sinensis exerted a concentration-dependent inhibitory effect on the migration of OSCC cells. The chemical composition of R. sinensis was investigated using liquid chromatography positive ion electrospray ionization tandem mass spectrometry (LC-ESI-MS/MS), and 33 compounds in the acetone and methanol extracts of R. sinensis were detected. CONCLUSION: The findings provide evidence supporting the beneficial effects of R. sinensis extract on inducing apoptosis in OSCC cells and exerting anti-cancer properties.

Antibacterial Activity of Culinary-Medicinal Polypore Mushroom Lentinus tigrinus (Agaricomycetes).

Medicinal mushrooms belonging to Lentinus spp. exhibit significant antibacterial activities, but little attention has been paid to their efficacy against the food-borne pathogen, Bacillus cereus. The present study for the first time quantitatively evaluated the antibacterial activity of different extracts from fruiting bodies of a well-authenticated Iranian native strain of medicinal mushroom, Lentinus tigrinus, against Gram-positive spore-forming bacterium B. cereus. The findings revealed that the acetone extract inhibited the growth of B. cereus at concentrations as low as 31.25 µg/ML, while it had no effect against Escherichia coli and Staphylococcus aureus even at 10,000 µg/ML. The rest of the bacteria were also susceptible to the acetone extract at concentrations greater than 5 mg/ML. Antibacterial activities of the methanol-ethyl acetate extract and the hot water extract were significantly weaker than that of the acetone extract, which contained high amounts of total phenols (5.83 ± 0.08 mg GAE/g, dw), while Fourier transform infrared spectroscopy (FT-IR) confirmed the presence of functional groups, such as hydroxyl, carbonyl, amide, and amine. Further studies by scanning electron microscopy (SEM) confirmed obvious changes in the morphology of B. cereus in response to the acetone extract of L. tigrinus. This study may suggest that L. tigrinus could be a good natural source for isolating and purifying antibacterial compounds against B. cereus.