Study of Liposomes Containing Extract from the Leaves of Protium heptaphyllum (Aubl.) March in Animals Submitted to a Mutagenic Model Induced by Cyclophosphamide.

Cyclophosphamide (CPA) is an alkylating agent used as a chemotherapy agent in the treatment of cancer, but it has immunosuppressive effects. Protium heptaphyllum (P. heptaphyllum) is a plant rich in triterpenes and flavonoids, with some bioactive and therapeutic properties presented in the literature. Thus, the present study aimed to investigate the chemoprotective potential of P. heptaphyllum extract inserted into liposomes against oxidative damage chemically induced by CPA. Male Swiss mice received 1.5 mg/kg of P. heptaphyllum liposomes as a pre-treatment for 14 consecutive days (via gavage) and 100 mg/kg of CPA in a single dose (via intraperitoneal) on the 15th day. After the experimental period, blood and organ samples were collected for histopathological and biochemical analyses, including superoxide dismutase (SOD), glutathione peroxidase (GPx), catalase (CAT), glutathione S-transferase (GST), reduced glutathione (GSH), thiobarbituric acid reactive substances (TBARS), ascorbic acid (ASA), carbonyl protein, cytokine measurement, and micronucleus testing. The results showed that liposomes containing P. heptaphyllum extract have an antimutagenic effect against damage induced to DNA by CPA, and that they also protect against oxidative stress, as verified by the increase in the antioxidant enzymes SOD and GPx. The improvement in alkaline phosphatase and creatinine markers suggests a beneficial effect on the liver and kidneys, respectively. However, the depletion of GSH in the liver and brain suggests the use of antioxidants for the metabolism of molecules generated in these tissues. In general, these data show good prospects for the use of P. heptaphyllum liposomes as a cancer chemoprotective agent, as well as possible antioxidant action, conceivably attributed to the flavonoids present in the plant extract.

Optimization of Phenolic Compounds Extraction from Aerial Parts of Fabiana punensis S. C. Arroyo by Ultrasound- and Microwave-Assisted Extraction.

Fabiana punensis S. C. Arroyo is a subshrub or shrub that is indigenous to the arid and semiarid region of northern Argentina and is known to possess several medicinal properties. The objective of this study was to optimize the extraction conditions so as to maximize the yield of bioactive total phenolic compound (TPC) and flavonoids (F) of F. punensis' aerial parts by using non-conventional extraction methods, namely ultrasound-assisted extraction, UAE, and microwave-assisted extraction, MAE, and to compare the biological activities and toxicity of optimized extracts vs. conventional extracts, i.e., those gained by maceration. Response Surface Methodology (RSM) was used to apply factorial designs to optimize the parameters of extraction: solid-to-liquid ratio, extraction time, ultrasound amplitude, and microwave power. The experimental values for TPC and F and antioxidant activity under the optimal extraction conditions were not significantly different from the predicted values, demonstrating the accuracy of the mathematical models. Similar HPLC-DAD patterns were found between conventional and UAE- and MAE-optimized extracts. The main constituents of the extracts correspond to phenolic compounds (flavonoids and phenolic acids) and apigenin was identified. All extracts showed high scavenger capacity on ABTS•+, O2•- and H2O2, enabling the inhibition of the pro-inflammatory enzymes xanthine oxidase (XO) and lipoxygenase (LOX). They also showed an antimutagenic effect in Salmonella Typhimurium assay and cytotoxic/anti-proliferative activity on human melanoma cells (SKMEL-28). Toxicological evaluation indicates its safety. The results of this work are important in the development of efficient and sustainable methods for obtaining bioactive compounds from F. punensis for the prevention of chronic degenerative diseases associated with oxidative stress, inflammation, and DNA damage.

Phytochemical Constituent Analysis of Phyllanthus emblica L. Fruit Nanoherbals by LC-HRMS and Their Antimutagenic Activity and Teratogenic Effects.

Pregnant women must be wary of using traditional medicines due to the possibility of their having oxytoxic effects. Indonesia is rich in plants containing antioxidants. One of these plants is Phyllanthus emblica L. This study aims to determine the phytochemical constituents of Phyllanthus emblica L. fruit nanoherbals by LC-HRMS analysis and their antimutagenic activity and teratogenic effects. The study commenced by producing nanoherbal extracts from P. emblica fruit. The phytochemical composition of these extracts was then analyzed using LC-HRMS. The nanoherbal extracts were also tested for their ability to prevent mutations, as indicated by a reduction in micronuclei observed in mouse femur bone marrow smear preparations. The teratogenicity test involved administering the P. emblica fruit nanoherbal at 100, 500, and 1000 mg/kg BW doses. The data were analyzed using SPSS. The phytochemical constituents of the P. emblica fruit nanoherbal include flavonoids, phenols, vitamins, and alkaloids. The P. emblica fruit nanoherbal exhibits antimutagenic activity, as evidenced by a statistical analysis that indicated a significant decrease in the quantity of micronuclei per 200 PCE compared to the negative control (p < 0.05). The administration of the P. emblica fruit nanoherbal at a dosage of 1000 mg/kg BW resulted in a teratogenic impact during the organogenesis stage, as shown by hemorrhage and anomalies in the sternum.

In vitro Propagation of Endemic Species Mahonia Jaunsarensis Ahrendt Through Callus Culture.

Mahonia jaunsarensis Ahrendt (Family Berberidaceae) an endemic species was successfully propagated in vitro. An efficient propagation protocol has been developed first time. The callus cultures were established from leaf explants on Murashige and Skoog (MS) medium supplemented with 2,4-Dichlorophenoxyacetic acid (2,4-D; 1 µM) and resulted 70% callus induction with green compact callus. When callus was transferred to MS medium containing Thidiazuron (TDZ; 0.75 µM), maximum average number of shoot (3.06) produced but shoot length (3.37 cm) and average leaf number (2.87) was increased upon transfer to MS medium containing N6-benzylaminopurine (BA; 6.0 µM) plus α-naphthalene acetic acid (NAA; 0.5 µM). In MS medium containing indole-3-butyric acid (IBA; 0.01 µM), the maximum rooting percentage (56%) and average root number (2.56) per shoot and root length (3.33 cm) were recorded. The rooted plantlets transferred in vermiculite + garden soil + farmyard manure (1:1:1) with maximum (55%) survival percentage under greenhouse condition. The phytochemical analysis of leaves obtained from tissue culture-raised plants revealed significantly higher levels of alkaloids (berberine and palmatine) than those obtained from wild plants. Similar trends were observed for antioxidant and antimutagenic activities. Results of this study offer a baseline for the conservation and sustainable utilization strategies for M. jaunsarensis.

Characterization of the Chemopreventive Properties of Cannabis sativa L. Inflorescences from Monoecious Cultivars Grown in Central Italy.

Hemp bioproducts hold great promise as valuable materials for nutraceutical and pharmaceutical applications due to their diverse bioactive compounds and potential health benefits. In line with this interest and in an attempt to valorize the Lazio Region crops, this present study investigated chemically characterized hydroalcoholic and organic extracts, obtained from the inflorescences of locally cultivated Felina 32, USO 31, Ferimon and Fedora 17 hemp varieties. In order to highlight the possible chemopreventive power of the tested samples, a bioactivity screening was performed, which included studying the antimutagenic activity, radical scavenging power, cytotoxicity in human hepatoma HepG2 cells, leakage of lactate dehydrogenase (LDH) and modulation of the oxidative stress parameters and glucose-6-phosphate dehydrogenase (G6PDH) involved in the regulation of the cell transformation and cancer proliferation. Tolerability studies in noncancerous H69 cholangiocytes were performed, too. The organic extracts showed moderate to strong antimutagenic activities and a marked cytotoxicity in the HepG2 cells, associated with an increased oxidative stress and LDH release, and to a G6PDH modulation. The hydroalcoholic extracts mainly exhibited radical scavenging properties with weak or null activities in the other assays. The extracts were usually well-tolerated in H69 cells, except for the highest concentrations which impaired cell viability, likely due to an increased oxidative stress. The obtained results suggest a possibility in the inflorescences from the Felina 32, USO 31, Ferimon and Fedora 17 hemp varieties as source of bioactive compounds endowed with genoprotective and chemopreventive properties that could be harnessed as preventive or adjuvant healing strategies.

Influence of Complexation with ß- and γ-Cyclodextrin on Bioactivity of Whey and Colostrum Peptides.

Dairy protein hydrolysates possess a broad spectrum of bioactivity and hypoallergenic properties, as well as pronounced bitter taste. The bitterness is reduced by complexing the proteolysis products with cyclodextrins (CDs), and it is also important to study the bioactivity of the peptides in inclusion complexes. Hydrolysates of whey and colostrum proteins with extensive hydrolysis degree and their complexes with ß/γ-CD were obtained in the present study, and comprehensive comparative analysis of the experimental samples was performed. The interaction of CD with peptides was confirmed via different methods. Bioactivity of the initial hydrolysates and their complexes were evaluated. Antioxidant activity (AOA) was determined by fluorescence reduction of fluorescein in the Fenton system. Antigenic properties were studied by competitive enzyme immunoassay. Antimutagenic effect was estimated in the Ames test. According to the experimental data, a 2.17/2.78-fold and 1.45/2.14-fold increase in the AOA was found in the ß/γ-CD interaction with whey and colostrum hydrolysates, respectively. A 5.6/5.3-fold decrease in the antigenicity of whey peptides in complex with ß/γ-CD was detected, while the antimutagenic effect in the host-guest systems was comparable to the initial hydrolysates. Thus, bioactive CD complexes with dairy peptides were obtained. Complexes are applicable as a component of specialized foods (sports, diet).

Interaction of heavy metals in Drosophila melanogaster larvae: Fourier transform infrared spectroscopy and single-cell electrophoresis study.

The present study evaluates the Murraya Koenigii (CuLE) and Tinospora Crispa (TiSE) antimutagenic effect and the impact of industrial soil and solid waste leachate on Drosophila larvae. Larvae were exposed to leachate prepared at different pH (7, 4.93, 2.88) and treated with TiSE and CuLE at different concentration (4 g/L and 6 g/L) mixed with standard Drosophila medium. Emphasis was given to the binding interaction of heavy metals with proteins in Drosophila. The change in structure and molecular composition in Drosophila by leachate containing heavy metals induced toxicity has been studied by using Fourier transform infrared (FTIR) spectroscopy. Results from the study demonstrated that CuLE/TiSE administration restored the level of oxidative stress as evidenced by an enhanced antioxidant system and a decrease in lipid peroxidation and protein oxidation. The amide I and amide II bands spectral shifting revealed the binding interaction. The shift in the peak of PO2- asymmetric stretching might be due to compositional changes in nucleic acids. Single-cell electrophoresis was performed to detect the DNA damage which also proved to be ameliorated by administration of CuLE/TiSE. The result concludes that CuLE/TiSE may have great potential in the protection of Drosophila larvae from leachate induced oxidative stress through antioxidant and antimutagenic mechanisms this might help to cope with environmental toxicants.Communicated by Ramaswamy H. Sarma.

Anticarcinogenic impact of extracellular vesicles (exosomes) from cord blood stem cells in malignant melanoma: A potential biological treatment.

Incidence of Malignant Melanoma has become the 5th in the UK. To date, the major anticancer therapeutics include cell therapy, immunotherapy, gene therapy and nanotechnology-based strategies. Recently, extracellular vesicles, especially exosomes, have been highlighted for their therapeutic benefits in numerous chronic diseases. Exosomes display multifunctional properties, including inhibition of cancer cell proliferation and initiation of apoptosis. In the present in vitro study, the antitumour effect of cord blood stem cell (CBSC)-derived exosomes was confirmed by the CCK-8 assay (p < 0.05) on CHL-1 melanoma cells and improve the repair mechanism on lymphocytes from melanoma patients. Importantly, no significant effect was observed in healthy lymphocytes when treated with the exosome concentrations at 24, 48 and 72 h. Comet assay results (OTM and %Tail DNA) demonstrated that the optimal exosome concentration showed a significant impact (p < 0.05) in lymphocytes from melanoma patients whilst causing no significant DNA damage in lymphocytes of healthy volunteers was 300 µg/ml. Similarly, the Comet assay results depicted significant DNA damage in a melanoma cell line (CHL-1 cells) treated with CBSC-derived exosomes, both the cytotoxicity of CHL-1 cells treated with CBSC-derived exosomes exhibited a significant time-dependent decrease in cell survival. Sequencing analysis of CBSC exosomes showed the presence of the let-7 family of miRNAs, including let-7a-5p, let-7b-5p, let-7c-5p, let-7d-3p, let-7d-5p and two novel miRNAs. The potency of CBSC exosomes in inhibiting cancer progression in lymphocytes from melanoma patients and CHL-1 cells whilst causing no harm to the healthy lymphocytes makes it a potential candidate as an anticancer therapy.

Resonance structure contributions, flexibility, and frontier molecular orbitals (HOMO-LUMO) of pelargonidin, cyanidin, and delphinidin throughout the conformational space: application to antioxidant and antimutagenic activities.

This research refers to the study and understanding of the conformational space of the positive-charged anthocyanidin structures in relation with the known chemical reactivities and bioactivities of these compounds. Therefore, the planar (P) and nonplanar (Z) conformers of the three hydroxylated anthocyanidins pelargonidin, cyanidin, and delphinidin were analyzed throughout the conformational space at the B3LYP/6-311 ++ G** level of theory. The outcome displayed eleven new conformers for pelargonidin, fifty-four for cyanidin, and thirty-one for delphinidin. Positive-charged quinoidal structures showed a significant statistical weight in the conformational space, thus coexisting simultaneously with other resonance structures, such that under certain reaction conditions, the anthocyanidins behave as positive-charged quinoidal structures instead of oxonium salts. The calculations of the permanent dipole moment and the polarizability showed relationships with the quantity and arrangement of hydroxyls in the structure. In addition, theoretical calculations were used to analyze the frontier molecular orbitals (HOMO-LUMO) of the three anthocyanidins. The novel conception of this work lies in the fact that dipole moment, polarizability, and HOMO-LUMO values were related to the reactivity/bioactivity of these three anthocyanidins. HOMO-LUMO energy gaps were useful to explain the antioxidant activity, while the percent atom contributions to HOMO were appropriate to demonstrate the antimutagenic activity as enzyme inhibitors, as well as the steric and electrostatic requirements to form the pharmacophore. Delphinidin was the strongest antioxidant anthocyanidin, and pelargonidin the best anthocyanidin with antimutagenic activity.

Antigenotoxic and antimutagenic effects of lignin derivative BP-C2 against dioxidine and cyclophosphamide in vivo in murine cells.

The study investigated antigenotoxic and antimutagenic activity of novel lignin-derived polyphenolic composition (BP-C2) with ammonium molybdate towards cyclophosphamide and dioxidine in the bone marrow, blood and liver cells of BALB/c mice. BP-C2 was given to mice via gavage at 60, 80 and 120 mg/kg once 1 h before single intraperitoneal injection of a genotoxic agent. 1.5 h and 3 h after dioxidine or cyclophosphamide injection, respectively, cellular suspensions were obtained from mice and assessed with the comet test and cytogenetic analysis of bone marrow cells. It was observed that antigenotoxic activity of BP-C2 against DNA damage induced by dioxidine, a prooxidant genotoxic agent, in the bone marrow, liver and blood cells of mice in vivo was more pronounced at 60 and 80 mg/kg than at 120 mg/kg. When cyclophosphamide was used to induce a DNA damage, the genoprotective effect of BP-C2 was observed in bone marrow, liver and blood cells at 60 mg/kg dose but the effect was not significant at 80 mg/kg. When co-administered with 120 mg/kg BP-C2, cyclophosphamide induced a higher level of DNA damage in liver cells, but its genotoxic effect in bone marrow and blood cells was the same as when it was administered alone. When assessing the effect of BP-C2 on chromosomal aberrations induced by cyclophosphamide and dioxidine in bone marrow cells, it was revealed that all three tested doses of BP-C2 significantly decreased the number of cells with chromosome abnormalities. Thus, BP-C2 has a pronounced antimutagenic and genoprotective effects.

Microencapsulation of Phenolic Extract from Sea Grape (Coccoloba uvifera L.) with Antimutagenic Activity.

This study aimed to microencapsulate the sea grape ethanolic extract by the spray drying process, characterizing the obtained powder, and evaluating its antimutagenicity activity. Microparticles showed a mean size of 6.28 µm and a spherical shape with a smooth surface. The powder had a low moisture content (4.02±0.92 %) and water activity (0.27±0.01), and high solubility (76±3.60 %). Moreover, hygroscopicity (14.75±2.63 g/100 g of powder) and bulk density (0.63±0.03 g/cm3 ) values suggested that this powder can be easily handled at a pilot or industrial scale. In addition, microencapsulation protected the extract against oxidation by ultraviolet light, improved its thermal stability, and its antimutagenicity activity was similar to fresh sea grape extract. In conclusion, the microencapsulation with maltodextrin by spray drying technique is an alternative to protect bioactive compounds from sea grapes against environmental conditions, maintaining their antimutagenic activity.

Chemical Composition, In Silico and In Vitro Antimutagenic Activities of Ethanolic and Aqueous Extracts of Tigernut (Cyperus esculentus).

Tigernut, also known as Cyperus esculentus, is said to be high in nutritional and medicinal value. The purpose of this study was to determine the C. esculentus's antimutagenic activity. The ethanolic and aqueous extracts of the nut were analyzed for chemical constituents, antioxidants, ultraviolet-visible, and gas chromatography-mass spectrometry using standard procedures. The extracts contained a total of 17 major compounds that were docked against human RecQ-like protein 5 (RECQL5) helicase protein. The antimutagenic property of the ethanolic extract in vitro was assessed using the Allium cepa chromosome assay. Onion bulbs were pre-treated with 200 mg/kg of ethanolic extract of C. esculentus for 24 h and then, grown in NaN3 (250 µg/L) for 24 h; onion bulbs were also first exposed to NaN3 (250 µg/L) for 24 h before treatment with 100 mg/kg and 200 mg/kg of the ethanolic extract respectively. Standard methods were used to determine the mitotic index and chromosomal aberrations. Results revealed that C. esculentus ethanolic extract contained flavonoids (22.47 mg/g), tannins (0.08 mg/g), alkaloids (19.71 mg/g), glycosides, phenol, and tannin and showed high scavenging activity against 2,2-diphenyl-1-picrylhydrazyland H2O2. Docking with RECQL5 showed good binding energies (∆G>-7) of five compounds in C. esculentus ethanolic extract. The A. cepa assay results revealed a significant (P<0.05) reduction in chromosomal aberrations and a higher mitotic index in groups treated with the C. esculentus ethanolic extract. The antimutagenic activity of C. esculentus ethanolic extract was attributed to its high levels of phytosterols and phenolic compounds.

Inhibition of Escherichia coli nitroreductase by the constituents in Syzygium aromaticum.

Gut bacterial nitroreductases play an important role in reduction of various nitroaromatic compounds to the corresponding N-nitroso compounds, hydroxylamines or aromatic amines, most of which are carcinogenic and mutagenic agents. Inhibition of gut nitroreductases has been recognized as an attractive approach for reducing mutagen metabolites in the colon, so as to prevent colon diseases. In this study, the inhibitory effects of 55 herbal medicines against Escherichia coli(E. coli) nitroreductase (EcNfsA) were examined. Compared with other herbal extracts, Syzygium aromaticum extract showed superior inhibitory potency toward EcNfsA mediated nitrofurazone reduction. Then, the inhibitory effects of 22 major constituents in Syzygium aromaticum against EcNfsA were evaluted. Compared with other tested natural compounds, ellagic acid, corilagin, betulinic acid, oleanic acid, ursolic acid, urolithin M5 and isorhamnetin were found with strong to moderate inhibitory effect against EcNfsA, with IC50 values ranging from 0.67 to 28.98 mol·L-1. Furthermore, the inhibition kinetic analysis and docking simulation demonstrated that ellagic acid and betulinic acid potently inhibited EcNfsA (Ki < 2 µmol·L -1) in a competitively inhibitory manner, which created strong interactions with the catalytic triad of EcNfsA. In summary, our findings provide new scientific basis for explaining the anti-mutagenic activity of Syzygium aromaticum, where some newly identified EcNfsA inhibitors can be used for developing novel agents to reduce the toxicity induced by bacterial nitroreductase.

Antioxidant and antimutagenic properties of probiotic Lactobacilli determined using LUX-biosensors.

The initial screening of probiotic strains in vitro, carried out by different methods, may omit strains that are promising from the point of view of biotechnology or, conversely, mark as promising strains those that will lose activity when transferred in vivo. It is known that the release of metabolites by probiotic bacteria, in particular, lactobacilli, is highly dependent on the biochemical context. In this work, we modified the method that was previously successfully used for the selection of probiotics for poultry, based on their antioxidant and DNA-protective properties. A comparison was made of this activity on standard media and on an artificial intestinal medium that mimics the intestines of a bird. As a result, three Lactobacillus strains were selected, which not only exhibit antioxidant and DNA-protective properties but also do not lose these activities in an artificial intestinal medium.

Antimutagenic Activity as a Criterion of Potential Probiotic Properties.

The antimutagenic activity of probiotic strains has been reported over several decades of studying the effects of probiotics. However, this activity is rarely considered an important criterion when choosing strains to produce probiotic preparations and functional food. Meanwhile, the association of antimutagenic activity with the prevention of oncological diseases, as well as with a decrease in the spread of resistant forms in the microbiota, indicates its importance for the selection of probiotics. Besides, an antimutagenic activity can be associated with probiotics' broader systemic effects, such as geroprotective activity. The main mechanisms of such effects are considered to be the binding of mutagens, the transformation of mutagens, and inhibition of the transformation of promutagens into antimutagens. Besides, we should consider the possibility of interaction of the microbiota with regulatory processes in eukaryotic cells, in particular, through the effect on mitochondria. This work aims to systematize data on the antimutagenic activity of probiotics and emphasize antimutagenic activity as a significant criterion for the selection of probiotic strains.

A perspective review on medicinal plant resources for their antimutagenic potentials.

Mutagens present in the environment manifest toxic effects and are considered as serious threat for human health and healthcare. Recent reports reveal that medicinal plant resources are being explored for identifying potent antimutagenic as well as cancer preventing agents. There is mounting evidence that cancer and other mutation-related diseases can be prevented with the use of medicinal pant resources including crude extracts, active fractions, phytochemicals, and pure phytomolecules. These medicinal plant resources possessing antimutagenic potentials have been shown to target molecular mechanisms underlying the mutagenic impacts. Technological advents and high-throughput screening/activity methods have revolutionized this field, though several potent plants and their active principles have been reported as effective antimutagens. The translational success rate needs to be improved, but the trends are encouraging. In this review, we present the current understandings and updates on various mutagens in the environment, toxicities related/attributed to them, the resultant mutations (and cancer), and how medicinal plants come to the rescue. A perspective review has been presented on whether and how medicinal plant resources can be an effective approach for addressing mutagens in the environment. An account of medicinal plant resources used as antimutagenic agents has been given along with the underlying mechanism of action and their therapeutic potential in various models of cancer. Recent success stories, current challenges, and future prospects are discussed.

Safety and biological activity evaluation of Uncaria rhynchophylla ethanolic extract.

Uncaria rhynchophylla (UR) belongs to the Rubiaceae family, and its dried hooks are usually used in traditional medicine. It is effective in treating diseases related to the central nervous system. This study aimed to evaluate the safety of UR extract, investigate its antimutagenic and antioxidative activities, and elucidate its active components. Extraction and fractionation of the UR extract resulted in yields of 6.71%, 0.037%, 0.042%, 0.152%, 0.332%, and 5.132%, for hexane, ether, DCM, EtOAC, and aqueous fractions, respectively. The four indole alkaloids, total phenolic content (TPC), and total flavonoid content (TFC) of UR extract and its subfractions were measured. Alkaloid content was highest in the UR extract. TPC was the highest in the EtOAC fraction (373.7 ± 20.9 mg gallic acid equivalent (GAE)/g), whereas TFC was the highest in the UR extract (33.5 ± 2.4 mg quercetin equivalent (QE)/g). To assess the safety of UR extract mutagenicity, cytotoxicity, and oxidative stress inducibility assays were performed. The UR extract (2000 µg/plate) showed excellent antimutagenic activity (above 90%) against BaP in both TA98 and TA100 strains. The UR extract exhibited efficient DPPH (RC50 239.2 ± 16.5 µg/mL) and ABTS scavenging activity (RC50 458.7 ± 25.0 µg/mL). The UR extract (150 µg/mL) showed cytoprotective activity (65.6% ± 9.2%) against t-BHP. Among the subfractions, the EtOAC fraction possessed the strongest activities, overall. UR generally showed excellent biological activity at nontoxic concentrations (determined in vitro in current work), although the chemical composition of UR requires further investigation prior to its potential future use.

Essential oils as anticancer agents: Potential role in malignancies, drug delivery mechanisms, and immune system enhancement.

Cancer retains a central place in fatality rates among the wide variety of diseases known world over, and the conventional synthetic medicaments, albeit used until now, produce numerous side effects. As a result, newer, better, and safer alternatives such as natural plant products, are gravely required. Essential oils (EOs) offer a plethora of bioactivities including antibacterial, antiviral, antioxidant, and anticancer properties, therefore, the use of EOs in combination with synthetic drugs or aromatherapy continues to be popular in many settings. In view of the paramount importance of EOs and their potential bioactivities, this review summarizes the current knowledge on the interconnection between EOs and cancer treatment. In particular, the current review presents an updated summary of the chemical composition of EOs, their current applications in cancer treatments based on clinical studies, and the mechanism of action against the cancer cell lines. Similarly, an overview of using EOs in aromatherapy and enhancing immunity during cancer treatment is provided. Further, this review focuses on the recent technological advancements such as the loading of EOs using protein microspheres, ligands, or nanoemulsions/nanoencapsulation, which offer multiple benefits in cancer treatment via site-specific and target-oriented delivery of drugs. The continuing clinical studies of EOs implicate that their pharmacological applications are a rewarding research area.

Broad-Spectrum Antibacterial Peptide Kills Extracellular and Intracellular Bacteria Without Affecting Epithelialization.

New antibacterial drugs with novel modes of action are urgently needed as antibiotic resistance in bacteria is increasing and spreading throughout the world. In this study, we aimed to explore the possibility of using APIM-peptides targeting the bacterial ß-clamp for treatment of skin infections. We selected a lead peptide, named betatide, from five APIM-peptide candidates based on their antibacterial and antimutagenic activities in both G+ and G- bacteria. Betatide was further tested in minimal inhibitory concentration (MIC) assays in ESKAPE pathogens, in in vitro infection models, and in a resistance development assay. We found that betatide is a broad-range antibacterial which obliterated extracellular bacterial growth of methicillin-resistant Staphylococcus epidermidis (MRSE) in cell co-cultures without affecting the epithelialization of HaCaT keratinocytes. Betatide also reduced the number of intracellular Staphylococcus aureus in infected HaCaT cells. Furthermore, long-time exposure to betatide at sub-MICs induced minimal or no increase in resistance development compared to ciprofloxacin and gentamicin or ampicillin in S. aureus and Escherichia coli. These properties support the potential of betatide for the treatment of topical skin infections.

Antiproliferative, apoptotic, and antimutagenic properties of stem bark and seed fractions of Polyalthia cerasoides (Roxb.).

AIMS: The aim was to compare the anticancer and antimutagenic potency of Polyalthia cerasoides seeds and stem bark. AIM OF THE STUDY: The aim of this study was to investigate the antiproliferative, apoptotic, antioxidation to DNA, and antimutagenic activity of alcoholic (PS-1 and PS-3) and petroleum ether (PS-2 and PS-4) stem bark and seed fractions of P. cerasoides. METHODS: P. cerasoides stem bark and seeds were extracted with ethanol: water mixture (9:1 ratio v: v) and fractionated with petroleum ether. Fractions were investigated for antiproliferative effect using cell by 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide, a tetrazole assay (cell line used liver [HepG2] and cervical [HeLa] cancer cell lines), DNA damage protection using hydroxyl radical and antimutagenic effect using chromosome aberration test. RESULTS: PS-1 (IC50 10 µg/ml) and PS-3 (IC50 11 µg/ml) showed maximum antiproliferative activity against HepG2 cell lines, whereas, PS-1 (IC50 10 µg/ml), PS-2 (IC50 24 µg/ml), and PS-3 (IC50 11 µg/ml) showed better antiproliferative activity against HeLa cell lines. PS-3 and PS-4 were protective against oxidation to the supercoiled DNA molecule. Further, petroleum ether extract of both seed (PS-2) and stem bark (PS-4) showed good antimutagenicity as revealed by the less chromosomal aberrations compared to PS-1 and PS-3 fractions. CONCLUSIONS: This study demonstrated the beneficial effect of fractions against oxidation of DNA, antiproliferative, apoptotic, and antimutagenic activity. Probably, this property would be attributable by their phenolic and steroid constituents. Therefore, this plant could be used as a potential source of nutraceutical agents.