Enhancing bioactivity of Callistemon citrinus (Curtis) essential oil through novel nanoemulsion formulation.

The main focus of this study was to create a stable and efficient nanoemulsion (NE) using Callistemon citrinus essential oil (EO). Various factors affecting the NE's stability were optimized including oil %, Tween 80%, time of sonication, and its accelerated stability was examined. The research also considered the antibacterial, antifungal, and larvicidal effects of the optimized NE (B10). The optimum NE stood out for its stability, featuring a particle size of 33.15 ± 0.32 nm. Analysis via IR spectroscopy confirmed successful EO encapsulation in B10. The formulation remained stable for six months, with B10 showing significantly higher antibacterial and antifungal potency compared to the pure oil. When samples were subjected to tests against Fusarium oxysporum, B10 exhibited a MIC value of 62.5 mg/mL, whereas the pure oil showed a MIC value of 250 mg/mL. This indicates that the B10 formulation was 50 times more effective than the EO. In terms of antibacterial activity against Escherichia coli, the MIC value was 0.256 mg/mL for B10 and 4 mg/mL for the EO. Also, pure oil and B10 displayed larvicidal effects against Chilo suppressalis (Walker) larvae, with B10 eliminating 95.2% of larvae in 48 h. Overall, stable and optimum C. citrinus NE with its strong antimicrobial qualities, shows promise as an effective fungicide and insecticide.

Volatile oil constituents, antioxidant and antibacterial activities of Lonicera caprifolium L. in different areas of Iran.

The genus of Lonicera is the largest genus of Caprifoliaceae family. This study revealed the composition, antioxidant, and antibacterial actions of essential oils of Lonicera caprifolium L. in different areas of Iran; Qom, Mashhad, Shiraz. Gas chromatography-mass spectrometry examination was applied to recognise the oil conformation. The essential oils of Qom included a high number of monoterpenes, with linalool as the significant constituent. In the essential oil of Mashhad, the main elements were methyl linoleate. The essential oil of Shiraz displayed a similar profile, including a large quantity of fatty acid, with methyl palmitate as the main component. The antioxidant activity was assessed via the DPPH exam, and the antimicrobial action was verified using the broth microdilution procedure. The essential oils of Qom revealed the maximum antimicrobial and antioxidant actions between the three regions, ascribed to its high concentration of monoterpenes and phenolic composites. Moreover, principal component analysis (PCA) and heat map successfully revealed the variation and correlation between metabolites of the three oils. These conclusions highlight the potential of L. caprifolium as natural foundations of antimicrobial and antioxidant representatives, with investigation required to reveal their therapeutic requests.

Crataegus pentagyna willd. Fruits, leaves and roots: phytochemicals, antioxidant and antimicrobial potentials.

BACKGROUND: The hawthorn has recently been used as a popular herbal medicine in food applications and phytotherapy, especially for the cardiovascular system. METHODS: In this study, phytochemicals were evaluated by LC-ESI-MS, GC-MS, and biological activity, including antioxidant (DPPH test) and antibacterial (broth dilution assay), in different extracts of Crataegus pentagyna fruit, leaf, and root. RESULTS: Globally, 49 phenolics were tentatively identified using HPLC-ESI-MS/MS in the hydro-methanolic extract of the fruit (major apigenin, caffeoylquinic acid derivative, and 4-O-(3'-O-glucopyranosyl)-caffeoyl quinic acid), 42 in the leaf (major salicylic acid, naringenin-6-C-glucoside, and naringin), and 33 in the root (major naringenin-7-O-neohesperidoside, isovitexin-2″-O-rhamnoside, and 4-O-(3'-O-glucopyranosyl)-caffeoyl quinic acid). The major group compounds analyzed by GC-MS in petroleum ether extracts were hydrocarbons (63.80%) and fatty acids and their derivatives (11.77%) in fruit, hydrocarbons (49.20%) and fatty acids and their derivatives (13.85%) in leaf, and hydrocarbons (53.96%) and terpenes (13.06%) in root. All samples exhibited promising phytochemical profile (total phenol, flavonoid, phenolic acid, and anthocyanin), antioxidant and antibacterial capacities, especially in hydro-methanolic extract of fruit (210.22 ± 0.44 mg GAE/g DE; 79.93 ± 0.54 mg QE/g DE; 194.64 ± 0.32 mg CAE/g DE; 85.37 ± 0.13 mg cyanidin 3-glucoside/100 g FW; DPPH: 15.43 ± 0.65 µg/mL; MIC: 0.15-0.62 µg/mL; and MBC: 0.62-1.25 mg/mL), followed by the leaf and root extracts, respectively. The PCA and heatmap analysis results distinguished metabolite profile differences for samples. CONCLUSION: The results of the present work provide scientific support for C. pentagyna as antimicrobial agents and natural antioxidants in human health and food preservation.

New bioactive compounds characterized by liquid chromatography-mass spectrometry and gas chromatography-mass spectrometry in hydro-methanol and petroleum ether extracts of Prosopis farcta (Banks & Sol.) J. F. Macbr weed.

The purpose of this study was to identify and characterize the chemical composition present in aerial parts of Prosopis farcta in petroleum ether and hydro-methanol extracts through LC-PDA-ESI-MS/MS and GC-MS techniques respectively for the first time. The plant samples were collected from northeast of Iran during maturity stage. LC-MS/MS profile revealed 47 phenolic compounds in hydro-methanol extracts, including phenolic acids, flavonoids, and their glycoside derivatives. Flavonoid-O-glycosides (19), flavonoid aglycones (11), phenolic acid derivatives (9), flavonoid-C-glycosides (4), and flavonoid-O, C-glycosides (1) were dominant class phenolics in all studied parts. The extracts contained a significant amount of major compounds, including gallic and vanillic acids, luteolin, apigenin, phloridzin, and vicenin-2. Also, GC-MS analysis of petroleum ether extracts showed that fatty acids, organic acids, steroids, terpenoids, and hydrocarbons were the group of major compounds in all parts. Twenty-four, 27, and 25 components were identified, which represent 99.2%, 96.1%, and 99.4% of the total composition in fruits, leaves, and stems, respectively. These results suggested that other genetic resources of P. farcta can be further explored to screen genotypes with high bioactive compounds and purification of phytochemical compounds, which are valuable to produce, expand, and develop natural antioxidants in production of bio-medicine and food.

Investigation of physicochemical properties, antimicrobial and antioxidant activity of edible films based on chitosan/casein containing Origanum vulgare L. essential oil and its effect on quality maintenance of cherry tomato.

Edible coatings prevent physicochemical and biological food deterioration. Using bioactive compounds like essential oils can enrich films. In this study, edible films from chitosan (C), casein (Z) and oregano (OEO) were developed, and their physicochemical, barrier, antimicrobial, antioxidant, and structural properties (FTIR, SEM) were investigated. The C1Z3 ratio had good mechanical and inhibitory properties, and OEO improves flexibility, barrier, hydrophobic, antimicrobial, and antioxidant properties. The physicochemical and microbiological properties of cherry tomatoes were affected by C1Z3 and C1Z3O1.5 coatings. Coated fruits were stored at 4 °C for 32 days. The best results for weight loss, shrinkage, and titratable acidity were found to be 17.88%, 31.12%, and 0.15% in C1Z3O1.5 coated cherry tomatoes, respectively.The TMAB of C1Z3O1.5 coated fruits was less than detectable and the fungal growth was inhibited for 28 days. Accordingly, by adding OEO to chitosan/casein coatings, the spoilage process of cherry tomatoes was delayed for long-term storage.

Biological effects of red beetroot and betalains: A review.

Over the past few years, the use of natural substances as protective or therapeutic agents has gained much attention worldwide. Recent modern studies have shown a variety of health benefits for red beetroot and its active compounds betalains (also betanin) such as antioxidative, anti-inflammation, anticancer, blood pressure and lipid lowering, also antidiabetic and anti-obesity effects. Betanin, the main component of the red beetroot, is a betalain glycosidic pigment, which is used as a food additive. This review summarizes findings in the literature and shows the therapeutic potential of red beetroot and its active compounds (betalains) as promising alternatives for supplemental therapies in multiple diseases.

Artemisia: a promising plant for the treatment of cancer.

Due to the promising features of the ancient herbal plant Artemisia, its biologic activity has been investigated for use in modern medicine. In this regard, Artemisia and its active phytochemicals have been introduced as having antimalarial, antioxidant, cytotoxic, antispasmodic, anthelmintic, neuroprotective, anti-inflammatory, and antimicrobial agents. In the case of cancer treatment, the plant species and its bioactive compounds target multiple pathways. Here we reviewed the scientific literature published up until 2018, which have explained the cytotoxic activity of the Artemisia species and their constituents. This review summarizes the published data found in PubMed, Science Direct and Scopus. Here, studies about the cytotoxicity and antitumor action on cancer cells and tumor bearing animals are discussed. Also, detailed molecular pathways affected by the plant and the phytochemistry of the cytotoxic active components are presented. Among all species and chemical constituents, the active ones have been selected and discussed in detail. The cytotoxic comparison made here may open a window for future works and selection of agents for cancer chemotherapy.

Scutellaria: Debates on the anticancer property.

The widespread use of plants as accessible anticancer agents leads to the identification of many natural source chemotherapeutic agents. Scutellaria one of the popular genus of flowering plants has been used for various human illnesses for thousands of years. Scutellaria has anti-metastatic, anti-proliferative, anti-invasion, anti-angiogenic and apoptosis effects in vitro as well as in vivo. Despite numerous reports on the cytotoxic-antitumor activity of the plant, there are still some issues need further consideration. Issues such as unjustified interpretations, lack of attention to the pharmacokinetics profile and weak study design may affect the final decision about the use of plants as anticancer agents and possibly needs reconsideration. In this review, we have summarized the potential health benefits of Scutellaria and its active components also the underlying mechanism of cytotoxicity and antitumor activity. Meanwhile we have discussed concerns may interfere with the precise conclusion.

Central nervous system diseases and Scutellaria: a review of current mechanism studies.

Scutellaria comprises many species traditionally used for cognitive and neurological conditions. In vitro and in vivo studies have supported the value of bioactive compounds of the genus Scutellaria for CNS disorders such as Alzheimer, cerebral ischemia, depression and anxiety. In particular, the effects of plants belonging to the genus Scutellaria and their components are detailed on cognitive ability such as memory, attention and learning. In this review, the pharmacology of CNS effect and the related molecular mechanisms of the plants belonging to the genus Scutellaria and active constituents have been discussed.

Potent Cytotoxic Natural Flavonoids: The Limits of Perspective.

BACKGROUND: Besides the numerous biologic and pharmacologic functions in the human body that act as potent antioxidants, flavonoids (flavones, flavanones, flavonols, flavanols and isoflavones) are noted as cancer preventive or therapeutic agents. METHODS: This review summarizes the published data using PubMed, Science Direct, and Scopus. RESULTS: In this context, recognition and introduction of the most active cytotoxic flavonoids as promising agents for cancer therapy gives insight for further evaluations. However, there are some critical points that may affect the entering of flavonoids as active cytotoxic phytochemicals in the clinical phase. Issues such as the abundance of active species in nature, the methods of extraction and purification, solubility, pharmacokinetic profile, presence of the chiral moieties, method of synthesis, and structure modification may limit the entry of a selected compound for use in humans. Although plenty of basic evidence exists for cytotoxic/antitumor activity of the versatility of flavonoids for entry into clinical trials, the above-mentioned concerns must be considered. CONCLUSION: This review is an effort to introduce cytotoxic natural flavonoids (IC50< 10 µM) that may have the potential to be used against various tumor cells. Also, active constituents, molecular mechanisms, and related clinical trials have been discussed as well as the limitations and challenges of using flavonoids in clinic.

Anti-melanogenesis and anti-tyrosinase properties of Pistacia atlantica subsp. mutica extracts on B16F10 murine melanoma cells.

Pistacia atlantica (P. atlantica) subsp. mutica has been used in traditional medicine and is famous for its medicinal properties. The aim of this study was to evaluate the effect of methanol (MeOH), n-hexane, dichloromethane (CH2Cl2), n-butanol (BuOH), ethyl acetate (EtOAc), water extracts and essential oil of P. atlantica subsp. mutica on melanin synthesis and oxidative stress in B16F10 melanoma cell line. The B16F10 cells viability after treatment with increasing concentrations of different extracts of the plant (0.2-200 µg/mL) was measured using resazurin. Essential oil composition was identified by gas-chromatography-mass spectrometry (GC-MS) analysis and inhibitory effect on synthesis of melanin, mushroom tyrosinase activity, cellular tyrosinase, and oxidative stress were evaluated by the colorimetric and fluorometric methods. The data showed extracts at concentrations 0.2-200 µg/mL, did not show significant toxicity on melanoma cells but concentrations of 200 µg/mL of essential oil had cytotoxic effect. Pistacia atlantica subsp. mutica could inhibit the mushroom tyrosinase activity. Also the amount of melanin in B16F10 cells declined. In addition, the ability of P. atlantica subsp. mutica extracts in decreasing the amount of reactive oxygen species in melanoma cells revealed remarkable antioxidant activity. In addition, all concentrations of essential oil had no significant effect in this study. The melanogenesis inhibitory and antioxidant effects of P. atlantica subsp. mutica on B16F10 cells may suggest the potential whitening activity of the plant for using in dermatological skin care products and for prevention of skin aging in cosmetic industry.

Synthesis of dual-action parthenolide prodrugs as potent anticancer agents.

Cancer stem cells are responsible for the failure of a large number of cancer treatments and the re-emergence of cancer in patients. Parthenolide is a potent anticancer sesquiterpene lactone that is also able to kill cancer stem cells. The main problem with this compound is its poor solubility in water. To solve this problem, medicinal chemists have tried to prepare amino-derivatives of parthenolide, however, most amino-derivatives have less potency than that of parthenolide. In this paper, we proposed a new approach to synthesize parthenolide derivatives with better solubility and higher potency. We prepared novel parthenolide derivatives through the aza-Michael addition of nitrogen-containing anticancer drug molecules (cytarabine and melphalan) to the α-methylene-γ-lactone group of parthenolide. Different types of catalysts were used to catalyze the aza-Michael addition. Among all the used catalysts, 1,8-diazabicyclo [5.4.0] undec-7-ene (DBU) was found to have the highest catalytic activity. In addition, we examined the effects of parthenolide-anticancer drug hybrids on the growth and proliferation of three cancer cell lines (MCF-7, LNcaP, Hep G2) and CHO. The parthenolide prodrugs showed potent cytotoxic property with IC50 values ranging from 0.2 to 5.2µM, higher than those of parthenolide and anticancer drugs (cytarabine and melphalan).

Labdane Diterpenoids from Salvia leriifolia: Absolute Configuration, Antimicrobial and Cytotoxic Activities.

Fractionation of an n-hexane extract of the aerial parts of Salvia leriifolia led to the isolation of two new (1, 2) and two known (3, 4) labdane diterpenoids, together with three other known compounds. The structures were established by a combination of 1D and 2D NMR, and HRESIMS. The structures of 1 and 3 were confirmed by single-crystal X-ray analysis. The absolute configuration of 1-4 was established by electronic circular dichroism spectroscopy. Compounds 1-4 were evaluated for their cytotoxic activities against MCF-7 human breast cancer cells. Labdanes 3 and 4 were additionally tested against MDA-MB231 human breast cancer and DU-145 human prostate cancer cell lines. Compound 4 showed IC50 values of 25, 50, and 50 µM against MCF-7, MDA-MB231, and DU-145 cells, respectively. Compounds 1-4 were tested for activity against gram-positive (Staphylococcus aureus) and gram-negative (Escherichia coli) bacteria. Compound 3 showed an MIC of 213 µM against methicillin-resistant S. aureus.