The impact of seasonal variation on the composition of the volatile oil of Polyalthia suberosa (Roxb.) Thwaites leaves and evaluation of its acetylcholinesterase inhibitory activity.

BACKGROUND: Polyalthia suberosa (Roxb.) Thwaites (Annonaceae) is a medicinal plant that has been reported for its various pharmacological potentials, such as its anti-inflammatory, analgesic, antioxidant, and neuropharmacological activities. This study aimed to analyze the leaf essential oils of P. suberosa (PSLO) collected in different seasons, to evaluate the acetylcholinesterase inhibitory activity, and to corroborate the obtained results via in-silico molecular docking studies. METHODS: The leaf essential oils of P. suberosa collected in different seasons were analyzed separately by GC/MS. The acetylcholinesterase inhibitory activity of the leaves oil was assessed via colorimetric assay. In-silico molecular docking studies were elucidated by virtual docking of the main compounds identified in P. suberosa leaf essential oil to the active sites in human acetylcholinesterase crystal structure. RESULTS: A total of 125 compounds were identified where D-limonene (0.07 - 24.7%), α-copaene (2.25 - 15.49%), E-ß-caryophyllene (5.17 - 14.42%), 24-noroleana-3,12-diene (12.92%), ß-pinene (0.14 - 8.59%), and α-humulene (2.49-6.9%) were the most abundant components. Results showed a noteworthy influence of the collection season on the chemical composition and yield of the volatile oils. The tested oil adequately inhibited acetylcholinesterase enzyme with an IC50 value of 91.94 µg/mL. Additionally, in-silico molecular docking unveiled that palmitic acid, phytol, p-cymene, and caryophyllene oxide demonstrated the highest fitting scores within the active sites of human acetylcholinesterase enzyme. CONCLUSIONS: From these findings, it is concluded that P. suberosa leaf oil should be evaluated as a food supplement for enhancing memory.

Chemical characterization of three different extracts obtained from Chelidonium majus L. (Greater celandine) with insights into their in vitro, in silico and network pharmacological properties.

Plant species C. majus, which is a very rich source of secondary metabolites, was used to obtain extracts, using a conventional extraction technique. For the extraction of bioactive molecules, three solvents were used: ethyl acetate, methanol and water, which differ from each other based on their polarity. The obtained extracts were examined in terms of chemical composition, antioxidant, enzyme inhibitory activity, and cytotoxic effects. The research results indicate that methanol was a better and more efficient extractant in the process of isolating bioactive compounds than ethyl acetate and water. The chemical composition of this solvent, i.e. its polarity, contributed the most to the extraction of alkaloids and flavonoids. The high content of total phenolic compounds in the methanol extract, as well as individual alkaloids, caused a very strong antioxidant activity, as well as a strong inhibitory power when it comes to inhibiting the excessive activity of cholinesterase and tyrosinase. Methanol and ethyl acetate extracts achieved very good cytotoxic activity against cancerous cells HGC-27 and HT-29 and did not exert a toxic effect on non-cancerous cell lines (HEK293). Extracts of plant species C. majus, especially methanol extract could be characterized as a very good starting plant material for the formulation of products intended for various branches of the food and pharmaceutical industry.

Variation of the essential oil components of Citrus aurantium leaves upon using different distillation techniques and evaluation of their antioxidant, antidiabetic, and neuroprotective effect against Alzheimer's disease.

Citrus fruit essential oil is considered one of the widely studied essential oils while its leaves attract less attention although being rich in nearly the same composition as the peel and flowers. The leaves of bitter orange or sour orange (Citrus aurantium L.) were extracted using three different techniques namely; hydrodistillation (HD), steam distillation (SD), and microwave-assisted distillation (MV) to compare their chemical composition. The three essential oil samples were analyzed through GC/FID and GC/MS analyses. The samples were tested in vitro using different antioxidant techniques (DPPH, ABTS, CUPRAC, FRAP, PBD, and MCA), neuroprotective enzyme inhibitory activities (acetylcholine and butyl choline enzymes), and antidiabetic activities (α-amylase and α-glucosidase). The results showed that thirty-five volatile ingredients were detected and quantified. Monoterpenes represented the most abundant class in the three essential oils followed by sesquiterpenes. C. aurantium essential oil carried potential antioxidant activity where SD exhibited the highest antioxidant activity, with values arranged in the following order: FRAP (200.43 mg TE/g), CUPRAC (138.69 mg TE/g), ABTS (129.49 mg TE/g), and DPPH (51.67 mg TE/g). SD essential oil also presented the most potent α-amylase (0.32) inhibition while the MV essential oil showed the highest α-glucosidase inhibition (2.73 mmol ACAE/g), followed by HD (2.53 mmol ACAE/g), and SD (2.46 mmol ACAE/g). The SD essential oil exhibited the highest BChE and AChE inhibitory activities (3.73 and 2.06 mg GALAE/g), respectively). Thus, bitter orange essential oil can act as a potential source of potent antioxidant, antidiabetic, and neuroprotective activities for future drug leads.

Chemical exploration of different extracts from Phytolacca americana leaves and their potential utilization for global health problems: in silico and network pharmacology validation.

Phytolacca americana L. is of great interest as a traditional additive in various folk remedies in several countries, including Turkey. We aimed to determine the chemical profile (assisted by high-Performance liquid chromatography-electrospray ionization-tandem mass apectrometry (HPLC-ESI-MS/MS) experiments of three extracts obtained by different polarity solvents viz. ethyl acetate (to extract semipolar compounds), methanol and water (to extract highly polar metabolites) from P. americana leaves. Their anti-diabetic effects were investigated in vitro by assessing their inhibition toα-amylase and α-glucosidase. Assessment of the neuroprotective potential of the three extracts was carried out against acetyl-(AChE) and butyryl-(BChE) cholinesterase enzymes. HPLC-ESI-MS/MS experiments showed a total of 17 chromatographic peaks primarily classified to six flavonoids, two saponins, and six fatty acids. Antioxidant assays revealed remarkable activity for the ethyl acetate and methanol extracts. The BChE inhibition was considerably more significant (4.08 mg galantamine equivalent (GALAE)/g) for the ethyl acetate extract, whereas the methanol extract had good inhibitory efficacy for AChE (2.05 mg GALAE/g). Through network pharmacology, the compounds' mechanism of action of targeted key gene in their associated diseases were identified. The hubb gene signal transducer and activator of transcription 3 (STAT3) and tumour necrosis factor (TNFα) where the P. americana compound's site of action in inflammation bowel disease. The results offer possibilities for the prospective application of P. americana in metabolic regulation, blood glucose control, and as a source of bioactive compounds with cholinesterase enzyme inhibitory characteristics which could be of relevance in the cosmetic or pharmaceutical industry for combating melanogenesis.Communicated by Ramaswamy H. Sarma.

In vivo hepatoprotective and nephroprotective effects of Stenocarpus sinuatus leaf extract against ifosfamide-induced toxicity in rats.

Ifosfamide (IFOS) is a broad-spectrum chemotherapeutic agent that has been extensively used for breast cancer and other solid tumors. Unfortunately, its use is associated with toxicities of several organs. Stenocarpus sinuatus is an Australian tree belonging to the Proteaceae family. In the current study, the phytochemical constituents of S. sinuatus methanol leaf extract (SSLE) were assessed. In addition, the protective effect of SSLE against IFOS-induced nephrotoxicity and hepatotoxicity was evaluated. Rats were randomly divided into six groups: control, IFOS (50 mg/kg), IFOS + SSLE (100 mg/kg), IFOS + SSLE (200 mg/kg), IFOS + SSLE (400 mg/kg), and SSLE (400 mg/kg). Hepatoprotective and nephroprotective potency of SSLE was assessed using different biochemical parameters. The phytochemical investigation resulted in the isolation of four flavonoid glycosides (kaempferol 3-O-ß- d-glucopyranosyl-(1→2)-α- l-rhamnopyranoside, kaempferol 3-O-α-rhamnopyranoside, isorhamnetin 3-O-ß- d-glucopyranosyl-(1→2)-α- l-rhamnopyranoside, and quercetin 3-O-ß- d-glucopyranosyl-(1→2)-α- l-rhamnopyranoside) and a coumarin (scopoletin). This is the first report on the isolated compounds from the genus Stenocarpus. SSLE showed enhancement of kidney and liver functions and reduction of oxidative stress and inflammation. The histopathology of the investigated organs confirmed the protective effect of SSLE. In conclusion, SSLE is considered as a promising candidate that can be used in defense against the toxic effects of IFOS after further clinical trials.

HPLC-ESI/MS-MS characterization of compounds in Dolomiaea costus extract and evaluation of cytotoxic and antiviral properties: molecular mechanisms underlying apoptosis-inducing effect on breast cancer.

BACKGROUND: Dolomiaea costus (syn: Saussurea costus; Family Asteraceae) occupies an important place in the traditional Chinese medicinal plants and is prescribed for a wide range of disorders. The current study aimed to tentatively identify the phytoconstituents of D. costus extract and to explore antiproliferative activity against human breast cancer cells and its possible apoptotic mechanism along with antiviral activity against human adenovirus 5 (Adv-5). METHODS: The phytoconstituents of 70% ethanol extract of D. costus were assessed using HPLC/ESI-MS/MS technique. The cell viability was investigated against breast cancer cell line (MCF-7) via 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Mechanistically, the apoptotic effects on the Bax, Bcl2 and Caspase 3 were determined via quantitative reverse transcriptase-polymerase chain reaction (RT-qPCR). Further, the antiviral activity was assessed against Adv-5 based on virucidal and adsorption mechanisms. RESULTS: The HPLC/MS analysis of the extract revealed tentative identification of twenty compounds of polyphenolic nature, mainly flavonoids, lignans, coumarins, and anthocyanidins. The plant extract showed a cytotoxic effect against MCF-7 and Vero cells with IC50 values of 15.50 and 44 µg/ml, respectively, indicating its aggressiveness against the proliferation of breast cancer cells as confirmed by apoptotic genes expression which revealed upregulation of Bax and Caspase 3 but further insight analysis is needed to explore exact mechanistic pathway. Antiviral activity against Adv-5 was observed at a non-toxic concentration of the tested extract. CONCLUSIONS: Such observations against human breast cancer and viral replication supported further studies for nanoformulations in drug delivery systems as targeting therapy and in vivo studies before biomedical applications.

A comprehensive review of the health benefits of flaxseed oil in relation to its chemical composition and comparison with other omega-3-rich oils.

Flaxseed (Linum usitatissimum L) is an ancient perennial plant species regarded as a multipurpose plant owing to its richness in omega-3 polyunsaturated fatty acids (PUFA) including α-linolenic acid (ALA). The extensive biochemical analysis of flaxseed resulted in the identification of its bioactive, i.e., lignans with potential application in the improvement of human health. Flaxseed oil, fibers, and lignans exert potential health benefits including reduction of cardiovascular disease, atherosclerosis, diabetes, cancer, arthritis, osteoporosis, and autoimmune and neurological disorders that have led to the diversification of flaxseed plant applications. This comprehensive review focuses on flaxseed oil as the major product of flaxseed with emphasis on the interrelationship between its chemical composition and biological effects. Effects reviewed include antioxidant, anti-inflammatory, antimicrobial, anticancer, antiulcer, anti-osteoporotic, cardioprotective, metabolic, and neuroprotective. This study provides an overview of flaxseed oil effects with the reported action mechanisms related to its phytochemical composition and in comparison, to other PUFA-rich oils. This study presents the most updated and comprehensive review summarizing flaxseed oil's health benefits for the treatment of various diseases.

Essential Oil of Cestrum diurnum L.: GC/MS Analysis, in Vitro and in Silico Anti-HCoV-229E Effects and Inhibitory Activity against LPS-Induced Inflammation.

Cestrum diurnum L. (Solanaceae) is a fragrant ornamental tree cultivated in different parts around the world. In this study, the essential oil (EO) of the aerial parts was extracted by hydrodistillation (HD), steam distillation (SD) and microwave-assisted hydro-distillation (MAHD). GC/MS analysis of the three EOs revealed that phytol represents the major component in SD-EO and MAHD-EO (40.84 and 40.04 %, respectively); while in HD-EO it only represented 15.36 %. The SD-EO showed a strong antiviral activity against HCoV-229E with IC50 of 10.93 µg/mL, whereas, MAHD-EO and HD-EO showed a moderate activity with IC50 values of 119.9 and 148.2 µg/mL, respectively. The molecular docking of EO major components: phytol, octadecyl acetate and tricosane showed a strong binding to coronavirus 3-CL (pro). Moreover, the three EOs (50 µg/mL) decreased the levels of NO, IL-6 and TNF-α and suppressed IL-6 and TNF-α gene expression in LPS-induced inflammation model in RAW264.7 macrophage cell lines.

GC/MS Analysis, Cytotoxicity, and Antiviral Activities of Annona glabra Hexane Extract Supported by In Silico Study.

Annona glabra Linn is employed in conventional medicine to treat a number of human disorders, including cancer and viruses. In the present investigation, the significant phytochemical components of Annona glabra hexane extract were identified using gas chromatography-mass spectrometry (GC-MS) analysis. Three major compounds were identified in the hexane extract: tritriacontane (30.23%), 13, 17-dimethyl-tritriacontane (22.44%), and limonene (18.97%). MTT assay was used to assess the cytotoxicity of the extract on six human cancer cell lines including liver (HepG-2), pancreas (PANC-1), lung (A-549), breast (MCF-7, HTB-22), prostate (PC-3), and colon (CACO-2, ATB-37). The extract exhibited significant cytotoxic activity against both CACO-2 and A-549 cancer cell lines (IC50 = 47 ± 0.74 µg/mL and 56.82 ± 0.92 µg/mL) in comparison with doxorubicin (IC50 = 31.91 ± 0.81 µg/mL and 23.39 ± 0.43 µg/mL) and of SI of 3.8 and 3.1, respectively. It also induced moderate-to-weak activities against the other cancerous cell lines: PC-3, PANC-1, MCF-7, and HepG-2 (IC50 = 81.86 ± 3.26, 57.34 ± 0.77, 80.31 ± 4.13, and 57.01 ± 0.85 µg/mL) in comparison to doxorubicin (IC50 = 32.9 ± 1.74, 19.07 ± 0.2, 15.48 ± 0.84 and 5.4 ± 0.22 µg/mL, respectively) and SI of 2.2, 3.1, 2.2, and 3.1, respectively. In vitro anti-HSV1 (Herpes simplex 1 virus) and HAV (Hepatitis A virus) activity was evaluated using MTT colorimetric assay with three different protocols to test protective, anti-replicative, and anti-infective antiviral activities, and three separate replications of each experiment were conducted. The plant extract showed promising protective and virucidal activity against HSV1 with no significant difference with acyclovir (79.55 ± 1.67 vs. 68.44 ± 7.62 and 70.91 ± 7.02 vs. 83.76 ± 5.67), while it showed mild protective antiviral activity against HAV (48.08 ±3.46) with no significant difference vs. acyclovir (36.89 ± 6.61). The selected main compounds were examined for their bioactivity through in silico molecular docking, which exhibited that limonene could possess the strongest antiviral properties. These findings support Annona glabra's conventional use, which is an effective source of antiviral and anticancer substances that could be used in pharmaceuticals.

Protective effect of acrocarpus fraxinifolius extract against hepatic fibrosis induced by Gamma irradiation and carbon tetrachloride in albino rats.

PURPOSE: Liver fibrosis is considered as one of the ultimate outcomes of chronic liver disorders, characterized by outrageous cell proliferation and abnormal deposition of extracellular matrix, resulting in sever pathological distortions in the architecture and performance of liver tissues. The present study aimed to investigate the protective properties of aqueous methanol extract of Acrocarpus fraxinifolius leaves (AFL) against liver fibrosis induced by dual toxicity of γ-irradiation and carbon tetrachloride (CCl4) in rats. METHODS: The animals were exposed to 2 Gy irradiation once/week concurrently with intraperitoneal administration of CCl4 (0.2 mL/100 g body weight) for seven weeks. Afterwards, liver toxicity and fibrosis were assessed biochemically at cellular and molecular as well as histopathological levels. RESULTS: The livers of intoxicated rats showed distinct structural and functional changes, compared with the normal rats. The administration of AFL (500 mg/kg, p.o) significantly ameliorated the histopathological manifestations of fibrotic liver evidenced by mitigated steatosis progression, necrosis, fibrotic septa, apoptotic bodies, and immunochistochemical studies of alpha-smooth muscle actin. Also, AFL increased the final body weight, total protein, albumin levels and albumin/globulin ratio. While, the absolute liver weight, liver enzymes, total cholesterol and triglycerides were reduced. A significant modulation was observed in hydroxyproline, transforming growth factor-ß and collagen-1expression. Furthermore, AFL exerted a direct effect on liver fibrosis by promoting extracellular matrix degradation via overexpression of the tissue inhibitor metalloproteinase-1, coupled with decease of metalloproteinase-9 activity. CONCLUSIONS: Our findings suggested that AFL effectively improved the architecture of fibrotic liver and modified the biochemical markers of liver fibrosis.

Chemical Constituents, Antioxidant, and Enzyme Inhibitory Activities Supported by In-Silico Study of n-Hexane Extract and Essential Oil of Guava Leaves.

Psidium guajava (Guava tree) is one of the most widely known species in the family Myrtaceae. The Guava tree has been reported for its potential antioxidant, anti-inflammatory, antimicrobial, and cytotoxic activities. In the current study, the chemical compositions of the n-hexane extract and the essential oil of P. guajava were investigated using the GC/MS analysis, along with an evaluation of their antioxidant potential, and an investigation into the enzyme inhibition of acetylcholinesterase (AChE), butyrylcholinesterase (BchE), tyrosinase, α-amylase, and α-glucosidase. Moreover, molecular docking of the major identified active sites of the target enzymes were investigated. The chemical characterization of the n-hexane extract and essential oil revealed that squalene (9.76%), α-tocopherol (8.53%), and γ-sitosterol (3.90%) are the major compounds in the n-hexane extract. In contrast, the major constituents of the essential oil are D-limonene (36.68%) and viridiflorol (9.68%). The n-hexane extract showed more antioxidant potential in the cupric reducing antioxidant capacity (CUPRAC), the ferric reducing power (FRAP), and the metal chelating ability (MCA) assays, equivalent to 70.80 ± 1.46 mg TE/g, 26.01 ± 0.97 mg TE/g, and 24.83 ± 0.35 mg EDTAE/g, respectively. In the phosphomolybdenum (PM) assay, the essential oil showed more antioxidant activity equivalent to 2.58 ± 0.14 mmol TE/g. The essential oil demonstrated a potent BChE and tyrosinase inhibitory ability at 6.85 ± 0.03 mg GALAE/g and 61.70 ± 3.21 mg KAE/g, respectively. The α-amylase, and α-glucosidase inhibitory activity of the n-hexane extract and the essential oil varied from 0.52 to 1.49 mmol ACAE/g. Additionally, the molecular docking study revealed that the major compounds achieved acceptable binding scores upon docking with the tested enzymes. Consequently, the P. guajava n-hexane extract and oil can be used as a promising candidate for the development of novel treatment strategies for oxidative stress, neurodegeneration, and diabetes mellitus diseases.

Sweroside Ameliorated Memory Deficits in Scopolamine-Induced Zebrafish (Danio rerio) Model: Involvement of Cholinergic System and Brain Oxidative Stress.

Sweroside is a secoiridoid glycoside and belongs to a large group of naturally occurring monoterpenes with glucose sugar attached to C-1 in the pyran ring. Sweroside can promote different biological activities such as antifungal, antibacterial, hepatoprotective, gastroprotective, sedative and antitumor, antioxidant, and neuroprotective activities. Zebrafish were given sweroside (12.79, 8.35, and 13.95 nM) by immersion once daily for 8 days, along with scopolamine (Sco, 100 µM) 30 min before the initiation of the behavioral testing to cause anxiety and memory loss. Employing the novel tank diving test (NTT), the Y-maze, and the novel object recognition test (NOR), anxiety-like reactions and memory-related behaviors were assessed. The following seven groups (n = 10 animals per group) were used: control, Sco (100 µM), sweroside treatment (2.79, 8.35, and 13.95 nM), galantamine (GAL, 2.71 µM as the positive control in Y-maze and NOR tests), and imipramine (IMP, 63.11 µM as the positive control in NTT test). Acetylcholinesterase activity (AChE) and the antioxidant condition of the brains were also evaluated. The structure of sweroside isolated from Schenkia spicata was identified. Treatment with sweroside significantly improved the Sco-induced decrease of the cholinergic system activity and brain oxidative stress. These results suggest that sweroside exerts a significant effect on anxiety and cognitive impairment, driven in part by the modulation of the cholinergic system activity and brain antioxidant action.

GC/MS analysis and potential synergistic effect of mandarin and marjoram oils on Helicobacter pylori.

Helicobacter pylori can cause chronic gastritis, peptic ulcer, and gastric carcinoma. This study compares chemical composition and anti-H. pylori activity of mandarin leaves and marjoram herb essential oils, and their combined oil. GC/MS analysis of mandarin oil revealed six compounds (100% identified), mainly methyl-N-methyl anthranilate (89.93%), and 13 compounds (93.52% identified) of marjoram oil, mainly trans-sabinene hydrate (36.11%), terpinen-4-ol (17.97%), linalyl acetate (9.18%), and caryophyllene oxide (8.25%)). Marjoram oil (MIC = 11.40 µg/mL) demonstrated higher activity than mandarin oil (MIC = 31.25 µg/mL). The combined oil showed a synergistic effect at MIC of 1.95 µg/mL (same as clarithromycin). In-silico molecular docking on H. pylori urease, CagA, pharmacokinetic and toxicity studies were performed on major compounds from both oils. The best scores were for caryophyllene oxide then linalyl acetate and methyl-N-methyl anthranilate. Compounds revealed high safety and desirable properties. The combined oil can be an excellent candidate to manage H. pylori.

Phytonutrients, Colorant Pigments, Phytochemicals, and Antioxidant Potential of Orphan Leafy Amaranthus Species.

The underutilized Amaranthus leafy vegetables are a unique basis of pigments such as ß-cyanins, ß-xanthins, and betalains with radical scavenging capacity (RSC). They have abundant phytonutrients and antioxidant components, such as pigments, vitamins, phenolics, and flavonoids. Eight selected genotypes (four genotypes from each species) of underutilized Amaranthus leafy vegetables were evaluated for phytonutrients, pigments, vitamins, phenolics, flavonoids, and antioxidants in a randomized complete block design under ambient field conditions with three replicates. The studied traits showed a wide range of variations across eight genotypes of two species of Amaranthus leafy vegetables. The highest fat, ß-xanthins, K, dietary fiber, Mg, ß-cyanins, Mn, chlorophyll ab, Zn, TP, TF, betalains, chlorophyll a content, and (RSC) (DPPH) and RSC (ABTS+) were obtained from A. tricolor accessions. Conversely, the highest protein, Cu, carbohydrates, Ca, and chlorophyll b content were obtained from A. lividus accessions. The highest dry matter, carotenoids, Fe, energy, and ash were obtained from A. tricolor and A. lividus. The accession AT2 confirmed the highest vit. C and RSC (DPPH) and RSC (ABTS+); AT5 had the highest TP content; and AT12 had the highest TF content. A. tricolor accessions had high phytochemicals across the two species, such as phytopigments, vitamins, phenolics, antioxidants, and flavonoids, with considerable nutrients and protein. Hence, A. tricolor accessions can be used as high-yielding cultivars comprising ample antioxidants. The correlation study revealed that vitamin C, pigments, flavonoids, ß-carotene, and phenolics demonstrated a strong RSC, and showed a substantial contribution to the antioxidant potential (AP) of A. tricolor. The investigation exposed that the accessions displayed a plentiful origin of nutritional values, phytochemicals, and AP with good quenching ability of reactive oxygen species (ROS) that provide enormous prospects for nourishing the mineral-, antioxidant-, and vitamin-threatened community.

New quinolizidine alkaloid and insecticidal activity of Sophora secundiflora and Sophora tomentosa against Culex pipiens (Diptera: Culicidae).

Phytochemical investigation of Sophora secundiflora alkaloid fraction led to isolation of one new quinolizidine alkaloid (1) 13-methoxyanagyrine together with six known ones (2-7). The insecticidal activity of 70% methanol extract of leaves of S. secundiflora, S. tomentosa and the isolated alkaloids were assessed against 3rd instar larvae of Culex pipiens (Diptera: Culicidae) using different concentrations and mortality rate was recorded. Sophora tomentosa extract showed highest mortality rate with median lethal concentration LC50 3.11 ppm after 24 h and 0.66 ppm after 48 h and anagyrine (6) exhibited remarkably insecticidal activity with LC50 value of 3.42 ppm after 24 h of exposure. Additionally, cytotoxic activity of alkaloid fraction of S. secundiflora, S. tomentosa and isolated alkaloids was also studied using crystal violet assay against MCF-7 and HEPG-2 cell lines. Anagyrine (6) exhibited IC50 values of 27.3 ± 0.7 and 30.2 ± 0.9 µg/mL against MCF-7 and HEPG-2 cancer cells, respectively.

The genus Schinus (Anacardiaceae): a review on phytochemicals and biological aspects.

The genus Schinus belongs to family 'Anacardiaceae' and includes about 29 species originating from South America, distributed to Peru, Chile, Argentina, Brazil and Paraguay and cultivated in Egypt. Traditionally, Schinus plants are used to alleviate several and diverse diseases including rheumatism, hypertension, ulcers, gastric distress, menstrual disorders, gonorrhea, bronchitis, gingivitis, conjunctivitis, dysentery, wounds, urinary tract, and eye infections. Several phytochemical studies on the Schinus plants revealed presence of diverse bioactive compounds such as flavonoids, bioflavonoids, phenolic acids, tannins, catechins, terpenoids and essential oils. Besides, some Schinus species and their isolated active compounds showed important biological activities such as antibacterial, antifungal, insecticidal, antiparasitic, analgesic, cytotoxic, antitumor, antioxidant, antihypertensive, anti-inflammatory, antimycobacterial, anti-Parkinson, anti-allergic, antiviral, wound healing, chemoprotective, anthelmintic and hepatoprotective. This review attempts to summarize the phytochemical profile and biological activities of Schinus species that could guide researchers to undertake further investigation.

Insights on the Inhibitory Power of Flavonoids on Tyrosinase Activity: A Survey from 2016 to 2021.

Tyrosinase is a multifunctional copper-containing oxidase enzyme that initiates melanin synthesis in humans. Excessive accumulation of melanin pigments or the overexpression of tyrosinase may result in skin-related disorders such as aging spots, wrinkles, melasma, freckles, lentigo, ephelides, nevus, browning and melanoma. Nature expresses itself through the plants as a source of phytochemicals with diverse biological properties. Among these bioactive compounds, flavonoids represent a huge natural class with different categories such as flavones, flavonols, isoflavones, flavan-3-ols, flavanones and chalcones that display antioxidant and tyrosinase inhibitor activities with a diversity of mechanistic approaches. In this review, we explore the role of novel or known flavonoids isolated from different plant species and their participation as tyrosinase inhibitors reported in the last five years from 2016 to 2021. We also discuss the mechanistic approaches through the different studies carried out on these compounds, including in vitro, in vivo and in silico computational research. Information was obtained from Google Scholar, PubMed, and Science Direct. We hope that the updated comprehensive data presented in this review will help researchers to develop new safe, efficacious, and effective drug or skin care products for the prevention of and/or protection against skin-aging disorders.

Orange fruit (Citrus sinensis) peel extract attenuates chemotherapy-induced toxicity in male rats.

Background: Cyclophosphamide (CYP) is a chemotherapy drug widely used in the treatment of several types of cancers and autoimmune disorders. Unfortunately, it causes severe side effects on many organs due to its oxidative stress effect. Objective: The present study aims to tentatively identify the phytochemical constituents of orange fruit (Citrus sinensis) peel extract (OFPE) and elucidate the chemopreventive effects of OFPE on CYP drug induced organ toxicity. Methods: The high performance liquid chromatography coupled with mass spectroscopy (HPLC-MS/MS) technique was used to identify the compounds. Thirty-five male rats were divided into five groups (GP; n = 7): GP1: normal control, GP2: OFPE 0.5 only, GP3: CYP-only, GP4: OFPE 0.25 + CYP, and GP5: OFPE 0.5 + CYP. Results: Twenty-nine compounds of polyphenolic nature, mainly flavonoids, anthocyanidins, phenolic acids and limonoids were characterized by HPLC-MS/MS analysis. Among these compounds, naringin, hesperidin, diosmin, rutin, neohesperidin and limonin were the predominant compounds in the examined extract. Serum cellular markers were found to be decreased significantly upon treatment with OFPE (especially high dose). Also, a significant prophylactic effect against liver, kidney, and heart injuries induced by CYP via decreasing inflammation (serum TNF-α, IL-1ß & IL-6) and lipid peroxidation (MDA) was also revealed. Also, an increase in antioxidant levels (serum TAO, and cellular GSH & CAT in tissue homogenates) confirmed the protective efficacy of OFPE against CYP toxicity. Conclusions: The present study reveals some chemopreventive properties and beneficial effects of OFPE on CYP-induced organ toxicity via its antioxidant status and immunoregulatory activities.

Potentiation of anti-Helicobacter pylori activity of clarithromycin by Pelargonium graveolens oil.

BACKGROUND AND STUDY AIM: Peptic ulcer is one of the most serious diseases in Egypt, affecting more than one-third of the population. Helicobacter pylori is the main organism responsible for peptic ulcer formation. These ulcers can lead to chronic active gastritis and lymphoma. As such, in this study, we evaluate the efficacy of Pelargonium graveolens oil for the treatment of H pylori, as well as its synergistic effects with the antibiotic clarithromycin (CLR). PATIENTS AND METHODS: We evaluated the chemical composition of P. graveolens volatile oil as well as its anti-Helicobacter activities. We assessed the volatile oil components using gas chromatography coupled with mass spectrometry. We determined anti-H. pylori potential using a micro-well dilution method. RESULTS: We identified 92 compounds from the oil. Citronellol, geraniol, citronellyl formate, and isolongifolan-7-α-ol were the predominant components (15.64%, 11.31%, 10.19%, and 7.84%, respectively). The oil exhibited a good activity against H. pylori at an minimal inhibitory concentration of 15.63 µg/ml. Once we combined the volatile oil with CLR, a significant synergistic effect appeared at an fractional inhibitory concentration index of 0.38 µg/ml. CONCLUSION: The in-vitro interaction between the P. graveolens oil and CLR improved the antimicrobial activity of the latter, suggesting that further studies are needed to determine formulations for potential antimicrobial applications in food and pharmaceuticals.

Baicalein 5,6-Dimethyl Ether Prevents Memory Deficits in the Scopolamine Zebrafish Model by Regulating Cholinergic and Antioxidant Systems.

Baicalein 5,6-dimethyl ether, a bioactive flavonoid isolated for the first time from Alnus rugosa, was explored for its capability to relieve memory deficits and decrease oxidative stress. We examined the neuropharmacological effects of baicalein 5,6-dimethyl ether on scopolamine (Sco)-induced zebrafish (Danio rerio) anxiety, amnesia, and brain oxidative stress and attempted to elucidate the underlying mechanisms. Anxiety-like behavior, exploratory behavior, and memory performance were measured using novel tank-diving test (NTT), Y-maze, and novel object recognition (NOR) tests. For 10 days, baicalein 5,6-dimethyl ether (1, 3, and 5 µg/L) was administered through immersion, whereas Sco (100 µM) was delivered 30 min before behavioral tests. Treatment with baicalein 5,6-dimethyl ether reduced anxiety and memory impairment, and increased exploratory behavior in specific tests, along with significant protection from neuronal oxidative stress in the brain tissue of Sco-treated zebrafish. Antioxidant and anti-acetylcholinesterase (AChE) activities of baicalein 5,6-dimethyl ether in the Sco-induced zebrafish were further confirmed using in vivo assays. In Sco-treated zebrafish, baicalein 5,6-dimethyl ether regulated cholinergic function by inhibiting AChE activity. Baicalein 5,6-dimethyl ether may be a promising candidate compound for treating anxiety and amnesia by restoring cholinergic activity and reducing brain oxidative stress, according to our findings.