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Sesquiterpenoids constitute the largest subgroup of terpenoids that have numerous applications in pharmaceutical, flavor, and fragrance industries as well as biofuels. Bergamotenes, a type of bicyclic sesquiterpenes, are found in plants, insects, and fungi with α-trans-bergamotene as the most abundant compound. Bergamotenes and their related structures (Bergamotane sesquiterpenoids) have been shown to possess diverse biological activities such as antioxidant, anti-inflammatory, immunosuppressive, cytotoxic, antimicrobial, antidiabetic, and insecticidal effects. However, studies on their biotechnological potential are still limited. This review compiles the characteristics of bergamotenes and their related structures in terms of occurrence, biosynthesis pathways, and biological activities. It further discusses their functionalities and potential applications in pharmaceutical, nutraceuticals, cosmeceuticals, and pest management sectors. This review also opens novel perspectives in identifying and harnessing bergamotenes for pharmaceutical and agricultural purposes.
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Plant extracts and their individual components have been used to manage skin aging for several decades. Recently, the discovery of new natural bioactive agents, that not only enhance the skin health but also offer protection against various deleterious factors, such as free radicals, ultraviolet radiation, and microbial infections, has been a potential target by many researchers. The aim of the current work was to investigate the phytochemical profile of an ethanol bark extract from Pseudobombax ellipticum, and to evaluate its antioxidant, antiaging and antibacterial activities in vitro. Molecular docking and molecular dynamics studies were adopted to estimate and confirm the binding affinity of several compounds and explain their binding pattern at the binding sites of four target enzymes associated with skin aging, namely collagenase, elastase, tyrosinase, and hyaluronidase. HPLC-MS/MS analysis led to the tentative identification of 35 compounds comprising phenolic acids, and their glycosides, procyanidins and flavonoid glycosides. The extract demonstrated a promising in vitro antioxidant activity in the DPPH and FRAP assays (IC50 56.45 and 15.34 µg/mL, respectively), and was able to inhibit the aforementioned key enzymes with comparable results to the reference drugs. In addition, the extract (6.25 mg/mL) inhibited the biofilm production of Pseudomonas aeruginosa and diminished the swimming and swarming motilities. The docked compounds revealed appreciable binding energy with the tested enzymes and were stable throughout the molecular dynamic simulations. In view of this data, P. ellipticum bark can be regarded as a good candidate for prospective application in derma-cosmeceutical preparations.
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CONTEXT: Withania (Solanaceae) species are known to be a rich source of withanolides, which have shown several biological properties. OBJECTIVE: To identify the compounds responsible for Withania adpressa Coss. antioxidant activity and further test them for their NF-κB inhibition and antiproliferative activity in multiple myeloma cells. MATERIALS AND METHODS: Compounds were obtained from the EtOAc extract of W. adpressa leaves. Structure elucidation was carried out mainly by 1D- and 2D-NMR, and mass spectrometry. Isolated compounds were tested in a dose-response for their in vitro NF-κB inhibition and antiproliferative activity in multiple myeloma cells after 5 and 72 h treatment, respectively. RESULTS: The fractionation resulted in the isolation of a new glycowithanolide named wadpressine (5) together with withanolide F, withaferin A, coagulin L, and nicotiflorin. The latter showed a moderate ability to scavenge free radicals in DPPH (IC50 = 35.3 µM) and NO (IC50 = 41.3 µM) assays. Withanolide F and withaferin A exhibited low µM antiproliferative activity against both multiple myeloma cancer stem cells and RPMI 8226 cells. Furthermore, they inhibited NF-κB activity with IC50 values of 1.2 and 0.047 µM, respectively. The other compounds showed a moderate inhibition of cell proliferation in RPMI 8226 cells, but were inactive against cancer stem cells and did not inhibit NF-κB activity. DISCUSSION AND CONCLUSIONS: One new glycowithanolide and four known compounds were isolated. Biological evaluation data gave further insight on the antitumor potential of withanolides for refractory cancers.
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Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología , Withania/química , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Antioxidantes/farmacología , Proliferación Celular/efectos de los fármacos , Flavonoides/química , Flavonoides/aislamiento & purificación , Flavonoides/farmacología , Células HEK293 , Humanos , Mieloma Múltiple/tratamiento farmacológico , FN-kappa B/antagonistas & inhibidores , Fenoles/química , Fenoles/aislamiento & purificación , Fenoles/farmacología , Extractos Vegetales/química , Hojas de la Planta/química , Witanólidos/química , Witanólidos/aislamiento & purificación , Witanólidos/farmacologíaRESUMEN
The phytoconstituents of the aqueous extract from Syzygium jambos L. (Alston) leaves were defined using HPLC-PDA-MS/MS and the antioxidant, anti-aging, antibacterial, and anti-biofilm activities of the extract were in silico and in vitro investigated. The antioxidant activities were performed using in vitro DPPH and FRAP assays as well as H2-DCFDA assay in HaCaT cells in which oxidative stress was induced by UVA radiation. Anti-aging activity was tested in vitro, using aging-related enzymes. The antibacterial, anti-biofilm and inhibitory effects on bacterial mobilities (swarming and swimming) were assessed against Pseudomonas aeruginosa. Results showed that S. jambos aqueous extract contained 28 phytochemicals belonging to different metabolite classes, mainly phenolic acids, gallic acid derivatives, flavonoids, and ellagitannins. Mineral content analysis showed that S. jambos leaves contained moderate amounts of nitrogen, potassium, manganese, magnesium, and zinc, relatively low amounts of phosphorus and copper, and high concentration of calcium and iron. The extract displayed strong antioxidant activities in vitro and inhibited UVA-induced oxidative stress in HaCaT cells. Docking the major compounds identified in the extract into the four main protein targets involved in skin aging revealed an appreciable inhibitory potential of these compounds against tyrosinase, elastase, hyaluronidase, and collagenase enzymes. Moreover, molecular dynamic simulations were adopted to confirm the binding affinity of some selected compounds towards the target enzymes. The extract exhibited pronounced in vitro anti-aging effects, compared to kojic acid and quercetin (the reference compounds). It also inhibited the growth of P. aeruginosa, counteracted its ability to form biofilm, and impeded its swarming and swimming mobilities. Altogether, these findings strongly propose S. jambos leaves as a promising source of bioactive metabolites for the development of natural cosmeceutical and dermatological agents.
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Piper cubeba L.f. (Piperaceae), known as cubeb, is a popular traditional herbal medicine used for the treatment of many diseases, especially digestive and respiratory disorders. The plant is rich in essential oil, found mainly in fruits, and this makes it economically important. Many traditional utilizations have been also validated from the plant and its isolated compounds owing to their antioxidant, antibacterial, anti-inflammatory and anticancer effects. These biological activities are attributed to the phytochemicals (phenolic compounds, lignans and alkaloids) and the essential oil of the plant. The present work aims to provide an up-to-date review on the traditional uses, phytochemistry and pharmacology of the plant and discusses the future perspectives to promote its valorization for nutritional- and health-promoting effects.
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Medicinal plants have been used since ancient times for human healthcare as drugs, spices, and food additives. The progress in technology and medicine observed, the last decades, has improved the quality of life and healthcare but with worrisome drawbacks. Side effects caused by synthetic drugs for instance originate sometimes irreversible health disorders. Natural substances, in contrast, are biologically and environmentally friendly. Syzygium jambos L. (Alston) also known as rose apple conveys a long history as essential traditional medicine with a broad spectrum of application in various cultures. The plant discloses a diverse group of secondary metabolites and extracts that displayed major susceptibilities towards various health concerns especially stress-related and inflammatory diseases. Despite a rich literature about the plant, the chemistry and biology of S. jambos have not been comprehensively reviewed yet. Accordingly, we present herein a literature survey of rose apple which aims to draw the chemical identity of the plant and establish a consistent discussion on the respective biological application of plant extracts and their corresponding traditional uses. The present work could provide a scientific basis for future studies and necessary information for further investigations of new drug discovery.
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Eichhornia crassipes (Mart.) Solms, commonly known as water hyacinth, is one of the world's most invasive aquatic plants of the Pontederiaceae family occurring in tropical and subtropical regions of the world. Although, E. crassipes causes significant ecological and socioeconomic issues such as a high loss in water resources, it has multipurpose applications since it is famous for many industrial applications such as bioenergy, biofertilizer production, wastewater treatment (absorption of heavy metals), and animal feed. Furthermore, E. crassipes is rich in diverse bioactive secondary metabolites including sterols, alkaloids, phenolics, flavonoids, tannins, and saponins. These secondary metabolites are well known for a wide array of therapeutic properties. The findings of this review suggest that extracts and some isolated compounds from E. crassipes possess some pharmacological activities including anticancer, antioxidant, anti-inflammatory, antimicrobial, skin whitening, neuroprotective, and hepatoprotective activities, among other biological activities such as allelopathic, larvicidal, and insecticidal activities. The present review comprehensively summarizes the chemical composition of E. crassipes, reported to date, along with its traditional uses and pharmacological and biological activities.
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ETHNOPHARMACOLOGICAL RELEVANCE: The genus Warburgia (family Canellaceae) is widely distributed over Afrotropical and Neotropical realms. Traditionally, W. salutaris (G. Bertol.) Chiov., and other Warburgia species are used as anti-inflammatory, antimalarial, antimicrobial, and for wound healing, and treating several skin complaints as well. Specifically, different extracts from W. salutaris were reported to possess diuretic, anti-inflammatory, and cytotoxic effects. AIM OF THE STUDY: This work aimed to investigate the phytochemical composition of an aqueous extract from W. salutaris bark, and evaluate its antioxidant and anti-aging activities in silico, in vitro, and in vivo. MATERIALS AND METHODS: HPLC-PDA-MS/MS was used to investigate the phytochemical components of the extract. The antioxidant potential of the extract was evaluated in vitro using DPPH and FRAP assays. The Caenorhabditis elegans nematodes model was adopted to investigate the antioxidant and the anti-aging effects in vivo by determining the worms' survival rate, level of ROS, HSP16 expression, and nuclear translocation of the transcription factor DAF16. Molecular operating environment (MOE) software was utilized for in silico molecular docking of the extract's components into different enzymes involved in the aging process. Anti-collagenase, anti-elastase, anti-tyrosinase, and anti-hyaluronidase assays were used to evaluate the anti-aging effects in vitro. RESULTS: HPLC-MS analysis furnished 30 compounds, among them catechin, 11α-hydroxy muzigadiolide, mukaadial, pereniporin B, and 11α-hydroxycinnamosmolide. The major components of the extract showed appropriate fitting in the binding site of the target enzymes adopted in the study with considerable minimum free binding energy relative to the standard inhibitors. The extract showed substantial in vitro antioxidant activity in DPPH and FRAP assays and in vitro anti-aging assays against collagenase, elastase, tyrosinase, and hyaluronidase with comparable IC50 values to the reference standards. Moreover, it attenuated oxidative stress in vivo as it significantly increased the survival rate of ROS stressed C. elegans worms, decreased intracellular ROS, decreased the juglone-induced HSP16 expression and enhanced the nuclear localization of DAF16 in a dose-dependent manner. CONCLUSION: Our results support the traditional use of W. salutaris to counteract inflammation and oxidative stress associated with several pathological conditions. In addition, W. salutaris bark extract can be considered as a substantial source for bioactive metabolites with strong potential as anti-aging and antioxidant agents.
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Antioxidantes , Magnoliopsida , Envejecimiento , Animales , Antioxidantes/uso terapéutico , Caenorhabditis elegans , Magnoliopsida/química , Simulación del Acoplamiento Molecular , Fitoquímicos/farmacología , Corteza de la Planta/química , Extractos Vegetales/uso terapéutico , Especies Reactivas de Oxígeno/metabolismo , Espectrometría de Masas en TándemRESUMEN
Salinity is a severe abiotic problem that has harmful impacts on agriculture. Recently, biostimulants were defined as bioprotectant materials that promote plant growth and improve productivity under various stress conditions. In this study, we investigated the effect of Crataegus oxyacantha extract as a biostimulant on tomato plants (Solanum lycopersicum) grown under salt stress. Concentrations of 20 mg/L, 30 mg/L, and 70 mg/L of C. oxyacantha extract were applied to tomato plants that were grown under salt stress. The results indicated that plants that were treated with C. oxyacantha extract had a higher ability to tolerate salt stress, as demonstrated by a significant (p < 0.05) increase in plant growth and photosynthetic pigment contents, in addition to a significant increase in tomato soluble sugars and amino acids compared to the control plants. In the stressed tomato plants, malondialdehyde increased and then decreased significantly with the different concentrations of C. oxyacantha extract. Furthermore, there was a significant improvement in the antioxidant enzyme activities of superoxide dismutase (SOD), glutathione peroxidase (GPx), glutathione S-transferase (GST), and glutathione reductase (GR) in the stressed plants, especially after treatment with 70 mg/L of the extract. Overall, our results suggest that C. oxyacantha extract could be a promising biostimulant for treating tomato plants under salinity stress.
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Caper (Capparis spinosa L.) is a perennial shrub of the family Capparaceae, endemic to circum-Mediterranean countries. Caper carries a renowned nutritional value, especially in terms of vitamins and antioxidants related to the occurrence of flavonoids, alkaloids, and glucosinolates as main secondary metabolites. Caper extracts have also shown to display antibacterial, antifungal, analgesic, antitumor, hepatoprotective, antioxidant, anti-inflammatory, and neuroprotective effects which correlate the uses of the plant in folk medicine against both metabolic and infectious diseases. The present review aims to provide exhaustive phytochemistry and pharmacological properties survey on Caper constituents. Attention has also been given to the nutritional values and traditional uses of main organs to pinpoint research gaps for future investigations on the plant.
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Water hyacinth (Eichhornia crassipes L.) was introduced as an invasive plant in freshwater bodies more particularly in Asia and Africa. This invasive plant grows rapidly and then occupies a huge layer of freshwater bodies. Hence, challenges are facing many countries for implementing suitable approaches for the valorization of the world's worst aquatic weed, and water hyacinth (WH). A critical and up-to-date review article has been conducted for more than 1 year, based on more than 100 scientific journal articles, case studies, and other scientific reports. Worldwide distribution of WH and the associated social, economic, and environmental impacts were described. In addition, an extensive evaluation of the most widely used and innovative valorization biotechnologies, leading to the production of biofertilizer and bioenergy from WH, and was dressed. Furthermore, an integrated search was used in order to examine the related advantages and drawbacks of each bioprocess, and future perspectives stated. Aerobic and anaerobic processes have their specific basic parameters, ensuring their standard performances. Composting was mostly used even at a large scale, for producing biofertilizers from WH. Nevertheless, this review explored some critical points to better optimize the conditions (presence of pollutants, inoculation, and duration) of composting. WH has a high potential for biofuel production, especially by implementing several pretreatment approaches. This review highlighted the combined pretreatment (physical-chemical-biological) as a promising approach to increase biofuel production. WH valorization must be in large quantities to tackle its fast proliferation and to ensure the generation of bio-based products with significant revenue. So, a road map for future researches and applications based on an advanced statistical study was conducted. Several recommendations were explored in terms of the choice of co-substrates, initial basic parameters, and pretreatment conditions and all crucial conditions for the production of biofuels from WH. These recommendations will be of a great interest to generate biofertilizers and bioenergy from WH, especially within the framework of a circular economy.