ABSTRACT
With an increase in life expectancy and decrease of quality-of-life couple with the high prevalence of diseases, diet is expected to play a key function in sustaining human health. Nutritionists, food technologists and medical experts are working in synergy to cater for the increasing demand of food with associated therapeutic benefits, commonly known as functional food, that may improve well-being and reduce the risk of diseases. Interestingly, the marine ecosystem, due to its abundant and phenomenal biodiversity of marine organisms, constitutes a vital source of a panoply of healthy foods supply for the thriving functional food industry. Marine organisms such as seaweeds, sea cucumbers, sponges, and mollusks amongst others are sources of thousands of biologically active metabolites with antioxidant, anti-parasitic, antiviral, anti-inflammatory and anticancer properties. Given the growing number of research and interest to probe into the therapeutic roles of marine products, this review was designed to provide a comprehensive summary of the therapeutic properties of marine organisms (macroalgae, sea cucumbers and fish among others) which are consumed worldwide, in addition to their potentials and as sources of functional ingredients for developing novel food and fostering wellness. The gap between research development and actual commercialization, and future prospects of marine-based products also summarized to some extent.
Subject(s)
Sea Cucumbers , Seaweed , Animals , Antioxidants/metabolism , Aquatic Organisms , Ecosystem , Functional Food , HumansABSTRACT
Boerhavia diffusa is a great tropical plant and is widely used for various traditional purposes. In the present study, we examined the influence of solvents (dichloromethane, ethyl acetate, methanol and infusion (water)) on chemical composition and biological capabilities of B. diffusa. An UHPLC-HRMS method was used to determine the chemical characterization. The biological ability was examined for antioxidant, enzyme inhibitory and anti-cancer effects. To evaluate antioxidant effects, different chemical methods (ABTS, DPPH, CUPRAC, FRAP, metal chelating and phosphomolybdenum) were applied. With regard to enzyme inhibitory properties, cholinesterases, amylase, glucosidase and tyrosinase were used. The MDA-MB-231 breast cancer cell line was chosen to determine anticancer activity. Based on the UHPLC-HRMS analysis, 37 specialized metabolites were dereplicated and identified in the studied extracts. Results revealed the presence of 15 hydroxybenzoic, hydroxycinnamic, acylquinic acids, and their glycosides, one rotenoid, seven flavonoids, 12 fatty acids and two other glycosides. Among the tested extracts, the methanol extract showed a stronger antioxidant ability compared with other extracts. The methanol extract also showed the best inhibitory effects on tyrosinase and glucosidase. In the anti-cancer evaluation, the methanol extract showed stronger anticancer effects compared with water extract. In summary, our observations can contribute to the establishment of B. diffusa as a potential candidate for functional applications in the preparation.
ABSTRACT
Resveratrol is a polyphenolic stilbene derivative widely present in grapes and red wine. Broadly known for its antioxidant effects, numerous studies have also indicated that it exerts anti-inflammatory and antiaging abilities and a great potential in cancer therapy. Regrettably, the oral administration of resveratrol has pharmacokinetic and physicochemical limitations such as hampering its effects so that effective administration methods are demanding to ensure its efficiency. Thus, the present review explores the published data on the application of resveratrol nanoformulations in cancer therapy, with the use of different types of nanodelivery systems. Mechanisms of action with a potential use in cancer therapy, negative effects, and the influence of resveratrol nanoformulations in different types of cancer are also highlighted. Finally, the toxicological features of nanoresveratrol are also discussed.
ABSTRACT
Spermacoce verticillata (L.) G. Mey. is commonly used in the folk medicine by various cultures to manage common diseases. Herein, the chemical and biological profiles of S.â verticillata were studied in order to provide a comprehensive characterization of bioactive compounds and also to highlight the therapeutic properties. The inâ vitro antioxidant activity using free-radical scavenging, phosphomolybdenum, ferrous-ion chelating and reducing power assays, and the inhibitory activity against key enzymes such as acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), tyrosinase, α-amylase and α-glucosidase of S.â verticillata extracts (dichloromethane, ethyl acetate, methanol and water) were investigated. The highest total phenolic and flavonoid content were observed in the methanolic and aqueous extracts. Exhaustive 2DNMR investigation has revealed the presence of rutin, ursolic and oleanoic acids. The methanolic extract, followed by aqueous extract have showed remarkable free radical quenching and reducing ability, while the dichloromethane extract was the best source of metal chelators. The tested extracts showed notable inhibitory activity against cholinesterases (AChE: 1.63-4.99â mg GALAE/g extract and BChE: 12.40-15.48â mg GALAE/g extract) and tyrosinase (60.85-159.64â mg KAE/g extract). No inhibitory activity was displayed by ethyl acetate and aqueous extracts against BChE and tyrosinase, respectively. All the tested extracts showed modest α-amylase inhibitory activity, while only the ethyl acetate and aqueous extracts were potent against α-glycosidase. This study further validates the use of S.â verticillata in the traditional medicine, while advocating for further investigation for phytomedicine development.
Subject(s)
Enzyme Inhibitors/pharmacology , Plant Extracts/pharmacology , Rubiaceae/chemistry , Acetylcholinesterase/metabolism , Agaricales/enzymology , Animals , Butyrylcholinesterase/metabolism , Electrophorus , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/metabolism , Horses , Magnetic Resonance Spectroscopy , Monophenol Monooxygenase/antagonists & inhibitors , Monophenol Monooxygenase/metabolism , Plant Extracts/chemistry , Plant Extracts/metabolism , Saccharomyces cerevisiae/enzymology , Swine , alpha-Amylases/antagonists & inhibitors , alpha-Amylases/metabolism , alpha-Glucosidases/metabolismABSTRACT
Epilepsy is a related chronic neurological condition of a predisposition for recurrent epileptic seizures, with various manifestations and causes. Although there are antiepileptic drugs, complementary natural therapies are widely used. The purpose of this systematic review was to analyze the antiepileptic/anticonvulsant pharmacological properties of plant-food derived bioactive molecules. In this regard, a systematic review of the PubMed database was made based on the inclusion criteria. Natural compounds/herbs with scientifically proven antiepileptic properties were selected. Experimental pharmacological studies in vitro and in vivo have shown that flavonoids, alkaloids and terpenoids may have anticonvulsant mechanisms similar to the new generation antiepileptic drugs. The relationships of structure-anticonvulsant effect, pharmacological models, seizure-inducing factors and response, effective dose were also analyzed and discussed. The results of in vitro and in vivo pharmacological studies analyzed in this systematic review support the clinical importance of plant-food-derived bioactive molecules for the complementary treatment of epilepsy. Thus, are opened new perspectives to develop new natural anticonvulsant drugs.
Subject(s)
Anticonvulsants/therapeutic use , Epilepsy/drug therapy , Phytochemicals/therapeutic use , Plant Extracts/therapeutic use , Plants, Medicinal/chemistry , Seizures/drug therapy , Alkaloids/pharmacology , Alkaloids/therapeutic use , Animals , Anticonvulsants/pharmacology , Flavonoids/pharmacology , Flavonoids/therapeutic use , Humans , Phytochemicals/pharmacology , Plant Extracts/pharmacology , Terpenes/pharmacology , Terpenes/therapeutic useABSTRACT
Alzheimer's disease (AD) and Parkinson's disease (PD) are notorious neurodegenerative diseases amongst the general population. Being age-associated diseases, the prevalence of AD and PD is forecasted to rapidly escalate with the progressive aging population of the world. These diseases are complex and multifactorial. Among different events, amyloid ß peptide (Aß) induced toxicity is a well-established pathway of neuronal cell death, which plays a vital function in AD. Glutamate, the major excitatory transmitter, acts as a neurotoxin when present in excess at the synapses; this latter mechanism is termed excitotoxicity. It is hypothesised that glutamate-induced excitotoxicity contributes to the pathogenesis of AD and PD. No cure for AD and PD is currently available and the currently approved drugs available to treat these diseases have limited effectiveness and pose adverse effects. Indeed, plants have been a major source for the discovery of novel pharmacologically active compounds for distinct pathological conditions. Diverse plant species employed for brain-related disorders in traditional medicine are being explored to determine the scientific rationale behind their uses. Herein, we present a comprehensive review of plants and their constituents that have shown promise in reversing the (i) amyloid-ß -related toxicity in AD models and (ii) glutamate-induced excitotoxicity in AD and PD models. This review summarizes information regarding the phytochemistry, biological and cellular activities, and clinical trials of several plant species in view to provide adequate scientific baseline information that could be used in the drug development process, thereby providing effective leads for AD and PD.
Subject(s)
Alzheimer Disease , Parkinson Disease , Plants, Medicinal , Aged , Alzheimer Disease/drug therapy , Amyloid beta-Peptides/toxicity , Glutamic Acid/toxicity , HumansABSTRACT
Croton hirtus L'Hér methanol extract was studied by NMR and two different LC-DAD-MSn using electrospray (ESI) and atmospheric pressure chemical ionization (APCI) sources to obtain a quali-quantitative fingerprint. Forty different phytochemicals were identified, and twenty of them were quantified, whereas the main constituents were dihydro α ionol-O-[arabinosil(1-6) glucoside] (133 mg/g), dihydro ß ionol-O-[arabinosil(1-6) glucoside] (80 mg/g), ß-sitosterol (49 mg/g), and isorhamnetin-3-O-rutinoside (26 mg/g). C. hirtus was extracted with different solvents-namely, water, methanol, dichloromethane, and ethyl acetate-and the extracts were assayed using different in vitro tests. The methanolic extracts presented the highest 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline)-6-sulfonic acid (ABTS), and ferric reducing antioxidant power (FRAP) values. All the tested extracts exhibited inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with a higher activity observed for dichloromethane (AChE: 5.03 and BChE: 16.41 mgGALAE/g), while the methanolic extract showed highest impact against tyrosinase (49.83 mgKAE/g). Taken together, these findings suggest C. hirtus as a novel source of bioactive phytochemicals with potential for commercial development.
Subject(s)
Antioxidants/chemistry , Cholinesterase Inhibitors/chemistry , Croton/chemistry , Glucosides/chemistry , Phytochemicals/chemistry , Phytosterols/chemistry , Terpenes/chemistry , Acetates/chemistry , Acetylcholinesterase/chemistry , Acetylcholinesterase/metabolism , Antioxidants/classification , Antioxidants/isolation & purification , Benzothiazoles/antagonists & inhibitors , Benzothiazoles/chemistry , Biphenyl Compounds/antagonists & inhibitors , Biphenyl Compounds/chemistry , Butyrylcholinesterase/chemistry , Butyrylcholinesterase/metabolism , Cholinesterase Inhibitors/isolation & purification , Croton/metabolism , Glucosides/classification , Glucosides/isolation & purification , Humans , Methanol/chemistry , Methylene Chloride/chemistry , Phytochemicals/classification , Phytochemicals/isolation & purification , Phytosterols/classification , Phytosterols/isolation & purification , Picrates/antagonists & inhibitors , Picrates/chemistry , Plant Extracts/chemistry , Solvents/chemistry , Structure-Activity Relationship , Sulfonic Acids/antagonists & inhibitors , Sulfonic Acids/chemistry , Terpenes/classification , Terpenes/isolation & purification , Water/chemistryABSTRACT
Toddalia asiatica (L.) Lam. is extensively used in traditional medicinal systems by various cultures. Despite its frequent use in traditional medicine, there is still a paucity of scientific information on T. asiatica growing on the tropical island of Mauritius. Therefore, the present study was designed to appraise the pharmacological and phytochemical profile of extracts (methanol, ethyl acetate and water) and essential oil obtained from aerial parts of T. asiatica. Biological investigation involved the evaluation of inâ vitro antioxidant and enzyme inhibitory potentials. The chemical profile of the EO was determined using gas chromatography coupled to mass spectrometry (GC/MS) analysis, while for the extracts, the total phenolic (TPC) and flavonoid content were quantified as well as their individual phenolic compounds by LC/MS/MS. Quinic acid, fumaric acid, chlorogenic acid, quercitrin and isoquercitrin were the main compounds in the extracts. Highest total phenolic (82.5±0.94â mg gallic acid equivalent (GAE/g)) and flavonoid (43.8±0.31â mg rutin equivalent (RE/g)) content were observed for the methanol extract. The GC/MS analysis has shown the presence of 26 compounds with linalool (30.9 %), linalyl acetate (20.9 %) and ß-phellandrene (7.9 %) being most abundant components in the EO. The extracts and EO showed notable antioxidant properties, with the methanol extract proved to be superior source of antioxidant compounds. Noteworthy anti-acetylcholinesterase (AChE) and anti-butyrylcholinesterase (BChE) effects were recorded for the tested samples, while only the methanol and ethyl acetate extracts were active against tyrosinase. With respect to antidiabetic effects, the extracts and EO were potent inhibitors of α-glucosidase, while modest activity was recorded against α-amylase. Docking results showed that linalyl acetate has the highest affinity to interact with the active site of BChE with docking score of -6.25â kcal/mol. The findings amassed herein act as a stimulus for further investigations of this plant as a potential source of bioactive compounds which can be exploited as phyto-therapeutics.
Subject(s)
Antioxidants/pharmacology , Enzyme Inhibitors/pharmacology , Oils, Volatile/pharmacology , Phytochemicals/pharmacology , Plant Extracts/pharmacology , Rutaceae/chemistry , Acetylcholinesterase/metabolism , Animals , Antioxidants/chemistry , Antioxidants/isolation & purification , Benzothiazoles/antagonists & inhibitors , Biphenyl Compounds/antagonists & inhibitors , Butyrylcholinesterase/metabolism , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/isolation & purification , Humans , Medicine, Traditional , Models, Molecular , Monophenol Monooxygenase/antagonists & inhibitors , Monophenol Monooxygenase/metabolism , Oils, Volatile/chemistry , Oils, Volatile/isolation & purification , Oxidative Stress/drug effects , Phytochemicals/chemistry , Phytochemicals/isolation & purification , Picrates/antagonists & inhibitors , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Plants, Medicinal/chemistry , Reactive Oxygen Species/metabolism , Sulfonic Acids/antagonists & inhibitors , alpha-Amylases/antagonists & inhibitors , alpha-Amylases/metabolism , alpha-Glucosidases/metabolismABSTRACT
Geophytes are gaining interest as sources of natural ingredients in nutraceutical and pharmaceutical area. In this sense, six bulbous plant species from Turkey are investigated, namely Hyacinthella campanulata K.Perss. & Wendelbo, Muscari neglectum Guss. ex Ten., Tulipa humilis herb., Iris stenophylla Hausskn. ex Baker, Galanthus elwesii Hook. f. and Crocus danfordiae Maw. with the aim to highlight their chemical compositions and biological properties. Polyphenolic profiles of the different plant parts (flower, bulb and leaf) of the six genotypes were evaluated using colorimetric methods as well LC-MS/MS. The antioxidant properties and enzymes inhibitory potential (α-amylase, α-glucosidase, tyrosinase and cholinesterases) of the extracts were determined. Overall, highest total phenolic content and total flavonoid content were observed in the leaf extracts of the studied species, except for M. neglectum (flower extract) and T. humilis (flower extract). LC-MS/MS analysis revealed the abundance of some phenolic compounds including quinic acid, hesperidin and chlorogenic acid in selective extracts. The extracts showed significant antioxidant potentials, with leaf extract of the I. stenophylla being more potent, which is linked to its high phenolic contents. All the extracts displayed notable anti-acetylcholinesterase (1.77 - 2.53 mg GALAE/g) and tyrosinase (54.9-67.20 mg KAE/g). Selective extracts have showed activity against butyrylcholinesterase, with bulb extract of M. neglectum (2.99 mg GALAE/g), I. stenophylla (2.53 mg GALAE/g) and G. elwesii (2.52 mg GALAE/g) showing highest activity. Modest activity was observed against α-amylase and α-glucosidase. The experimental data gathered herein is the first report on the phytochemical and biological attributes of these bulbous plant species which project them as potential sources of biologically active compounds for phytomedicines and nutraceuticals development.
Subject(s)
Plant Extracts , Tandem Mass Spectrometry , Chromatography, Liquid , Dietary Supplements , Plant Extracts/pharmacology , TurkeyABSTRACT
Khaya senegalensis A. Juss (Meliaceae) is a popular medicinal plant, widely used in the management of various ailments in the African traditional medicine. This study attempts to investigate into the different extraction methods (homogenizer-assisted extraction (HAE), maceration (MAC), infusion and Soxhlet (SE) extraction) on the pharmacological properties and chemical profiles of K. senegalensis. Antioxidant properties and inhibitory potential against key enzymes were assessed and bioinformatics analysis was conducted on selected limonoids to predict putative pharmacokinetics and protein targets underlying the pharmacological effects. Overall, the leaf extracts showed notable flavonoid (20.59-104.43 mg RE/g) content and the stem barks extracts displayed the highest total phenolic (87.69-46.28 mg GAE/g), phenolic acid (62.96-107.22 mg CE/g), flavanol (3.60-135.40 mg CAE/g) contents. All extracts showed remarkable antioxidant activities, with the MAC-Water leaf extract being most active in all the assays. Regarding stem bark, the MAC-MeOH extract exerted the highest free radical scavenging abilities, while HAE and MAC extracts were better sources of reducing agent and metal chelators. The HAE-MeOH, MAC-Water, and SE extracts showed noteworthy inhibitory activity against AChE, BChE (only stem barks), tyrosinase and α-glucosidase (only stem barks). All extracts displayed moderate inhibitory activities against α-amylase. The bioinformatics approach showed that khayanoside A and C interacted with multiple isoforms of metalloproteinase, while humilin B and khayanone interacted with opioid receptors. To sum up, the chemical profiles and biological activities of K. senegalensis were closely dependent on the extraction methods. Results amassed from this study showed that K. senegalensis is a potent source of bioactive compounds which could be explored as a functional food.
Subject(s)
Meliaceae , Plants, Medicinal , Antioxidants/pharmacology , Flavonoids , Plant Extracts/pharmacologyABSTRACT
BACKGROUND: Diabetes Mellitus (DM) is a severe endocrine metabolic disease coupled with various long-term complications. A plethora of targets have been identified, however, with possible adverse effects. Therefore, researchers are in the perpetual quest for safe and more effective therapeutics. Natural products, particularly derived from plants, have proven to exert anti-diabetic effects via diverse mechanisms. METHODS: An overview of DM pathogenesis and its associated micro- and macro-vascular complications is presented. Possible underlying mechanisms of herbal remedies in DM management are provided, highlighting some key therapeutic targets. The review also appraises the recent progress of herbal products in treating DM through regulating inflammation and gut microbiota. Finally, currently available pharmacological treatments are discussed. RESULTS: The results show that numerous plants have proven to be promising sources of insulin secreting agents, α-glucosidase and α-amylase inhibitors. Among the non- conventional targets, inhibition of key enzymes such as lipase, cholinesterases and angiotensin converting enzyme has been directly and/or indirectly linked to DM and DM complications. For instance, hypericin, pseudohypericin and I3,II8-biapigenin isolated from Hypericum perforatum L., and palmatine and columbamine isolated from Dichocarpum auriculatum (Franch.) W. T. Wang & P. K have been found to be powerful lipase and cholinesterase inhibitors, respectively. Moreover, a number of plant-derived compounds such as feruloylated oligosaccharides from maize bran, baicalein and berberine are reported to mediate anti-diabetic property via modulation of gut microbiota. CONCLUSION: The information amassed in this review is anticipated to provide useful scientific baseline information to support advanced research in natural antidiabetic drug development.
Subject(s)
Biological Products , Diabetes Mellitus , Biological Products/therapeutic use , Diabetes Mellitus/drug therapy , Humans , Hypoglycemic Agents/therapeutic use , Insulin , alpha-GlucosidasesABSTRACT
Members of Scorzonera genus are known for their potential application in both food and pharmaceutical industries. The present study reports the chemical component and bioactivity of the dichloromethane, ethyl acetate, hexane, methanol and infused extracts of Scorzonera hieraciifolia Hayek aerial parts and roots. The methanolic extracts of both aerial parts and roots were good sources of total phenolic and flavonoid content. For the aerial parts, the infused and methanolic extracts showed highest (p < 0.05) free radical scavenging (2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid (ABTS)), reducing (cupric reducing antioxidant capacity (CUPRAC))and ferric reducing antioxidant power (FRAP)) and metal chelating capacities. Whilst, for the root extracts, overall most remarkable free scavenging and reducing activity was observed for the methanolic extracts (p < 0.05) while the hexane extracts showed highest metal chelating activity. The inhibitory activity of the extracts was evaluated against key enzymes. Overall, the hexane extracts of both aerial parts (acetylcholinesterase (AChE): 2.27 ± 0.04 and butyrlcholinesterase (BChE): 5.75 ± 0.48 mg galantamine equivalent (GALAE)/g) and roots (AChE: 2.44 ± 0.35 and BChE: 53.17 ± 0.22 mg GALAE/g) were most potent against AChE and BChE, suggesting a role for the more lipophilic compounds in this regard. The highest inhibitory activity against tyrosinase was displayed by methanolic extracts of aerial parts (64.70 ± 0.26 mg kojic acid equivalent (KAE)/g) and roots (63.63 ± 0.20 mg KAE/g). Modest activity was observed against α-amylase and α-glucosidase, two major enzymes implicated in the pathology of diabetes. Liquid chromatography-mass spectrometry (LC-MS) and nuclear magnetic resonance (NMR) analysis showed the presence of 40 compounds such as caffeic, ursolic, betulinic and oleanolic acid and their derivatives in the studied extracts. Multivariate analysis showed that the biological activities were dependent on the plant parts used as well as on the type of solvent used. Overall, the results showed that S. hieraciifolia is a valuable source of phytochemicals for both the nutraceutical and pharmaceutical sectors.
Subject(s)
Plant Extracts , Scorzonera , Antioxidants/pharmacology , Flavonoids , Phytochemicals , Plant Extracts/pharmacologyABSTRACT
The present study outlines the phenolic composition and pharmacological properties of different extracts of Digitalis cariensis Boiss. ex Jaub. & Spach root and aerial parts. The metabolic profiles of the studied extracts were characterized by UHPLC-MS. The in vitro antioxidant and enzyme (acetylcholinesterase (AChE), butyrylcholinesterase (BChE), tyrosinase, α-amylase, and α-glucosidase) inhibitory potential of the extracts were determined. Bioinformatics and docking investigations were also conducted to support the enzyme inhibition test and predict putative targets for potential pharmacological applications. Overall, the methanolic extract followed by the water extract of the D. cariensis root were found to be superior source of antioxidant compounds except for metal chelating ability, in which the water extract of the root (26.34 ± 1.54 mg EDTAE/g) and aerial parts (16.47 ± 0.88 mg EDTAE/g) have showed the highest activity. The tested extracts were potent against AChE (9.11 ± 0.27-9.79 ± 0.28 mg GEs/g extract), α-amylase (0.12 ± 0.01- 0.50 ± 0.01 mmol ACEs/g extract) and α-glucosidase (0.28 ± 0.01-17.29 ± 0.24 mmol ACEs/ g extract). Notable activity against tyrosinase was displayed by the methanolic extracts (Root-MeOH: 123.71 ± 2.70 and aerial parts - MeOH: 137.96 ± 1.07 mg KAE/g extract), while none of the extracts were potent against BChE. According to docking investigations, the observed anti-tyrosinase effect could be related, at least partially, to the presence of luteolin, rosmarinic acid and kaempferol in the extracts. Results amassed herein is the first report on the biological attributes of D. cariensis, which validate the pharmacological uses of this plant.
Subject(s)
Antioxidants , Digitalis , Antioxidants/pharmacology , Monophenol Monooxygenase , Phenols/pharmacology , Plant Extracts/pharmacologyABSTRACT
Schistosomiasis, a parasitic disease caused by trematodes of the genus Schistosoma, is the second most prevalent parasitic disease in the world. It affects around 200 million people. Clinical treatment, prophylaxis, and prevention are performed in countries susceptible to schistosomiasis. In the pharmacological treatment for an acute form of schistosomiasis, the use of antiparasitics, mainly praziquantel, is more common. As an alternative way, prevention methods such as reducing the population of intermediate hosts (mollusks) with molluscicides are important in the control of this disease by interrupting the biological cycle of this etiological parasite. Despite the importance of pharmacological agents and molluscicides, they have side effects and environmental toxicity. In addition, they can lead to the development of resistance enhancing of parasites, and lead to the search for new and effective drugs, including resources of vegetal origin, which in turn, are abundant in the affected countries. Thus, the purpose of this review is to summarize recent studies on botanical products with potential for the control of schistosomiasis, including anti-Schistosoma and molluscicide activities. In addition, species and plant derivatives according to their origin or geographical importance indicating a possible utility of local resources for countries most affected by the disease are presented.
ABSTRACT
Globally, approximately 12% of the population is inflicted by various types of urolithiasis. Standard treatments are available both to avert and treat urolithiasis, but with significant adverse side effects. Pentacyclic triterpenes represent a group of naturally occurring compounds which holds immense potential as therapeutic for treating kidney stone. This review aims to provide an integrative description on how pentacyclic triterpenes can effectively treat calcium oxalate urolithiasis through various mechanisms such as antioxidant, anti-inflammatory, diuretic, and angiotensin-converting enzyme inhibition. Some of the pentacylic triterpenes which shows promising activities include lupeol, oleanolic acid, betulin, and taraxasterol. Moreover, future perspectives in the development of pentacyclic triterpenes in formulations/drugs for urinary stone prevention are highlighted. It is anticipated that compiled information would serve as a scientific baseline to advocate further investigations on the potential of pentacyclic triterpenes in urolithiasis remediation.
Subject(s)
Nephrolithiasis/drug therapy , Pentacyclic Triterpenes/therapeutic use , Animals , Humans , Phytotherapy , Plants, MedicinalABSTRACT
Achyranthes aspera Linn. (Amaranthaceae), commonly known as the Prickly Chaff flower, is used as herbal medicine in the Ivorian's culture, Africa. Nonetheless, there is currently a paucity of scientific information on A. aspera from the Ivory Coast. Herein, the antioxidant activity of A. aspera extracts (methanol, dichloromethane, ethyl acetate and infusion) as well as the enzymatic inhibitory potentials towards key enzymes in human diseases, namely Alzheimer's disease, (cholinesterases: AchE and BChE), type 2 diabetes (α-glucosidase and α-amylase) and hyperpigmentation (tyrosinase) were assessed. The total phenolic (TPC) and flavonoid (TFC) content was determined using colorimetric methods and the individual compounds were characterized using ultra-high performance liquid chromatography coupled with hybrid quadrupole-Orbitrap high resolution mass spectrometry (UHPLC-HRMS). Furthermore, a network pharmacology analysis was conducted to predict putative targets of identified phenolic compounds. The highest TPC was observed in the infused extract (28.86 ± 0.12 mg GAE/g), while the dichloromethane extract (38.48 ± 1.48 mg RE/g) showed the highest level of TFC. UHPLC-HRMS analysis has revealed an abundance of fatty acids, flavonoids, phenols and acylquinic acids. Among tested extracts, the infused extract displayed the highest free radical quenching, reducing and metal-chelating ability. The extracts (except infusion) were effective as enzyme inhibitors against AChE, while only methanolic and infused extracts showed noteworthy anti-BChE effects. The methanolic extract showed a remarkable antityrosinase effect (56.24 ± 5.05 mg KAE/g), as well. Modest to moderate inhibitory activity was observed against α-amylase (all extracts) and α-glucosidase (only dichloromethane extract). Finally, the network pharmacology analysis suggested the carbonic anhydrase II enzyme as a putative target for explaining, at least in part, the traditional use of A. aspera preparations as diuretic and blood clotting agent. Data amassed herein tend to validate the use of A. aspera in traditional medicine, as well as act as a stepping stone for further studies in the quest for novel phytopharmaceuticals. In this context, it is desirable that this study will contribute to the validation of the traditional uses of this plant in the African herbal medicine, and to the valorization of the whole chain production of A. aspera, as a local and sustainable botanical resource.
Subject(s)
Achyranthes/chemistry , Phytochemicals/chemistry , Phytochemicals/pharmacology , Plant Extracts/chemistry , Plant Extracts/pharmacology , Plants, Medicinal/chemistry , Computational Biology/methods , Computer Simulation , Drug Monitoring , Fatty Acids, Nonesterified/chemistry , Flavonoids/chemistry , Glycosides/chemistry , Humans , Metabolome , Metabolomics/methods , Phenols/chemistry , Structure-Activity RelationshipABSTRACT
Among the major neurodegenerative disorders (NDDs), Alzheimer's disease (AD) and Parkinson's disease (PD), are a huge socioeconomic burden. Over many centuries, people have sought a cure for NDDs from the natural herbals. Many medicinal plants and their secondary metabolites are reported with the ability to alleviate the symptoms of NDDs. The major mechanisms identified, through which phytochemicals exert their neuroprotective effects and potential maintenance of neurological health in ageing, include antioxidant, anti-inflammatory, antithrombotic, antiapoptotic, acetylcholinesterase and monoamine oxidase inhibition and neurotrophic activities. This article review the mechanisms of action of some of the major herbal products with potential in the treatment of NDDs according to their molecular targets, as well as their regional sources (Asia, America and Africa). A number of studies demonstrated the beneficial properties of plant extracts or their bioactive compounds against NDDs. Herbal products may potentially offer new treatment options for patients with NDDs, which is a cheaper and culturally suitable alternative to conventional therapies for millions of people in the world with age-related NDDs.
ABSTRACT
In this study, we attempted for the first time to determine the phytochemical compositions and biopharmaceutical properties of the methanolic and aqueous extracts of Morinda morindoides fruits and seeds. Antioxidant propensities of the extracts were determined via free radical-scavenging, phosphomolybdenum, metal chelating, and reducing power assays. Inhibitory activities against cholinesterases (acetylcholinesterase (AChE) and butyrylcholinesterase (BChE)), tyrosinase, α-amylase, and α-glucosidase were assessed. Moreover, the total phenolic and flavonoid contents were determined. High Performance Liquid Chromatography coupled to Electrospray Ionization Quadrupole Time-of-Flight Mass Spectrometry (HPLC-ESI-Q-TOF-MS) analysis was performed to establish the chemical profile of the investigated extracts. The tested extracts showed remarkable antioxidant abilities with aqueous fruit extract being most potent in all assays, except for ferrous ion chelating assay. Overall, the methanolic extracts were potent inhibitors of the tested enzymes. In conclusion, M. morindoides may be endorsed as promising sources of bioactive compounds and used for designing functional foods. PRACTICAL APPLICATIONS: In recent years, new compounds from plant sources have attracted great interest to design functional foods. Thus, we aimed to detect biological and chemical properties of Morinda morindoides fruits and seeds, a widely used as food with medicinal properties in Africa. Based on our findings, fruits extracts exhibited stronger activity when compared to seed extracts. Also, chemical identification was performed for each extracts. The presented findings could provide valuable information into the pool of scientific knowledge and may be basis for the design of novel functional applications from M. morindoides.
Subject(s)
Antioxidants , Morinda , Africa , Antioxidants/pharmacology , Chromatography, High Pressure Liquid , Enzyme Inhibitors/pharmacology , Fruit , Plant Extracts/pharmacology , Seeds , Spectrometry, Mass, Electrospray IonizationABSTRACT
BACKGROUND: In this investigation, the chemical and biological profiles of three Turkish Crataegus species (Crataegus orientalis, Crataegus szovitsii and Crataegus tanacetifolia) were studied in order to provide the first comprehensive characterization and their health-promoting potential. In this respect, polyphenolic profiles were evaluated using ultrahigh-performance liquid chromatography-quadrupole time-of-flight mass spectrometry. The in vitro antioxidant activities of the Crataegus samples were evaluated by using free-radical scavenging, phosphomolybdenum, ferrous-ion chelating, and reducing power assays. The inhibitory activities against α-glucosidase, amylase, cholinesterases (acetylcholinesterase (AChE) and butyrylcholinesterase (BChE)), and tyrosinase were also established. RESULTS: The untargeted metabolomic approach highlighted the effect of both extraction types and species on the phenolic profiles of different Crateagus tissues (i.e. leaves and twigs). The methanolic extracts showed the maximum radical scavenging and reducing activity in all test systems, whereas for ferrous-ion chelating assays the decocted and infused extracts showed the highest activity. Only the methanolic extracts were effective against AChE and BChE. The extract tested showed remarkable inhibitory effects against tyrosinase and α-glucosidase, whereas all the extracts exhibited modest inhibition against α-amylase. Overall, the twig extracts of the three species studied showed superior antioxidant and enzyme inhibitory activities. CONCLUSION: On the basis of these results, the three Crataegus species can be classified as potent bioresources for high-value phytochemicals, which warrant further investigations for developing novel nutraceuticals. © 2019 Society of Chemical Industry.