Antiurolithiatic effects of pentacyclic triterpenes: The distance traveled from therapeutic aspects

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. © 2020 Wiley Periodicals, Inc

Insights on the use of a-lipoic acid for therapeutic purposes

a-lipoic acid (ALA, thioctic acid) is an organosulfur component produced from plants, animals, and humans. It has various properties, among them great antioxidant potential and is widely used as a racemic drug for diabetic polyneuropathy-associated pain and paresthesia. Naturally, ALA is located in mitochondria, where it is used as a cofactor for pyruvate dehydrogenase (PDH) and a-ketoglutarate dehydrogenase complexes. Despite its various potentials, ALA therapeutic efficacy is relatively low due to its pharmacokinetic profile. Data suggests that ALA has a short half-life and bioavailability (about 30%) triggered by its hepatic degradation, reduced solubility as well as instability in the stomach. However, the use of various innovative formulations has greatly improved ALA bioavailability. The R enantiomer of ALA shows better pharmacokinetic parameters, including increased bioavailability as compared to its S enantiomer. Indeed, the use of amphiphilic matrices has capability to improve ALA bioavailability and intestinal absorption. Also, ALA’s liquid formulations are associated with greater plasma concentration and bioavailability as compared to its solidified dosage form. Thus, improved formulations can increase both ALA absorption and bioavailability, leading to a raise in therapeutic efficacy. Interestingly, ALA bioavailability will be dependent on age, while no difference has been found for gender. The present review aims to provide an updated on studies from preclinical to clinical trials assessing ALA’s usages in diabetic patients with neuropathy, obesity, central nervous system-related diseases and abnormalities in pregnancy.N. Martins would like to thank the Portuguese Foundation for Science and Technology (FCT-Portugal) for the Strategic project ref. UID/BIM/04293/2013 and “NORTE2020 - Northern Regional Operational Program” (NORTE-01-0145-FEDER-000012)

Resveratrol-Based Nanoformulations as an Emerging Therapeutic Strategy for Cancer

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.CR would like to acknowledge the UID/EQU/00511/2020 Project—Laboratory of Process Engineering, Environment, Biotechnology and Energy (LEPABE), financed by national funds through FCT/MCTES (PIDDAC). NC-M acknowledges the Portuguese Foundation for Science and Technology under the Horizon 2020 Program (PTDC/PSI-GER/28076/2017). Some of the components of the illustrations are taken from freepik and flaticon

Evaluation of antioxidant and enzyme inhibition properties of croton hirtus l’hér. Extracts obtained with different solvents

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 β ionol-O-[arabinosil(1-6) glucoside] (80 mg/g), β-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

Comprehensive bioactivity and chemical characterization of the endemic plant Scorzonera hieraciifolia Hayek extracts: A promising source of bioactive compounds

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\u2032-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 \ub1 0.04 and butyrlcholinesterase (BChE): 5.75 \ub1 0.48 mg galantamine equivalent (GALAE)/g) and roots (AChE: 2.44 \ub1 0.35 and BChE: 53.17 \ub1 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 \ub1 0.26 mg kojic acid equivalent (KAE)/g) and roots (63.63 \ub1 0.20 mg KAE/g). Modest activity was observed against \u3b1-amylase and \u3b1-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

Untargeted metabolomic profiling of three Crataegus species (hawthorn) and their in vitro biological activities

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\u2013quadrupole 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 \u3b1-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 \u3b1-glucosidase, whereas all the extracts exhibited modest inhibition against \u3b1-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. \ua9 2019 Society of Chemical Industry

Chemical and Biological Characterization of Erigeron Floribundus (Kunth) Sch.Bip Extracts Obtained by Four Isolation Procedures

In the present investigation, extracts of Erigeron floribundus leaves obtained by four isolation procedures, including homogenizer-assisted extraction, maceration, sonication and Soxhlet extraction, were compared for their qualitative and quantitative phytochemical composition as well as for their antioxidant and enzyme inhibitory activities. The total phenolic, phenolic acid and flavanol contents were highest in homogenizer-assisted extraction, while maceration contained slightly higher total flavanol content. High-performance liquid chromatography\u2013mass spectrometry (HPLC-DAD-MSn) analysis revealed that the hydroxycinnamic esters of quinic acids were the most abundant constituents in the isolates. The results showed that the extracts are promising sources of antioxidants with the homogenizer-assisted approach the most suitable. The extracts displayed notable enzyme inhibitory effects against acetylcholinesterases (7.98 \ub1 0.12 to 8.40 \ub1 0.09 mg galatamine equivalents (GALAE)/g extract) and tyrosinase (122.73 \ub1 0.43 to 111.36 \ub1 1.65 mg kojic acid equivalents (KAE)/g extract). In conclusion, the results demonstrate promising biological activities of E. floribundus isolates obtained via innovative extraction techniques, thereby offering preliminary information for the validation of the traditional medicinal uses of this plant

Biological Insights and NMR Metabolic Profiling of Different Extracts of Spermacoce verticillata (L.) G. Mey

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. verticillata were studied in order to provide a comprehensive characterization of bioactive compounds and also to highlight the therapeutic properties. The in 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. 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: 1.63–4.99 mg GALAE/g extract and BChE: 12.40–15.48 mg GALAE/g extract) and tyrosinase (60.85–159.64 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. verticillata in the traditional medicine, while advocating for further investigation for phytomedicine development

A comprehensive evaluation of the chemical profiles and biological properties of six geophytes from Turkey: Sources of bioactive compounds for novel nutraceuticals

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