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1.
Biomed Pharmacother ; 167: 115382, 2023 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-37778271

RESUMO

Clivia miniata (Lindl) is a member of the family Amaryllidaceae known for its chemically diverse alkaloids with a wide range of biological activities. Many reports revealed a direct role of oxidative stress in the early stage of Alzheimer's disease (AD). Meanwhile, ß-site amyloid precursor protein cleavage enzyme 1 (BACE-1) is a molecular target for the treatment of AD. We aimed to investigate C. miniata root, bulb, and aerial part chemical profiling, antioxidant, BACE-1, and AChE enzyme inhibitory activities. Results showed that the total root had the most potent radical scavenging activity as compared to the total bulb and aerial part, respectively. Ethanol root extract had the most potent BACE-1 inhibitory activity (IC50 = 0.02 ± 0.001 µg/mL) as compared to the bulb and aerial part (IC50 = 0.93 ± 0.13, 1.80 ± 0.24 µg/mL), respectively. Moreover, the total root extract mitigated AChE enzyme activity more than total bulb and aerial fractions with IC50 values of (0.06 ± 0.02, 0.58 ± 0.3, and 1.89 ± 0.42 µg/mL, respectively. Bioassay-guided acid-base fractionation confirmed superior BACE-1 inhibitory activity of the root fractions particularly, methylene chloride and ethyl acetate fractions with (IC50 values of 0.21 ± 0.60 and 0.01 ± 0.001 µg/mL), respectively. UPLC-MS analysis of ethyl acetate and methylene chloride fractions of C. miniata root led to the identification of eight phenolics and thirteen alkaloids, respectively. Molecular docking studies against BACE-1 protein revealed that lycorine di-hexoside, miniatine, and cliviaaline were the most promising hits. Further investigation of anti-AD potential of the aforementioned small molecules is required.


Assuntos
Alcaloides , Doença de Alzheimer , Amaryllidaceae , Antioxidantes/farmacologia , Simulação de Acoplamento Molecular , Cromatografia Líquida , Cloreto de Metileno , Espectrometria de Massas em Tandem , Alcaloides/farmacologia , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Doença de Alzheimer/tratamento farmacológico , Componentes Aéreos da Planta , Inibidores da Colinesterase/farmacologia , Inibidores da Colinesterase/química
2.
J Mol Recognit ; 36(7): e3015, 2023 07.
Artigo em Inglês | MEDLINE | ID: mdl-37021769

RESUMO

Recent interest has focused on the biosynthesis of metal nanoparticles (NPs), particularly from plants. The production of precipitate served as an early indicator of the presence in the present study's use of ZnO NPs green synthesis of these particles, which was further validated by; Fourier transform infrared spectroscopy, x-ray diffraction. Additionally, the Brunauer-Emmett-Teller was used to calculate the surface area, which came out to be 119.12 m2 /g. Since the true effects of new pollutants, including medicines, on the environment and human health are not well understood, their presence in aquatic systems poses a severe hazard. For this reason, the antibiotic Ibuprofen (IBP) was absorbable to ZnO-NPs in this search. As opposed to fitting to Langmuir isothermally, the adsorption process was discovered to be pseudo-second-order kinetically, and the reaction was determined to be a chemisorption process. The process was endothermic and spontaneous, according to thermodynamic studies. Maximizing IBP removal from aqueous solution required the use of a Box-Behnken surface statistical design with four components, four levels, and response surface modeling. Solution pH, IBP concentration, duration, and dose were the four parameters that were utilized. The regeneration process, which is employed for five cycles with excellent efficiency, is the best benefit of using ZnO-NPs. Examine the elimination of pollutants from actual samples as well. However, the adsorbent is quite effective at reducing biological activity. At high concentrations of ZnO-NPs demonstrated notable antioxidant activity and Red Blood Cell (RBC) hemocompatibility and no discernible hemolysis was seen. ZnO-NPs demonstrated a notable percent suppression of α-amylase up to 53.6% at 400 µg/mL, and so displayed potential as an antidiabetic. Cyclooxygenase was suppressed by ZnO-NPs in an anti-inflammatory test (COX-1 & COX-2) up to 56.32% and 52.04% at a concentration of 400 µg/mL, respectively. Significant anti-Alzheimer potential was demonstrated by ZnO-NPs at 400 µg/mL by inhibiting Acetyl cholinesterase and Butyl cholinesterase up to 68.98 ± 1.62% and 62.36%, respectively. We concluded that guava extract is helpful for ZnO-NP reduction and capping. The bioengineered NPs could prevent Alzheimer's, diabetes, and inflammation and were biocompatible.


Assuntos
Nanopartículas Metálicas , Nanopartículas , Óxido de Zinco , Humanos , Óxido de Zinco/química , Óxido de Zinco/farmacologia , Ibuprofeno , Adsorção , Nanopartículas/química , Nanopartículas Metálicas/química , Antibacterianos/farmacologia , Preparações Farmacêuticas , Espectroscopia de Infravermelho com Transformada de Fourier , Extratos Vegetais/química
3.
Life (Basel) ; 12(10)2022 Oct 11.
Artigo em Inglês | MEDLINE | ID: mdl-36295014

RESUMO

Teucrium polium L. is commonly used in folk medicine to treat hypertension and diabetes and to heal wounds. The present work aimed to evaluate the different biological activities of T. polium hydroalcoholic extract, its total phenol and flavonoid content, and its mineral elements. Results showed that T. polium extract showed significant antioxidant potential in 2-diphenyl-1-picrylhydrazyl (DPPH) assay with IC50 equal to 8.68 µg/mL but with moderate activity in galvinoxyl assay with IC50 of 21.82 µg/mL and mild activity in the ß-carotene assay. It also showed a pronounced anti-hyperglycemic activity using α-amylase inhibitory assay (IC50 = 111.68 µg/mL) and exceeds that of acarbose. T. polium showed excellent activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with IC50 values of 28.69 and 4.93 µg/mL, respectively, postulating its promising anti-Alzheimer potential. The plant extract exhibited a strong anti-inflammatory effect with Bovine Serum Albumin (BSA) denaturation inhibitory potential estimated by 97.53% at 2 mg/mL, which was further confirmed by the in vivo carrageen-induced edema model. The extract revealed its richness in flavonoids and phenols, evidenced by its polyphenols content (36.35 ± 0.294 µg GAE/mg) and flavonoids (24.30 ± 0.44 µg QE/mg). It is rich in minerals necessary for human health, such as calcium, potassium, iron, sodium, magnesium, manganese and zinc. Molecular docking performed for previously identified compounds on human α-amylase, 5-lipoxygenase (5-LOX) and acetylcholine esterase confirmed the results. Thus, it can be concluded that T. polium can be a good candidate for alleviating many health-debilitating problems and can be highly beneficial in the pharmaceutical industry and medical research.

4.
Molecules ; 27(17)2022 Aug 26.
Artigo em Inglês | MEDLINE | ID: mdl-36080247

RESUMO

Combretaceae, an immense family involving species (500) or genera (20), originates in tropical and subtropical regions. This family has evinced medicinal values such as anti-leishmanial, cytotoxic, antibacterial, antidiabetic, antiprotozoal, and antifungal properties. Conocarpus lancifolius (C. lancifolius) methanol extract (CLM) was prepared, then compound isolation performed by open column chromatography, and compound structure was determined by spectroscopic techniques (13C NMR, IR spectroscopy, 1H-NMR, mass spectrometry UV-visible, and 2D correlation techniques). Molecular docking studies of ligand were performed on transcriptional regulators 4EY7 and 2GV9 to observe possible interactions. Phytochemical screening revealed the presence of secondary metabolites including steroids, cardiac glycosides, saponins, anthraquinones, and flavonoids. The isolated compound was distinguished as lancifolamide (LFD). It showed cytotoxic activity against human breast cancer, murine lymphocytic leukemia, and normal cells, human embryonic kidney cells, and rat glioma cells with IC50 values of 0.72 µg/mL, 2.01 µg/mL, 1.55 µg/mL, and 2.40 µg/mL, respectively. Although no cytotoxic activity was noticed against human colon cancer and human lung cancer, LFD showed 24.04% inhibition against BChE and 60.30% inhibition against AChE and is therefore beneficial for Alzheimer's disease (AD). AChE and LFD interact mechanistically in a way that is optimum for neurodegenerative disorders, according to molecular docking studies. Methanol and dichloromethane extract of C. lancifolius and LFD shows antibacterial and antifungal activity against antibiotic resistance Bacillus subtilis, Streptococcus mutans, Brevibacillus laterosporus, Salmonella Typhi, Candida albicans, and Cryptococcus neoformans, respectively. LFD shows antiviral activity against HSV-1 with 26% inhibition IP. The outcomes of this study support the use of LFD for cognitive disorders and highlight its underlying mechanism, targeting AChE, DNA-POL, NF-KB, and TNF-α, etc., for the first time.


Assuntos
Inibidores da Colinesterase , Combretaceae , Herpes Simples , Herpesvirus Humano 1 , Acetilcolinesterase/metabolismo , Animais , Inibidores da Colinesterase/química , Combretaceae/química , Herpesvirus Humano 1/efeitos dos fármacos , Humanos , Metanol , Camundongos , Simulação de Acoplamento Molecular , Extratos Vegetais/química , Ratos
5.
Chem Biodivers ; 19(9): e202200272, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-35938449

RESUMO

This study aimed to investigate the chemical composition of essential oils isolated from Acca sellowiana (feijoa) leaves and stems and elaborate on their relevance as natural anti-aging, coupled with molecular-docking studies. The isolated oils were analysed using gas chromatography-mass spectrometry analysis and investigated for inhibitory effects against acetylcholinesterase, ß-secretase, collagenase, elastase and tyrosinase. Molecular-modelling study was performed using MOE-Dock program to evaluate binding interactions of major components with the above-mentioned targets. The leaf oil revealed the predominance of caryophyllene oxide (24.3 %), linalool (7.9 %), and spathulenol (6.6 %), while the stem oil was presented by caryophyllene oxide (38.1 %), α-zingiberene (10.1 %) and humulene oxide II (6.0 %). The stem oil expressed superior inhibitory activities against acetylcholinesterase (IC50 =0.15±0.01 µg/mL), ß-secretase (IC50 =3.99±0.23 µg/mL), collagenase (IC50 =408.10±20.80 µg/mL), elastase (IC50 =0.17±0.01 µg/mL) and tyrosinase (IC50 =8.45±0.40 µg/mL). The valuable binding interactions and docking scores were observed for caryophyllene oxide and α-zingiberene with acetylcholinesterase. Besides, α-zingibirene followed by linalool and τ-cadinol revealed tight fitting with collagenase and elastase. Additionally, linalool, spathulenol and τ-cadinol showed the best binding energy to tyrosinase. This study provides valuable scientific data on A. sellowiana as potential candidates for the development of natural antiaging formulations. The current study provided scientific evidence for the potential use of feijoa essential oils in antiaging formulations and as an adjuvant for the prophylaxis against Alzheimer disease.


Assuntos
Feijoa , Óleos Voláteis , Acetilcolinesterase , Monoterpenos Acíclicos , Secretases da Proteína Precursora do Amiloide , Feijoa/química , Simulação de Acoplamento Molecular , Sesquiterpenos Monocíclicos , Monofenol Mono-Oxigenase/análise , Óleos Voláteis/química , Óxidos , Elastase Pancreática/análise , Folhas de Planta/química , Sesquiterpenos Policíclicos , Sesquiterpenos , Terpenos
6.
Saudi J Biol Sci ; 29(4): 2836-2855, 2022 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-35531221

RESUMO

Gold nanoparticles with tiny sizes and biostability are particularly essential and are employed in a variety of biomedical applications. Using a reducing agent and a stabilising agent to make gold nanoparticles has been reported in a number of studies. Gold nanoparticles with a particle size of 25.31 nm were synthesized in this study utilising Hylocereus polyrhizus (Red Pitaya) extract, which functions as a reducing and stabilising agent. The extract of Red Pitaya is said to be a powerful antioxidant and anti-cancer agent. Because of its substantial blood biocompatibility and physiological stability, green production of gold nanoparticles with H. polyrhizus fruit extract is an alternative to chemical synthesis and useful for biological and medical applications. The formation and size distribution of gold nanoparticles were confirmed by HPLC, UV-Vis spectrophotometer, X-ray diffraction (XRD), Dynamic light scattering (DLS), Zeta potential, Transmission electron microscopy (TEM), Fourier transformed infrared spectroscopy (FTIR), Energy dispersive X-ray (EDX) and X-ray photoelectron spectroscopy (XPS). The well-analysed NPs were used in various biological assays, including anti-diabetic, anti-inflammatory, anti-Alzheimer, and antioxidant (DPPH), and cytotoxic investigations. The NPs also showed a dose-dependent cytotoxic activity against HCT-116, HepG2 and MCF-7 cell lines, with IC50 of 100 µg/mL for HCT-116 cells, 155 µg/mL for HepG2, and for MCF-7 cells the value was 165 µg/mL respectively. Finally, the outstanding biocompatibility of Au-NPs has led to the conclusion that they are a promising choice for various biological applications.

7.
Molecules ; 27(10)2022 May 18.
Artigo em Inglês | MEDLINE | ID: mdl-35630702

RESUMO

Neurodegenerative diseases, among which one of the more common is Alzheimer's disease, are the one of the biggest global public health challenges facing our generation because of the increasing elderly population in most countries. With the growing burden of these diseases, it is essential to discover and develop new treatment options capable of preventing and treating them. Neurodegenerative diseases, among which one of the most common is Alzheimer's disease, are a multifactorial disease and therefore demand multiple therapeutic approaches. One of the most important therapeutic strategies is controlling the level of acetylcholine-a neurotransmitter in cholinergic synapses-by blocking the degradation of acetylcholine using acetylcholinesterase inhibitors such as tacrine, galantamine, donepezil and rivastigmine. However, these drugs can cause some adverse side effects, such as hepatotoxicity and gastrointestinal disorder. Thus, the search for new, more effective drugs is very important. In the last few years, different active constituents from plants have been tested as potential drugs in neurodegenerative disease therapy. The availability, lower price and less toxic effects of herbal medicines compared with synthetic agents make them a simple and excellent choice in the treatment of neurodegenerative diseases. The empirical approach to discovering new drugs from the systematic screening of plant extracts or plant-derived compounds is still an important strategy when it comes to finding new biologically active substances. The aim of this review is to identify new, safe and effective compounds that are potential candidates for further in vivo and clinical tests from which more effective drugs for the treatment of Alzheimer's disease could be selected. We reviewed the methods used to determine anti-Alzheimer's disease activity. Here, we have discussed the relevance of plant-derived compounds with in vitro activity. Various plants and phytochemical compounds have shown different activity that could be beneficial in the treatment of Alzheimer's disorders. Most often, medicinal plants and their active components have been investigated as acetylcholinesterase and/or butyrylcholinesterase activity inhibitors, modifiers of ß-amyloid processing and antioxidant agents. This study also aims to highlight species with assessed efficacy, usable plant parts and the most active plant components in order to identify species and compounds of interest for further study. Future research directions are suggested and recommendations made to expand the use of medicinal plants, their formulations and plant-derived active compounds to prevent, mitigate and treat Alzheimer's disease.


Assuntos
Doença de Alzheimer , Doenças Neurodegenerativas , Plantas Medicinais , Acetilcolina , Acetilcolinesterase/uso terapêutico , Idoso , Doença de Alzheimer/tratamento farmacológico , Doença de Alzheimer/metabolismo , Butirilcolinesterase/uso terapêutico , Inibidores da Colinesterase/farmacologia , Inibidores da Colinesterase/uso terapêutico , Humanos , Doenças Neurodegenerativas/tratamento farmacológico , Compostos Fitoquímicos/uso terapêutico , Plantas Medicinais/química
8.
Environ Sci Pollut Res Int ; 29(45): 67981-67996, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-35525893

RESUMO

Alzheimer's disease (AD) is a slowly progressive brain degenerative disorder which gradually impairs memory, thinking, and ability to perform easy routine tasks. This degenerative disorder mainly targets the elderly people and has imposed an endemic burden on society. Hence, there is a crucial need to investigate the efficacious herbal pharmacotherapies that can effectively mitigate and prevent the pathological hallmarks of AD. The current study aims to explore the potential efficacy of curcuminoid-rich extract (CRE) and its ternary complex (TC). Experimental rodents were administered with AlCl3 (300 mg/kg) to induce AD and treated with rivastigmine, curcuminoid crude extract, CRE, and TC orally for three consecutive weeks. Neurobehavioral, biochemical, and histopathological studies were performed from the last week of the study period. The mRNA expression of different pathological biomarkers was estimated by RT-qPCR analysis. The results of the study suggested that CRE and TC significantly improved the behavioral, biochemical parameters and acetylcholinesterase inhibitory activity in treatment groups. Histological analysis was also carried out indicating that the neurodegenerative changes and neuronal loss were stabilized by CRE and TC supplementation. CRE and TC supplementation remarkably downregulated the interleukin-1α, tumor necrosis factor-α, interleukin-1ß, acetylcholinesterase, and ß-secretase pathological gene expression. Hence, it was concluded that CRE and TC may act as promising candidates in the prevention of AD via numerous underlying signaling pathways.


Assuntos
Doença de Alzheimer , Fármacos Neuroprotetores , Acetilcolinesterase/metabolismo , Cloreto de Alumínio/toxicidade , Doença de Alzheimer/tratamento farmacológico , Secretases da Proteína Precursora do Amiloide/metabolismo , Secretases da Proteína Precursora do Amiloide/uso terapêutico , Animais , Biomarcadores/metabolismo , Misturas Complexas/uso terapêutico , Misturas Complexas/toxicidade , Diarileptanoides/uso terapêutico , Diarileptanoides/toxicidade , Modelos Animais de Doenças , Humanos , Interleucina-1alfa/uso terapêutico , Interleucina-1alfa/toxicidade , Interleucina-1beta/metabolismo , Fármacos Neuroprotetores/uso terapêutico , RNA Mensageiro , Rivastigmina/uso terapêutico , Rivastigmina/toxicidade , Fator de Necrose Tumoral alfa/metabolismo
9.
J Food Biochem ; 46(7): e14153, 2022 07.
Artigo em Inglês | MEDLINE | ID: mdl-35403720

RESUMO

Ziziphi Spinosae Semen (the dried seeds of Ziziphus jujuba Mill. var. spinosa, Rhamnaceae) is a well-known traditional Chinese medicine (TCM) with high edible and pharmaceutical value. It contains abundant phytochemicals and possesses multiple biological activities. Phytochemicals include saponins, flavonoids, alkaloids, fatty acids, and others. Among them, saponins and flavonoids are considered to be the characteristic components of Ziziphi Spinosae Semen. Both crude extracts and isolated compounds exhibit excellent bioactivities, including sedative-hypnosis, anti-anxiety, antidepressant, anticancer, anti-inflammatory, anti-Alzheimer's disease (AD), and others. Its potential therapeutic effect on AD has received increasing attention in recent years. Updated reviews to summarize the current research progress and deficiencies are urgently needed. This review summarized its pharmacological activity, quality control, and application. In addition, the existing problems and future development directions are also discussed. PRACTICAL APPLICATIONS: Ziziphi Spinosae Semen is a vital traditional Chinese medicine that has a varied therapeutic effects. It is also added to food products due to its nontoxic properties. Reliable pharmacological studies have confirmed that it has multiple pharmacological activities. Particularly, its potential therapeutic effect on Alzheimer's disease (AD) has received significant attention, which makes Ziziphi Spinosae Semen an important potential candidate in the research of new drugs and health foods for the prevention of AD. This paper reviews the recent studies on Ziziphi Spinosae Semen in the treatment of AD. In addition, the quality control methods and practical applications are systematically summarized. It may provide essential guidance for the further utilization of Ziziphi Spinosae Semen in food and pharmaceutical industry.


Assuntos
Saponinas , Ziziphus , Cromatografia Líquida de Alta Pressão/métodos , Flavonoides/análise , Controle de Qualidade , Saponinas/química , Sementes/química , Ziziphus/química
10.
J Food Sci ; 87(3): 1244-1256, 2022 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-35122250

RESUMO

Phyllanthus emblica L. pomace is a waste residue obtained following juicing that contains many polyphenols. In this study, NKA-II resin was selected as the optimal macroporous resin for separation and employed to separate the crude polyphenol extract of P. emblica pomace. The separation conditions were optimized, and the polyphenol content, polyphenol components, antioxidant activity, and potential anti-Alzheimer's effects of the extract were measured before and after purification. Results showed that the polyphenol content of the purified extract was 656.85 mg/g, which was 2.1 times higher than that of the nonpurified form. Further, the polyphenol components of the pomace, which was like that of the fruit, did not vary after purification. The antioxidant activity of the purified extract was also significantly improved. Moreover, purified extract significantly reduced the paralysis rate of the transgenic Caenorhabditis elegans model of Alzheimer's disease, and the mechanism was related to maintenance of redox homeostasis. PRACTICAL APPLICATION: The polyphenol content and antioxidant activity of purified polyphenol from Phyllanthus emblica L. pomace extracts were significantly improved using optimal separation methods with NKA-II macroporous resin and 70% aqueous ethanol as the eluent in this study. Moreover, purified polyphenols showed potential effects in alleviating Alzheimer's disease. These results suggest that polyphenols separated from P. emblica pomace are valuable for further research and development, and the utilization rate of P. emblica fruit is improved due to the further development of P. emblica pomace.


Assuntos
Phyllanthus emblica , Antioxidantes/análise , Antioxidantes/farmacologia , Frutas/química , Phyllanthus emblica/química , Extratos Vegetais/química , Polifenóis/análise , Polifenóis/farmacologia
11.
Plant Foods Hum Nutr ; 77(1): 62-67, 2022 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-34853948

RESUMO

Elsholtzia rugulosa Hemsl., a species of the Labiatae family, has a long history of use as a honey plant, herbal tea, and folk medicine in China. However, little is known about its composition and biological activities. The present study aimed to investigate the total phenol and flavonoid contents, phytochemical composition, and multiple biological activities of this plant. The total flavonoid content of the ethyl acetate fraction (EAF) was higher than those of the petroleum ether fraction (PEF), n-butanol fraction (NBF), and water fraction (WF). The EAF also had much stronger antioxidant, cytotoxic, hepatoprotective, and acetylcholinesterase (AChE) and α-glucosidase inhibitory activities than the PEF, NBF, and WF. More importantly, the IC50 values of the EAF and NBF against α-glucosidase were much lower than that of the positive control acarbose, indicating their potent α-glucosidase inhibitory activities. The isolation of the EAF led to the acquisition of 9 compounds, four of which (ß-daucosterol, methyl rosmarinate, betulinic acid, and oleanolic acid) possessed significant α-glucosidase inhibitory activities. Maltol 6'-O-(5-O-p-coumaroyl)-ß-D-apiofuranosyl-ß-D-glucopyranoside and rosmarinic acid were the major phenolic compounds in the EAF according to the HPLC-DAD analysis. All these findings indicate that the EAF, NBF, and some isolated compounds have the potential to be developed as antidiabetic drugs. Moreover, the dual inhibition of AChE and butyrylcholinesterase (BChE) of certain fractions indicates their potential in the development of anti-Alzheimer's disease drugs. The present study provides a new understanding of the phytochemistry and bioactivity of E. rugulosa.


Assuntos
Hipoglicemiantes , Lamiaceae , Acetilcolinesterase , Antibacterianos , Antioxidantes/química , Butirilcolinesterase , Flavonoides/química , Hipoglicemiantes/química , Lamiaceae/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , alfa-Glucosidases
12.
J Food Biochem ; 45(12): e13975, 2021 12.
Artigo em Inglês | MEDLINE | ID: mdl-34676566

RESUMO

Daucus carota L. ssp. major (DCM) plant is widely used in traditional medicine to treat some types of cancer and various diseases. Therefore, we evaluated the biological activities of this plant to define its effects against prostate cancer (PCa), Alzheimer's disease (AD), oxidation, and diabetes mellitus (DM) as well as identified its phenolic composition. To determine the anti-cancer properties of the plant extract, we treated PCa cells with the extract at a concentration range of 0.25, 0.5, 1, 2, and 4 mg/ml. Significant results were obtained against the PC3 cells compared to normal PNT1a prostate epithelial cells. As a result of precise measurements at the millimolar level, it was observed that the plant extract showed an effective inhibition (IC50 ) against glutathione S-transferase (GST; 12.84 mM), acetyl cholinesterase (AChE; 15.07 mM), and α-Gly (11.75 mM) enzymes when compared with standard inhibitors. Antioxidant activities of DCM methanol extract were determined via two well-known in vitro techniques. The extracts showed antioxidant activities against the DPPH and ABTS+ . The LC-ESI-MS/MS was used to determine the phenolic compounds of methanol extract from DCM. Chlorogenic acid (2,089.096 µg/g), shikimic acid (193.14 µg/g), and coumarin (113.604 µg/g) were characterized as major phenolic compounds. In addition, the interactions of chlorogenic acid, chrysin, coumarin, and shikimic acid with the used three enzymes have been calculated using molecular docking simulation. PRACTICAL APPLICATIONS: Plant natural phenolic compounds have protective effects such as anti-inflammatory, antioxidant, anticarcinogen, and enzyme inhibitory. Therefore, it has an important place in the food and pharmaceutical industry. The present study aims to reveal the enzyme inhibitory, antioxidant, and anticarcinogenic properties of the Daucus carota ssp. Major (DCM) plant extract. Significant results were obtained against the PC3 cells compared to normal PNT1a prostate epithelial cells. DCM extract demonstrated considerable antioxidant activity and inhibitory potential on used metabolic enzymes. These biological effects are thought to have a relationship with rich chemical composition.


Assuntos
Acetilcolinesterase , Daucus carota , Glutationa Transferase , Glicosídeo Hidrolases , Humanos , Masculino , Simulação de Acoplamento Molecular , Células PC-3 , Compostos Fitoquímicos , Extratos Vegetais/farmacologia , Próstata , Espectrometria de Massas em Tandem
13.
Brain Res Bull ; 174: 281-295, 2021 09.
Artigo em Inglês | MEDLINE | ID: mdl-34216649

RESUMO

Rehmannia glutinosa, the fresh or dried root of Rehmannia glutinosa (Gaertn.) Libosch. ex Fisch. & Mey., and Gardenia, the fruit of Gardenia jasminoides Ellis from Rubiaceae, both are famous traditional Chinese medicines that have been traditionally used in China. Catalpol and geniposide, as two kinds of iridoid glycosides with high activities, are the main bioactive components in Rehmannia glutinosa and Gardenia jasminoides Ellis, respectively. Over the past few decades, catalpol and geniposide have been widely studied for their therapeutic effects. The preclinical experiments demonstrated that they possessed significant neuroprotective activities against Alzheimer's disease, Parkinson's disease, stroke, and depression, etc. In this paper, the pharmacological effects and mechanisms of catalpol and geniposide on Alzheimer's disease and Parkinson's disease from 2005 to now were systematically summarized and comprehensively analyzed. At the same time, the pharmacokinetic characteristics of the analyzed compounds were also described, hoping to provide some enlightenment for the design, research, and development of iridoid glycosides.


Assuntos
Doença de Alzheimer/tratamento farmacológico , Antiparkinsonianos/uso terapêutico , Glucosídeos Iridoides/uso terapêutico , Iridoides/uso terapêutico , Doença de Parkinson/tratamento farmacológico , Animais , Medicamentos de Ervas Chinesas/farmacologia , Medicamentos de Ervas Chinesas/uso terapêutico , Gardenia/química , Humanos , Glucosídeos Iridoides/farmacologia , Iridoides/farmacologia , Medicina Tradicional Chinesa , Rehmannia/química
14.
J Sep Sci ; 44(9): 2006-2014, 2021 May.
Artigo em Inglês | MEDLINE | ID: mdl-33650266

RESUMO

In this study, a rapid and highly efficient method was developed for the separation of eight isoquinoline alkaloids using supercritical fluid chromatography. The separation conditions were carefully optimized including stationary phases, additives, backpressure, and temperature. Compared to high-performance liquid chromatography, the use of supercritical fluid chromatography could provide a 13 times faster separation. Subsequently, the method was validated and applied for the determination of eight alkaloids from different parts of Mahonia bealei (Fort.) Carr. (stem, root, leaf, and seed). The results indicated a good repeatability with relative standard deviations for overall precisions lower than 3.2%. The limit of detection was between 0.4 and 2.3 µg/mL while limit of quantitation ranged from 1.5 to 7.5 µg/mL. Recovery ranged from 95.7 to 102.5% indicating a validity of recovery. The content of total eight alkaloids was the highest in stem (66.0 µg/g) and root (65.1 µg/g) compared to leaf or seed. Moreover, anti-acetylcholinesterase activity for those extracts was evaluated by Ellman's colorimetric assay. As a result, the acetylcholinesterase inhibitory activity of the extracted samples was in the following decreasing order: stem > root > leaf or seed. In conclusion, the results indicated that supercritical fluid chromatography could be a useful tool for quality control of Mahonia bealei (Fort.) Carr. containing alkaloids as active compounds.


Assuntos
Alcaloides/isolamento & purificação , Isoquinolinas/isolamento & purificação , Mahonia/química , Alcaloides/química , Cromatografia com Fluido Supercrítico , Isoquinolinas/química , Estrutura Molecular , Folhas de Planta/química , Raízes de Plantas/química , Caules de Planta/química , Plantas Medicinais/química , Sementes/química
15.
Fitoterapia ; 151: 104867, 2021 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-33621655

RESUMO

Salvia castanea (Family Labiatae), a perennial fragrant herb with castaneous flowers, is mainly distributed in areas with an altitude of 2500-3750 m. The roots of this plant were used as a tea drink by local residents to strengthen physical health. The aim of present study was to acquire secondary metabolites of the ethanol extract obtained from the whole plant of S. castanea and to evaluate their potential anti-Alzheimer's disease. Six new sesquiterpene lactones, salcastanins A-F (1-6), together with three known guaiane-type sesquiterpenoids nubiol (7), nubdienolide (8), and nubenolide (9), were separated from the whole plant of S. castanea. The structures of these compounds were determined by HRESIMS and NMR experiments. The absolute configurations of 1-6 were ascertained by electronic circular dichroism (ECD) experiments. The humanized Caenorhabditis elegans AD pathological model was used to evaluate anti-Alzheimer's disease (AD) activities of 1-9. The results showed the compounds 1-3 and 7 significantly delayed AD-like symptoms of worm paralysis phenotype, which could be used as novel anti-AD candidates.


Assuntos
Doença de Alzheimer/tratamento farmacológico , Extratos Vegetais/química , Salvia/química , Sesquiterpenos/farmacologia , Animais , Caenorhabditis elegans/efeitos dos fármacos , China , Modelos Animais de Doenças , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Sesquiterpenos/isolamento & purificação
16.
J Diet Suppl ; 18(2): 183-226, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-32242751

RESUMO

Withania somnifera, commonly known as "Ashwagandha" or "Indian ginseng" is an essential therapeutic plant of Indian subcontinent regions. It is regularly used, alone or in combination with other plants for the treatment of various illnesses in Indian Systems of Medicine over the period of 3,000 years. Ashwagandha (W. somnifera) belongs to the genus Withania and family Solanaceae. It comprises a broad spectrum of phytochemicals having wide range of biological effects. W. somnifera has demonstrated various biological actions such as anti-cancer, anti-inflammatory, anti-diabetic, anti-microbial, anti-arthritic, anti-stress/adaptogenic, neuro-protective, cardio-protective, hepato-protective, immunomodulatory properties. Furthermore, W. somnifera has revealed the capability to decrease reactive oxygen species and inflammation, modulation of mitochondrial function, apoptosis regulation and improve endothelial function. Withaferin-A is an important phytoconstituents of W. somnifera belonging to the category of withanolides been used in the traditional system of medicine for the treatment of various disorders. In this review, we have summarized the active phytoconstituents, pharmacologic activities (preclinical and clinical), mechanisms of action, potential beneficial applications, marketed formulations and safety and toxicity profile of W. somnifera.


Assuntos
Extratos Vegetais/farmacologia , Withania , Vitanolídeos , Humanos , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/toxicidade , Extratos Vegetais/toxicidade , Withania/química , Vitanolídeos/farmacologia , Vitanolídeos/toxicidade
17.
Int J Pharm ; 593: 120138, 2021 Jan 25.
Artigo em Inglês | MEDLINE | ID: mdl-33278497

RESUMO

Plant-based remedies have been widely used for the management of variable diseases due to their safety and less side effects. In the present study, we investigated Saussurea lappa CB. Clarke. (SL) given its largely reported medicinal effects. Specifically, our objective was to provide an insight into a new polymethyl methacrylate based nanocapsules as carriers of SL essential oil and characterize their biologic functions. The nanoparticles were prepared by nanoprecipitation technique, characterized and analyzed for their cytotoxicity, anti-inflammatory, anti-Alzheimer and antidiabetic effects. The results revealed that the developed nanoparticles had a diameter around 145 nm, a polydispersity index of 0.18 and a zeta potential equal to +45 mV and they did not show any cytotoxicity at 25 µg·mL-1. The results also showed an anti-inflammatory activity (reduction in metalloprotease MMP-9 enzyme activity and RNA expression of inflammatory cytokines: TNF-α, GM-CSF and IL1ß), a high anti-Alzheimer's effect (IC50 around 25.0 and 14.9 µg·mL-1 against acetylcholinesterase and butyrylcholinesterase, respectively), and a strong antidiabetic effect (IC50 were equal to 22.9 and 75.8 µg·mL-1 against α-amylase and α-glucosidase, respectively). Further studies are required including the in vivo studies (e.g., preclinical), the pharmacokinetic properties, the bioavailability and the underlying associated metabolic pathways.


Assuntos
Nanocápsulas , Óleos Voláteis , Saussurea , Anti-Inflamatórios/farmacologia , Inibidores da Colinesterase/farmacologia , Hipoglicemiantes/farmacologia , Óleos Voláteis/farmacologia , Extratos Vegetais
18.
J Food Biochem ; 44(11): e13472, 2020 11.
Artigo em Inglês | MEDLINE | ID: mdl-33000487

RESUMO

In this study, Salvia aegyptiaca and Salvia verbenaca aerial part decoction and methanol extracts (SAE DE, SAE ME, SVR DE, and SVR ME) were screened for their in vitro antioxidant, anti-Alzheimer, and antidiabetic enzymes inhibition activities. The antioxidant properties of Salvia extracts were determined using DPPH radical scavenging, ABTS radical scavenging, Alkaline DMSO superoxide radical scavenging, ß-carotene bleaching, reducing power, and metal chelating activity assays. All extracts showed high antioxidant capacity and the antioxidant properties with the best performance were detected in the SAE ME and SVR ME. The extracts of S. aegyptiaca and S. verbenaca showed a low inhibitory activity of acetylcholinesterase (AChE), whereas, the methanol extract of S. aegyptiaca had the highest inhibitory activity on butyrylcholinesterase (BChE) (71.60 ± 4.33% for 100 µg/ml) compared to the other extracts. In vitro inhibitory effect on diabetic enzymes showed that the ME inhibited α-amylase enzyme with an IC50 86 and 101 µg/ml for SAE and SVR, respectively. Similarly, both extracts inhibited α-glucosidase with (IC50 97 and 150 µg/ml, respectively). The decoction extracts exhibited lower activity on both enzymes. PRACTICAL APPLICATIONS: It is becoming evident that oxidative stress is involved in several acute and chronic diseases. Counteracting free radical generation has become one of the widest fields of research worldwide. This study deals with the in vitro antioxidant activity of two plants from the Salvia genus as well as the assessment of their in vitro inhibitory properties of four key enzymes implicated in diabetes and Alzheimer's disease. Concerning the practical applications of our work, it can be explored in its antioxidant part as a food supplement to prevent the excess of free radicals in the body and also in other industrial practices. Another potential use is in the prevention and amelioration of both diabetes and Alzheimer's disease symptoms for the extracts that had enzyme inhibitory activity, but this deserves further toxicological and in vivo studies.


Assuntos
Antioxidantes , Salvia , Antioxidantes/farmacologia , Inibidores da Colinesterase/farmacologia , Extratos Vegetais/farmacologia , alfa-Amilases , alfa-Glucosidases
19.
Molecules ; 25(11)2020 Jun 03.
Artigo em Inglês | MEDLINE | ID: mdl-32503261

RESUMO

Alzheimer's disease (AD) is a progressive neurodegenerative disorder. To fight the disease, natural products, including mulberry, with antioxidant activities and inhibitory activities against key enzymes (acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and beta-secretase 1 (BACE-1)) are of interest. However, even in the same cultivars, mulberry trees grown in different populated locations might possess disparate amounts of phytochemical profiles, leading to dissimilar health properties, which cause problems when comparing different cultivars of mulberry. Therefore, this study aimed to comparatively investigate the phytochemicals, antioxidant activities, and inhibitory activities against AChE, BChE, and BACE-1, of twenty-seven Morus spp. cultivated in the same planting area in Thailand. The results suggested that Morus fruit samples were rich in phenolics, especially cyanidin, kuromanin, and keracyanin. Besides, the aqueous Morus fruit extracts exhibited antioxidant activities, both in single electron transfer (SET) and hydrogen atom transfer (HAT) mechanisms, while strong inhibitory activities against AD key enzymes were observed. Interestingly, among the twenty-seven Morus spp., Morus sp. code SKSM 810191 with high phytochemicals, antioxidant activities and in vitro anti-AD properties is a promising cultivar for further developed as a potential mulberry resource with health benefits against AD.


Assuntos
Antioxidantes/farmacologia , Inibidores Enzimáticos/farmacologia , Morus/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Acetilcolinesterase , Doença de Alzheimer/prevenção & controle , Secretases da Proteína Precursora do Amiloide/antagonistas & inibidores , Ácido Aspártico Endopeptidases/antagonistas & inibidores , Butirilcolinesterase/química , Proteínas Ligadas por GPI/antagonistas & inibidores , Humanos
20.
Fitoterapia ; 142: 104536, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-32145310

RESUMO

Commiphoins A-C (1-3), three new cadinane-type sesquiterpenes, together with two known cadinane-type sesquiterpenes (4 and 5) were isolated from the resinous exudates of Commiphora myrrha. Their structures and relative configurations were established on the basis of comprehensive spectroscopic methods, including HRESIMS, 1D and 2D NMR analyses. Compounds 1 and 3-5 were screened for anti-Alzheimer's disease (AD) activities using the AD pathological model in Caenorhabditis elegans. The results showed that they all had significant anti-AD activities.


Assuntos
Doença de Alzheimer/tratamento farmacológico , Commiphora/química , Sesquiterpenos Policíclicos/isolamento & purificação , Animais , Animais Geneticamente Modificados , Caenorhabditis elegans , Avaliação Pré-Clínica de Medicamentos , Sesquiterpenos Policíclicos/química , Sesquiterpenos Policíclicos/uso terapêutico , Resinas Vegetais/química
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