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1.
Pak J Pharm Sci ; 36(2): 565-577, 2023 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-37530166

RESUMEN

Currently, prolong use of standard anti-epileptics may cause tolerance and ineffective for about 30% of epileptic patients. Medicinal plants provide an attractive therapeutic effect in preventing and treating seizures in traditional and folk medicine. In this study, we investigate the antiepileptic effects of PTAT decoction on acute and chronic seizure models in mice and explore the potential mechanisms. PTAT decoction dose-dependently protected mice against MES and PTZ induced seizure. Meanwhile, it decreased the seizure severity and reduced seizure-caused anxious behavior in the PTZ-kindling mice, suggesting a significant antiepileptic activity and anxiolytic/anxiogenic potential. PTAT decoction dose-dependently increased the levels of GSH and the activity SOD and CAT, while decreased the level of MDA in the hippocampi of treated mice. Furthermore, a significant decrease in the proinflammatory cytokine levels, including TNF-α, IL-1ß, IL-6 and MCP-1 was found in treated mice compared with the mice in the vehicle + PTZ group. Moreover, PTAT decoction dose-dependently reversed the alterations induced by PTZ in GABA, GABA-T, L-GAD and glutamate levels in kindling mice, showing an effect on the modulation of the GABA neurotransmission. Thus, PTAT decoction has a promising anticonvulsant activity mediated via multiple mechanisms, which might be used as an up-and-coming phytotherapy strategy in the management of epilepsy and its complications.


Asunto(s)
Acorus , Epilepsia , Polygala , Ratones , Animales , Anticonvulsivantes/efectos adversos , Acorus/metabolismo , Polygala/metabolismo , Pentilenotetrazol/toxicidad , Convulsiones/inducido químicamente , Convulsiones/tratamiento farmacológico , Convulsiones/prevención & control , Epilepsia/inducido químicamente , Epilepsia/tratamiento farmacológico , Estrés Oxidativo , Ácido gamma-Aminobutírico/farmacología , Ansiedad/inducido químicamente , Ansiedad/tratamiento farmacológico , Inflamación/tratamiento farmacológico
2.
Metab Brain Dis ; 38(6): 1877-1893, 2023 08.
Artículo en Inglés | MEDLINE | ID: mdl-37043151

RESUMEN

Epilepsy is a serious public health problem in the world. At present, over 30% of affected patients remain refractory to currently available treatment. Medicinal plants as pharmaceuticals and healthcare treatments have been frequently used in the management of epilepsy in China for many centuries. Gastrodia elata-Acous tatarinowii (GEAT), as a classic and most commonly used herb pair in traditional Chinese medicine (TCM), has been employed to control seizures for thousands of years. However, the animal experiment data on its anticonvulsant effect is limited in the literature. Thus, this study aimed to reveal the therapeutic actions of GEAT decoction against seizures in mice. UHPLC-MS/MS was performed to analyze the chemical components of GEAT decoction. The mice were given GEAT decoction for 7 days, and MES, PTZ, and 3-MP injection was given 30 min after the last administration. Video monitoring was performed for comparisons. In addition, the PTZ-induced kindling models were conducted to investigate the seizure severity, anxiety and cognitive profile, inflammation, and oxidative stress parameters in mice. The results showed that GEAT decoction dose-dependently protected mice against MES, 3-MP, and PTZ-induced acute seizures. Furthermore, GEAT decoction significantly ameliorated seizure severity, decreased the accumulation of inflammatory mediators TNF-α, IL-1ß, and IL-6, mitigated oxidative stress, as well as alleviated anxious-like behavior and cognitive deficits in PTZ-kindled mice. These results suggest that GEAT decoction possesses certain anticonvulsant properties, which might be clinically useful as phytotherapy alone or as an adjunct therapy for the prevention and treatment of seizures and epilepsy.


Asunto(s)
Acorus , Epilepsia , Gastrodia , Ratones , Animales , Anticonvulsivantes/efectos adversos , Gastrodia/química , Acorus/química , Espectrometría de Masas en Tándem , Convulsiones/inducido químicamente , Convulsiones/tratamiento farmacológico , Convulsiones/prevención & control , Epilepsia/inducido químicamente , Epilepsia/tratamiento farmacológico , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico
3.
Phytochemistry ; 210: 113626, 2023 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-36871902

RESUMEN

A. calamus var. angustatus Besser is an important traditional medicinal herb commonly used in China and other Asian countries. This study is the first systematic review of the literature to thoroughly analyze the ethnopharmacological application, phytochemistry, pharmacology, toxicology and pharmacokinetic properties of A. calamus var. angustatus Besser and provides a rationale for future research and prospects for application in clinical treatment. Information on relevant studies investigating A. calamus var. angustatus Besser was collected from SciFinder, the Web of Science, PubMed, CNKI, Elsevier, ResearchGate, ACS, Flora of China, and Baidu Scholar, etc. up to December 2022. In addition, information was also obtained from Pharmacopeias, books on Chinese herbal classics, local books, as well as PhD and MS dissertations. A. calamus var. angustatus Besser has played an important role in the herbal treatment of coma, convulsion, amnesia, and dementia for thousands of years. Studies investigating the chemical constituents of A. calamus var. angustatus Besser have isolated and identified 234 small-molecule compounds and a few polysaccharides. Among them, simple phenylpropanoids represented by asarone analogues and lignans are the two main active ingredients, which can be considered characteristic chemotaxonomic markers of this herb. In vitro and in vivo pharmacological studies indicated that crude extracts and active compounds from A. calamus var. angustatus Besser display a wide range of pharmacological activities, especially as treatment for Alzheimer's disease (AD), and anticonvulsant, antidepressant-like, anxiolytic-like, anti-fatigue, anti-Parkinson, neuroprotection, and brain protection properties, providing more evidence to explain the traditional medicinal uses and ethnopharmacology. The clinical therapeutic dose of A. calamus var. angustatus Besser does not present any toxic effects, but its main active ingredients α-asarone and ß-asarone at excessive dose may lead to toxicity, and in particular, their respective epoxide metabolites may exert potential toxicity to the liver. This review provides a reference and further information for the future development and clinical application of A. calamus var. angustatus Besser.


Asunto(s)
Acorus , Medicamentos Herbarios Chinos , Plantas Medicinales , Medicamentos Herbarios Chinos/química , Etnofarmacología , Medicina Tradicional China , Fitoquímicos , Extractos Vegetales/química
4.
BMC Nurs ; 21(1): 352, 2022 Dec 12.
Artículo en Inglés | MEDLINE | ID: mdl-36503477

RESUMEN

BACKGROUND: Fatigue is a symptom characterized by an elevated prevalence in patients undergoing hemodialysis, which may cause extreme mental and muscular debilitation, significantly influencing social interaction, life quality and well-being. However, the significance of fatigue to patients undergoing hemodialysis has not been recognized yet, and prevention and management of fatigue in this population have not been thoroughly investigated. Additionally, previous studies mainly focused on muscular fatigue, while mental fatigue has been seldom discussed. This study aims to investigate the interaction between nurses and multidisciplinary of nonpharmacological integrated care interventions (NICIs) and assess the impact of fatigue on patients undergoing hemodialysis. METHODS: The integrative nonpharmacological care interventions in this study included walking, motivational interviewing (MI) and health education regarding behavioral self-management. A single-center randomized controlled trial was conducted in the dialysis center of the nephrological department in a tertiary affiliated hospital of medical university from January to June 2019. A total of 118 patients were selected and randomly divided into the intervention group (IG) and the control group (CG). Four patients dropped out during the study, and 114 patients were enrolled for the eventual analysis. The 60 patients in the IG received routine nursing combined with integrated care interventions, while the 54 patients in the CG received routine nursing only. This study lasted for six months. RESULTS: The experimental group exhibited significant reductions of overall fatigue (2.26 vs. 0.48), mental fatigue (1.41 vs. 0.54), muscular fatigue (2.13 vs. 0.75), and some biochemical indicators (e.g., serum urea) (P<0.05), compared with the CG. CONCLUSIONS: Nurses and multidisciplinary teams have been demonstrated to play a key role and interplay function in chronic disease management. Hence, the nurse-led multidisciplinary NICIs significantly alleviated total fatigue (muscular fatigue and mental fatigue) and improved other parameters. TRIAL REGISTRATION: ChiCTR-IOR-16008621 (March 18, 2016).

5.
Front Pharmacol ; 13: 918071, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36052142

RESUMEN

Solanum nigrum Linn., is a common edible medicinal herb of the Solanaceae family which is native to Southeast Asia and is now widely distributed in temperate to tropical regions of Europe, Asia, and America. Traditionally, it has been used to treat various cancers, acute nephritis, urethritis, leucorrhea, sore throat, toothache, dermatitis, eczema, carbuncles, and furuncles. Up to now, 188 chemical constituents have been identified from S. nigrum. Among them, steroidal saponins, alkaloids, phenols, and polysaccharides are the major bioactive constituents. Investigations of pharmacological activities of S. nigrum revealed that this edible medicinal herb exhibits a wide range of therapeutic potential, including antitumor, anti-inflammatory, antioxidant, antibacterial, and neuroprotective activities both in vivo and in vitro. This article presents a comprehensive and systematic overview of the botanical, traditional uses, phytochemical compositions, pharmacological properties, clinical trials, and toxicity of S. nigrum to provide the latest information for further exploitation and applications of S. nigrum in functional foods and medicines.

6.
Pharmacol Res ; 185: 106458, 2022 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-36152740

RESUMEN

Our initial studies detected elevated levels of 3,4-dihydroxyphenyllactic acid (DHPLA) in urine samples of patients with severe heart disease when compared with healthy subjects. Given the reported anti-inflammatory properties of DHPLA and related dihydroxylated phenolic acids (DPAs), we embarked on an exploratory multi-centre investigation in patients with no urinary tract infections to establish the possible pathophysiological significance and therapeutic implications of these findings. Chinese and Caucasian patients being treated for severe heart disease or those conditions associated with inflammation (WBC ≥ 10 ×109/L or hsCRP ≥ 3.0 mg/L) and/or hypoxia (PaO2 ≤ 75 mmHg) were enrolled; their urine samples were analyzed by HPLC, HPLC-MS, GC-MS and biotransformation assays. DHPLA was detected in urine samples of patients, but undetectable in healthy volunteers. Dynamic monitoring of inpatients undergoing treatment showed their DHPLA levels declined in proportion to their clinical improvement. In DHPLA-positive patients' fecal samples, Proteus vulgaris and P. mirabilis were more abundant than healthy volunteers. In culture, these gut bacteria were capable of reversible interconversion between DOPA and DHPLA. Furthermore, porcine and rodent organs were able to metabolize DOPA to DHPLA and related phenolic acids. The elevated levels of DHPLA in these patients suggest bioactive DPAs are generated de novo as part of a human's defense mechanism against disease. Because DHPLA isolated from Radix Salvia miltiorrhizae has a multitude of pharmacological activities, these data underpin the scientific basis of this medicinal plant's ethnopharmacological applications as well as highlighting the therapeutic potential of endogenous, natural or synthetic DPAs and their derivatives in humans.


Asunto(s)
Cardiopatías , Inflamación , Humanos , Porcinos , Animales , Hipoxia , Dihidroxifenilalanina
7.
J Pain Res ; 15: 1221-1232, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-35502404

RESUMEN

Purpose: Inflammation and accompanying pain is a common global health problem that seriously affects human quality of life worldwide. Here, we aimed to investigate the anti-nociceptive and anti-inflammatory activities of the ethyl acetate extract of B. chinensis (EAEBc) along with the underlying mechanisms of action. Methods: The in vitro anti-inflammatory activity of EAEBc was explored using an LPS-induced RAW264.7 cell inflammatory model. Nitric oxide (NO) production, tumor necrosis factor (TNF)-α, interleukin (IL)-1ß, and IL-6 levels were evaluated. In vivo anti-nociceptive and anti-inflammatory activities of EAEBc were assessed with the aid of classical experimental mouse models. In addition, LPS-induced biomarker contents (TNF-α, IL-1ß, IL-6, NO, iNOS, and PGE2) and formalin-induced serum inflammatory factors (NO, PGE2, 5-HT, ß-EP, substance P, and NE) were determined in mice. Results: In vitro, EAEBc significantly reduced LPS-induced NO generation and suppressed the production of TNF-α, IL-1ß, and IL-6 in RAW264.7 cells in a concentration-dependent manner. In vivo, EAEBc downregulated serum TNF-α, IL-1ß, IL-6, NO, iNOS, and PGE2 contents in mice with LPS-induced inflammation in a dose-dependent manner. EAEBc displayed anti-inflammatory activity in carrageenan-induced paw edema and xylene ear edema tests. Intragastric administration of EAEBc at test doses of 100 and 200 mg/kg led to inhibition of nociception and capillary permeability induced by acetic acid to varying degrees. Similarly, EAEBc exerted analgesic effects in the formalin and hot plate tests. In particular, the administration of EAEBc reversed the changes in the levels of inflammatory indicators NO, PGE2, 5-HT, ß-EP, substance P, and NE in a mouse model of formalin-induced pain. Conclusion: Our findings provide considerable evidence to support the extensive application of B. chinensis in traditional medicine and demonstrate the utility of this plant species as an effective candidate for prevention or treatment of various pain and inflammation-related conditions.

8.
Front Pharmacol ; 12: 699899, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-34475822

RESUMEN

Averrhoa carambola L. (star fruit) is an edible fruit that is extensively cultivated in southern China, Southeast Asia, India, and northern South America. It has a sweet and juicy taste and is frequently used in fruit salads and fruit platters, as a garnish in cocktail drinks and beverages, or squeezed into juice and served as a beverage. Traditionally, it has been used for treating diabetes and diabetic nephropathy, arthralgia, vomiting, lithangiuria, coughing, hangovers, and chronic paroxysmal headache for thousands of years. Currently, approximately 132 compounds have been isolated from A. carambola. Among them, flavonoids, benzoquinone, and their glycosides have been considered as biologically active substances, which are responsible for various biological activities. Pharmacological studies have revealed that crude extracts or monomeric compounds from A. carambola exhibit multiple bioactivities, such as anti-oxidant, anti-hyperglycemic, anti-obesity, anti-hyperlipidemic, anti-tumor, anti-inflammatory, hepatoprotective, cardioprotective, anti-hypertensive, neuroprotective, and others. Thus, A. carambola is a valuable treatment in Chinese medicine with therapeutic potential for multiple diseases, especially diabetes and diabetes-related diseases. Even though it is a very promising candidate in the development of functional food and the pharmaceutical industry, reports on its bioactivities have only been conducted in vivo and in vitro and there is a gap in research regarding clinical settings and safety. This review therefore provides a comprehensive and systematic overview of current progress on botany, ethnopharmacology, phytochemistry, pharmacology, and toxicity of A. carambola, providing a valuable reference for further developments and applications of A. carambola in the pharmaceutical industry and functional food.

9.
Carbohydr Polym ; 261: 117863, 2021 Jun 01.
Artículo en Inglés | MEDLINE | ID: mdl-33766352

RESUMEN

Codonopsis pilosula (Franch.) Nannf., as a well-known homology plant of medicine and food, has the function of replenishing the Qi, strengthening the spleen and tonifying the lung, nourishing the blood and engendering the liquid in traditional Chinese medicine. Accumulating evidence has demonstrated that the C. pilosula polysaccharides (CPPs) are one of the major and representative pharmacologically active macromolecules and present multiple biological activities both in vitro and in vivo methods, such as immunomodulatory, antitumor, antioxidant, neuroprotective, antiviral, anti-inflammatory, anti-fatigue, hypoglycemic, anti-hypoxia, renoprotective, gastroprotective, hepatoprotective, and prebiotic. The purpose of the present review is to provide comprehensively and systematically reorganized information in the extraction and purification, structure characterization, biological activities and the underlying mechanisms of action as well as toxicities of CPPs to support their therapeutic potentials and sanitarian functions. New valuable insights for the future researches regarding CPPs were also proposed in the fields of therapeutic agents and functional foods.


Asunto(s)
Codonopsis/química , Polisacáridos/química , Polisacáridos/aislamiento & purificación , Polisacáridos/farmacología , Animales , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Antioxidantes/farmacología , Suplementos Dietéticos/análisis , Medicamentos Herbarios Chinos/química , Medicamentos Herbarios Chinos/aislamiento & purificación , Medicamentos Herbarios Chinos/farmacología , Alimentos Funcionales/análisis , Humanos , Medicina Tradicional China , Estructura Molecular , Fitoterapia , Raíces de Plantas/química
10.
Phytochemistry ; 184: 112649, 2021 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-33440297

RESUMEN

Euphorbia helioscopia L. which is called "Zeqi" in China, is a medicinal plant extensively distributed worldwide, especially in China, and has been widely used for decades to treat various diseases including edema, phlegm and cough, malaria, dysentery, scab, tuberculous fistula, osteomyelitis, and cancer. The present review aims to provide up-to-date information on E. helioscopia, including its traditional uses, phytochemistry, quality control, pharmacological research, toxicology, and human studies in exploring future scientific and therapeutic potentials in disease treatment. So far, a total of 173 terpenoids, as well as polyphenols, steroids, lipids, and volatile oils have been isolated and identified from E. helioscopia. Among them, diterpenoids and flavonoids are the most important and abundant bioactive constituents. Modern pharmacological studies have demonstrated that E. helioscopia has outstanding bioactivities especially on antiproliferative and multidrug resistance modulating. Nevertheless, most of these studies were carried out in vitro. The quality control, metabolites identification, in-depth in-vivo studies as well as toxicology and human studies for the crude extracts and active components are still very limited. Consequently, more well-designed pre-clinical and clinical studies are required to justify their reported therapeutic potential.


Asunto(s)
Euphorbia , Plantas Medicinales , China , Etnofarmacología , Fitoquímicos/farmacología , Fitoterapia , Extractos Vegetales/farmacología
11.
Am J Chin Med ; 48(1): 47-76, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-31964158

RESUMEN

The genus Saururus, belonging to Saururaceae, contains two species, S. cernuus L. and S. chinensis (Lour) Baill. with common utilization in traditional medicine from Asia to North America for the treatment of edema, beriberi, jaundice, leucorrhea, urinary tract infections, hypertension, hepatitis diseases, and tumors. An extensive review of literature was made on traditional uses, phytochemistry, and ethnopharmacology of Saururus using ethno-botanical books, published articles, and electronic databases. The 147 of chemical constituents have been isolated and identified from S. cernuus and S. chinensis, and lignans, flavonoids, alkaloids, anthraquinones, saponins, and phenols are the major constituents. Various pharmacological investigations in many in vitro and in vivo models have revealed the potential of the genus Saururus with anti-inflammatory, antitumor, anti-oxidant, hepatoprotective, antimelanogenic, lipid-lowering, and bone protective activities, supporting the rationale behind numerous of its traditional uses. Due to the noteworthy pharmacological properties, Saururus can be a better option for new drug discovery. Data regarding many aspects of this plant such as toxicology, pharmacokinetics, quality-control measures, and the clinical value of the active compounds is still limited which call for additional studies.


Asunto(s)
Medicamentos Herbarios Chinos/química , Medicamentos Herbarios Chinos/farmacología , Fitoquímicos/química , Fitoquímicos/farmacología , Saururaceae/química , Humanos , Estructura Molecular
12.
Front Pharmacol ; 11: 569800, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-33551795

RESUMEN

Juglans mandshurica Maxim., also known as "Manchurian walnut" (Chinese) and "Onigurumi" (Japanese), is a medicinal plant widely distributed in Western and Central Asia, especially in China. It has been traditionally used to treat cancer, gastric ulcers, diarrhea, dysentery, dermatosis, uterine prolapse, and leukopenia. To date, more than 400 constituents including quinones (e.g. naphthoquinones, anthraquinones, naphthalenones, tetralones), phenolics, flavonoids, triterpenoids, coumarins, lignans, phenylpropanoids, diarylheptanoids, and steroids, were isolated and structurally identified from different plant parts of J. mandshurica. Among them, quinones, phenolics, triterpenoids, and diarylheptanoids, as the major bioactive substances, have been extensively studied and displayed significant bioactivity. Previous studies have demonstrated that J. mandshurica and a few of its active components exhibit a wide range of pharmacologically important properties, such as antitumor, immunomodulatory, anti-inflammatory, neuroprotective, anti-diabetic, antiviral, antimicrobial, and anti-melanogenesis activities. However, many investigations on biological activities were mainly based on crude extracts of this plant, and the major bioactive ingredients responsible for these bioactivities have not been well identified. Further in vitro and in vivo studies on the mechanisms of action of the pure bioactive compounds, and more elaborate toxicity studies as well as clinical studies are needed to ensure safety and effectiveness of the plant for human use. Taken together, the present review will provide some specific useful suggestions guide to further investigations and applications of this plant in the preparation of medicines and functional foods.

13.
Carbohydr Polym ; 229: 115548, 2020 Feb 01.
Artículo en Inglés | MEDLINE | ID: mdl-31826474

RESUMEN

Despite the number of approved antivirals has considerably increased, these existing drugs are not always efficacious or well-tolerated and drug-resistant virus strains are rapidly emerging. Nowadays, many polysaccharides as independent or the main bioactive ingredients have been approved as medicines. The present report aims to provide systematically reorganized information on antiviral polysaccharides derived from edible and medicinal plants and mushrooms (PsEMPM) to people for better utilization of them. PsEMPM can inhibit the infection of viruses by interfering with a few steps in the virus life cycle and/or improving the host antiviral immune responses. Polyanionic nature and sulfates are in many cases required antiviral potency of PsEMPM, while it not only is a function of high charge density but also associated with distinct structural specificities. Plenty of efforts have been devoted to achieving the discovery of novel antiviral polysaccharides, however, the detailed structural characteristics of PsEMPM still merit further in-depth investigation.


Asunto(s)
Agaricales/metabolismo , Antivirales/química , Plantas Medicinales/metabolismo , Polisacáridos/farmacología , Internalización del Virus/efectos de los fármacos , Antivirales/farmacología , Virus de la Hepatitis A/fisiología , Raíces de Plantas/metabolismo , Polisacáridos/química
14.
Food Chem ; 309: 125715, 2020 Mar 30.
Artículo en Inglés | MEDLINE | ID: mdl-31685368

RESUMEN

Rhodomyrtus tomentosa (Aiton) is a flowering plant native to southern and southeastern Asia. Up to date, 106 chemical constituents have been isolated and identified from R. tomentosa. Among these compounds, triterpenoids, flavonoids, phenols and meroterpenoids are the major constituents. Investigations of pharmacological activities of R. tomentosa revealed that this edible medicinal herb exhibits a wide range of therapeutic potential including antibacterial, antitumor, anti-inflammatory and antioxidant activities both in vivo and in vitro. The purpose of this review is to provide an overview of R. tomentosa studies until 2019. This article also intends to review advances in the botanical, phytochemical, pharmacological studies and industrial applications of R. tomentosa, which will provide a useful bibliography for further investigations and applications of R. tomentosa in medicines and foods.


Asunto(s)
Myrtaceae/química , Fitoquímicos/química , Antibacterianos/química , Antibacterianos/farmacología , Antiinflamatorios/química , Antiinflamatorios/farmacología , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/farmacología , Antioxidantes/química , Supervivencia Celular/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Humanos , Myrtaceae/metabolismo , Fitoquímicos/farmacología , Plantas Medicinales/química , Plantas Medicinales/metabolismo
15.
Front Pharmacol ; 10: 1236, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-31736750

RESUMEN

Actinidia chinensis Planch. (A. chinensis), commonly known as Chinese kiwifruit, is a China native fruit, which becomes increasingly popular due to attractive economic, nutritional, and health benefits properties. The whole plant including fruits, leaves, vines, and roots of A. chinensis are used mainly as food or additive in food products and as folk medicine in China. It is a good source of triterpenoids, polyphenols, vitamin C, carbohydrate, amino acid, and minerals. These constituents render the A. chinensis with a wide range of pharmacological properties including antitumor, antioxidant, anti-inflammatory, immunoregulatory, hypolipemic, antidiabetic, and cardiovascular protective activities, suggesting that it may possibly be value in the prevention and treatment of pathologies associated to cancer, oxidative stress, and aging. This minireview provides a brief knowledge about the recent advances in chemistry, biological activities, utilization, and storage of Chinese kiwifruit. Future research directions on how to better use of this crop are suggested.

16.
Eur J Med Chem ; 183: 111650, 2019 Dec 01.
Artículo en Inglés | MEDLINE | ID: mdl-31539780

RESUMEN

Inspired by the traditional Chinese herbal pair of Polygala tenuifolia-Acori Tatarinowii for treating epilepsy, 33 novel substituted cinnamic α-asaronol esters and analogues were designed by Combination of Traditional Chinese Medicine Molecular Chemistry (CTCMMC) strategy, synthesized and tested systematically not only for anticonvulsant activity in three mouse models but also for LDH inhibitory activity. Thereinto, 68-70 and 75 displayed excellent and broad spectra of anticonvulsant activities with modest ability in preventing neuropathic pain, as well as low neurotoxicity. The protective indices of these four compounds compared favorably with stiripentol, lacosamide, carbamazepine and valproic acid. 68-70 exhibited good LDH1 and LDH5 inhibitory activities with noncompetitive inhibition type, and were more potent than stiripentol. Notably, 70, as a representative agent, was also shown as a moderately positive allosteric modulator at human α1ß2γ2 GABAA receptors (EC50 46.3 ±â€¯7.3 µM). Thus, 68-70 were promising candidates for developing into anti-epileptic drugs, especially for treatment of refractory epilepsies such as Dravet syndrome.


Asunto(s)
Anisoles/química , Anticonvulsivantes/química , Cinamatos/química , Medicamentos Herbarios Chinos/química , Ésteres/química , L-Lactato Deshidrogenasa/antagonistas & inhibidores , Polygala/química , Regulación Alostérica , Animales , Anisoles/farmacología , Anticonvulsivantes/farmacología , Carbamazepina/química , Carbamazepina/farmacología , Cinamatos/farmacología , Dioxolanos/química , Dioxolanos/farmacología , Diseño de Fármacos , Medicamentos Herbarios Chinos/farmacología , Ésteres/farmacología , Humanos , Medicina Tradicional China , Ratones , Estructura Molecular , Neuralgia/prevención & control , Receptores de GABA-A/metabolismo , Relación Estructura-Actividad , Ácido Valproico/química , Ácido Valproico/farmacología
17.
Bioorg Chem ; 88: 102832, 2019 07.
Artículo en Inglés | MEDLINE | ID: mdl-31102809

RESUMEN

Epilepsy is a group of neurological disorders characterized by recurrent seizures that disturbs about 60 million people worldwide. In this article, a novel series of 3,4,5-trimethoxycinnamic acid (TMCA) ester derivatives 1-35 were designed inspired from the traditional Chinese herb pair drugs Polygala tenuifolia and Gastrodia elata and synthesized followed by in vivo and in silico evaluation of their anticonvulsant potential. All the synthesized derivatives were biologically evaluated for their anticonvulsant potential using two acute model of seizures induced in mice, the maximal electroshock (MES) and sc-pentylenetetrazole (PTZ) models. Simultaneously, the motor impairment as a surrogate of acute neurotoxicity and in vitro screening of cytotoxicity against HepG-2 cells line were assessed through the rotarod performance test and CCK-8 assay, respectively. In addition, the physicochemical and pharmacokinetic parameters of the active compounds were determined. Our results showed that compounds 5, 7, 8, 13, 20, 25, 28, 30 and 32 exhibited preferable anticonvulsant activity in primary evaluation, with compounds 28 and 32 being the most promising anticonvulsant agents in according to results of subsequent pharmacology and toxicity evaluation. Additionally, the molecular modeling experiments predicted good binding interactions of part of the obtained active molecules with the gamma-aminobutyric acid (GABA) transferas. Therefore, it could be concluded that the synthesized derivatives 28 and 32 would represent useful lead compounds for further investigation in the development of anticonvulsant agents.


Asunto(s)
Anticonvulsivantes/uso terapéutico , Cinamatos/uso terapéutico , Convulsiones/tratamiento farmacológico , 4-Aminobutirato Transaminasa/química , 4-Aminobutirato Transaminasa/metabolismo , Animales , Anticonvulsivantes/síntesis química , Anticonvulsivantes/metabolismo , Anticonvulsivantes/farmacología , Sitios de Unión , Cinamatos/síntesis química , Cinamatos/metabolismo , Cinamatos/farmacología , Diseño de Fármacos , Epilepsia/tratamiento farmacológico , Gastrodia/química , Células Hep G2 , Humanos , Masculino , Ratones , Simulación del Acoplamiento Molecular , Estructura Molecular , Pentilenotetrazol , Polygala/química , Unión Proteica , Convulsiones/inducido químicamente , Relación Estructura-Actividad , Porcinos
18.
Mol Immunol ; 108: 81-88, 2019 04.
Artículo en Inglés | MEDLINE | ID: mdl-30784766

RESUMEN

High altitude cerebral edema (HACE), whose development process is associated with oxidative stress and inflammatory response, is a life-threatening condition caused by rapid ascent speed to high altitudes. Phenylethanoid glycosides (PhGCs) are primary active constituents isolated from Phlomis younghusbandii Mukerjee that reportedly exhibit potent anti-oxidant and anti-inflammatory activities. The present study aims to investigate the protective effect of phenylethanoid glycosides (PhGCs) from P. younghusbandii in acute hypobaric hypoxia (AHH) - stimulated HACE rats and its underlying mechanisms. The expression of pro-inflammatory cytokine levels (IL-1ß, TNF-α, and IL-6) was detected by RT-PCR and ELISA at mRNA and protein levels in brain tissues. Western blotting was carried out to measure the major protein levels (IL-1ß, TNF-α, and NF-κB) in brain tissues. The oxidative stress biomarkers (MDA, SOD, and GSH) were evaluated using kits. Results demonstrate that PhGCs significantly improved pathological changes in brain tissues, reduced the brain's water content, and attenuated the production and mRNA expression of pro-inflammatory cytokines. Furthermore, the increased oxidative stress and the decrease in anti-oxidant stress system under the AHH condition were also abrogated reversely through PhGCs treatment by elevating the levels of SOD and GSH and suppressing the accumulation of MDA. Simultaneously, there was also a significant reduction in NF-κB, IL-1ß, and TNF-α protein expression levels in brain tissues, suggesting that blocking the NF-κB signaling pathway activation prevented the production of pro-inflammatory cytokines. Taken together, these findings indicate that PhGCs may afford a protectively intervene in HACE through the suppression of oxidative stress and inflammatory response via the inhibition of the NF-κB signaling pathway, indicating that PhGCs are promising agents for the treatment of acute HACE.


Asunto(s)
Mal de Altura/tratamiento farmacológico , Edema Encefálico/tratamiento farmacológico , Edema Encefálico/etiología , Glicósidos/uso terapéutico , Hipoxia/complicaciones , Alcohol Feniletílico/uso terapéutico , Phlomis/química , Enfermedad Aguda , Animales , Citocinas/genética , Citocinas/metabolismo , Glicósidos/farmacología , Mediadores de Inflamación/metabolismo , Masculino , FN-kappa B/metabolismo , Estrés Oxidativo/efectos de los fármacos , Alcohol Feniletílico/farmacología , ARN Mensajero/genética , ARN Mensajero/metabolismo , Ratas Wistar , Transducción de Señal/efectos de los fármacos , Agua
19.
J Ethnopharmacol ; 231: 337-354, 2019 Mar 01.
Artículo en Inglés | MEDLINE | ID: mdl-30472402

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: The dried fruit of Tetradium ruticarpum is frequently utilized as a common traditional medicine in China, Japan and Korea. It has been widely used for the treatment of various diseases such as headache, menorrhalgia, dermatophytosis, celialgia, emesis and aphtha and so on. AIM OF THIS REVIEW: Despite the wide biological activities of Tetradium plants, there is no current review summarizing medicinal properties of the genus of plants; thus, this review aims to systematically summarize studies on botanical characteristics, traditional uses, phytochemical ingredients, quality control, pharmacokinetics, pharmacological activities and toxicity of Tetradium species to demonstrate their therapeutic capacity. MATERIALS AND METHODS: Information and materials related to Tetradium species were obtained from scientific databases such as Google Scholar, Wikipedia, Web of Science, PubMed, ScienceDirect, ACS Publications, SciFinder. Information was also gathered from International Plant Names Index, Global Biodiversity Information Facility, Chinese Pharmacopoeia and Traditional Chinese Medicine classics, etc. All studies of this genus were included in this review until July 2018. RESULTS: Tetradium is widely assessed regarding its phytochemistry and biological activities. Approximately 131 chemical compounds, including alkaloids, saponins, phenols and other compounds, have been isolated from Tetradium plants. Among these components, alkaloid evodiamine is the most representative active ingredients of Tetradium plants. These compounds isolated from Tetradium plants exhibit a wide range of biological activities in vitro and in vivo including antitumor, antibacterial, anti-inflammatory, insecticide, cardioprotective and lipid-lowering, treating CNS disorders, digestive system regulation and endocrine system improving activities. Furthermore, alkaloids could be used as markers for quality identification and evaluation of medicinal materials and their preparations. Information on evaluating the safety and pharmacokinetics of Tetradium often focuses on the alkaloids, thus further study and clinical data are required to enable the drug safety of the utilization of Tetradium plants. CONCLUSIONS: Phytochemical and pharmacological studies of Tetradium plants have proved Tetradium plants are important medicinal herb resource. However, well-designed randomized clinical trials are necessary to confirm the therapeutic benefits of this genus in clinical settings.


Asunto(s)
Evodia , Fitoterapia , Animales , Humanos , Medicina Tradicional , Fitoquímicos/farmacología , Fitoquímicos/uso terapéutico , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico
20.
Am J Chin Med ; 46(4): 707-737, 2018.
Artículo en Inglés | MEDLINE | ID: mdl-29737210

RESUMEN

Traditional Chinese medicine (TCM) has a long history and been widely used in prevention and treatment of epilepsy in China. This paper is intended to review the advances in the active anticonvulsant compounds isolated from herbs in the prescription of TCM in the treatment of epilepsy. These compounds were introduced with the details including classification, CAS number specific structure and druggability data. Meanwhile, much of the research in these compounds in the last two decades has shown that they exhibited favorable pharmacological properties in treatment of epilepsy both in in vivo and in vitro models. In addition, in this present review, the evaluation of the effects of the anticonvulsant classical TCM prescriptions is discussed. According to these rewarding pharmacological effects and chemical substances, the prescription of TCM herbs could be an effective therapeutic strategy for epilepsy patients, and also could be a promising source for the development of new drugs.


Asunto(s)
Anticonvulsivantes/aislamiento & purificación , Medicamentos Herbarios Chinos/química , Epilepsia/tratamiento farmacológico , Fitoterapia , Alcaloides/química , Alcaloides/aislamiento & purificación , Anticonvulsivantes/química , Anticonvulsivantes/farmacología , Anticonvulsivantes/uso terapéutico , Combinación de Medicamentos , Epilepsia/prevención & control , Flavonoides/química , Flavonoides/aislamiento & purificación , Humanos , Conformación Molecular , Fenoles/química , Fenoles/aislamiento & purificación , PubMed , Triterpenos/química , Triterpenos/aislamiento & purificación
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