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1.
Front Neurosci ; 18: 1349059, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38560046

RESUMEN

Introduction: Acupuncture analgesia (AA) is widely used in clinical practice. The autonomic nervous system (ANS) may be an important pathway for acupuncture signal transduction. However, real-time changes in autonomic function during AA and the effect of "needle sensation" remain unclear. Methods: We established a human pain model in healthy adults and randomly assigned 128 participants to the model, sham acupuncture, and acupuncture groups in a 1:1:2 ratio. Heart rate variability (HRV), including total power (TP), low-frequency power (LF), high-frequency power (HF), ratio of LF to HF (LF/HF), standard deviation of the normal-normal intervals (SDNN), and root mean square of successive interval differences (RMSSD), were used to assess autonomic function. The visual analog scale (VAS) and efficiency were used to assess the analgesic effect of acupuncture. The Massachusetts General Hospital acupuncture sensation scale (MASS) was used to indicate the intensity of the needle sensation. Anxiety levels were also measured. Finally, the correlation of MASS with HRV, VAS, and anxiety levels was analyzed. Results: VAS decreased after 10 min of needling and 5 min after needle withdrawal in the acupuncture group compared with those in the model group (p = 0.038, p = 0.020). The efficacy rates were 82.0, 50.0, and 61.3% in the acupuncture, model, and sham groups, respectively. These represent significant differences between the acupuncture group and the model and sham acupuncture groups (p < 0.001 in each case). No differences were observed between the model and sham acupuncture groups. HF, TP, SDNN, and RMSSD were all increased in the acupuncture group compared with those in the model group (p = 0.045, p = 0.041, p = 0.002, p = 0.006, respectively). No differences were observed in the sham acupuncture group compared to the model group (p = 0.632, p = 0.542, p = 0.093, p = 0.222, respectively). The LF and LF/HF did not differ among all three groups. A positive correlation was observed between MASS and RMSSD2, LF2, RMSSD4, TP4, VAS5, and anxiety levels. Conclusion: AA was associated with enhanced vagal activity. The intensity of needle sensation was positively correlated with vagal and sympathetic nerve activities. Acupuncture is an effective means of regulating autonomic function, and needle sensation may be an important modulator.

2.
Molecules ; 29(4)2024 Feb 08.
Artículo en Inglés | MEDLINE | ID: mdl-38398534

RESUMEN

Vaccinium dunalianum leaf buds make one of the most commonly used herbal teas of the Yi people in China, which is used to treat articular rheumatism, relax tendons, and stimulates blood circulation in the body. In addition, 6'-O-caffeoylarbutin (CA) is a standardized extract of V. dunalianum, which has been found in dried leaf buds, reaching levels of up to 31.76%. Because of the uncommon phenomenon, it is suggested that CA may have a potential therapeutic role in hyperlipidemia and thrombosis. This study was designed to study the efficacy of CA on treating hyperlipidemia and thrombosis and the possible mechanisms behind these effects. Hyperlipidemia and thrombosis zebrafish models were treated with CA to observe variations of the integrated optical density within the vessels and the intensity of erythrocyte staining within the hearts. The possible mechanisms were explored using network pharmacology and molecular docking. The results demonstrate that CA exhibits an excellent hypolipidemic effect on zebrafish at concentrations ranging from 3.0 to 30.0 µg/mL and shows thrombosis inhibitory activity in zebrafish at a concentration of 30.0 µg/mL, with an inhibition rate of 44%. Moreover, network pharmacological research shows that MMP9, RELA, MMP2, PRKCA, HSP90AA1, and APP are major targets of CA for therapy of hyperlipidemia and thrombosis, and may relate to pathways in cancer, chemical carcinogenesis-receptor activation, estrogen signaling pathway, and the AGE-RAGE signaling pathway in diabetic complications.


Asunto(s)
Arbutina , Ácidos Cafeicos , Medicamentos Herbarios Chinos , Hiperlipidemias , Trombosis , Animales , Arbutina/análogos & derivados , Fibrinolíticos/farmacología , Hiperlipidemias/tratamiento farmacológico , Simulación del Acoplamiento Molecular , Farmacología en Red , Trombosis/tratamiento farmacológico , Pez Cebra
3.
Int J Mol Sci ; 25(2)2024 Jan 12.
Artículo en Inglés | MEDLINE | ID: mdl-38256044

RESUMEN

Tyrosinase is vital in fruit and vegetable browning and melanin synthesis, crucial for food preservation and pharmaceuticals. We investigated 6'-O-caffeoylarbutin's inhibition, safety, and preservation on tyrosinase. Using HPLC, we analyzed its effect on mushroom tyrosinase and confirmed reversible competitive inhibition. UV_vis and fluorescence spectroscopy revealed a stable complex formation with specific binding, causing enzyme conformational changes. Molecular docking and simulations highlighted strong binding, enabled by hydrogen bonds and hydrophobic interactions. Cellular tests showed growth reduction of A375 cells with mild HaCaT cell toxicity, indicating favorable safety. Animal experiments demonstrated slight toxicity within safe doses. Preservation trials on apple juice showcased 6'-O-caffeoylarbutin's potential in reducing browning. In essence, this study reveals intricate mechanisms and applications of 6'-O-caffeoylarbutin as an effective tyrosinase inhibitor, emphasizing its importance in food preservation and pharmaceuticals. Our research enhances understanding in this field, laying a solid foundation for future exploration.


Asunto(s)
Arbutina/análogos & derivados , Ácidos Cafeicos , Monofenol Monooxigenasa , , Animales , Simulación del Acoplamiento Molecular , Preparaciones Farmacéuticas
4.
Acupunct Med ; 42(1): 14-22, 2024 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-37800350

RESUMEN

BACKGROUND: Postoperative gastrointestinal dysfunction (PGD) is one of the most common complications among patients who have undergone thoracic surgery. Acupuncture has long been used in traditional Chinese medicine to treat gastrointestinal diseases and has shown benefit as an alternative therapy for the management of digestive ailments. This study aimed to explore the therapeutic effectiveness of acupuncture as a means to aid postoperative recovery of gastrointestinal function in patients undergoing thoracoscopic surgery. METHODS: In total, 112 patients aged 18-70 years undergoing thoracoscopic surgery between 15 June 2022 and 30 August 2022 were randomized into two groups. Patients in the acupuncture group (AG) first received acupuncture treatment 4 h after surgery, and treatment was repeated at 24 and 48 h. Patients in the control group (CG) did not receive any acupuncture treatment. Both groups received the same anesthetic protocol. Ultrasound-guided thoracic paravertebral block (TPVB) was performed in the paravertebral spaces between T4 and T5 with administration of 20 mL of 0.33% ropivacaine. All patients received patient-controlled intravenous analgesia (PCIA) after surgery. RESULTS: Median time to first flatus [interquartile range] in the AG was significantly less than in the CG (23.25 [18.13, 29.75] vs 30.75 [24.13, 45.38] h, p < 0.001). Time to first fluid intake after surgery was significantly less in the AG, as compared with the CG (4 [3, 7] vs 6.5 [4.13, 10.75] h, p = 0.003). Static pain, measured by visual analog scale (VAS) score, was significantly different on the third day after surgery (p = 0.018). Dynamic pain VAS scores were lower in the AG versus CG on the first three postoperative days (p = 0.014, 0.003 and 0.041, respectively). CONCLUSION: Addition of acupuncture appeared to improve recovery of postoperative gastrointestinal function and alleviate posteoperative pain in patients undergoing thoracoscopic surgery. Acupuncture may represent a feasible strategy for the prevention of PGD occurrence. TRIAL REGISTRATION NUMBER: ChiCTR2200060888 (Chinese Clinical Trial Registry).


Asunto(s)
Terapia por Acupuntura , Enfermedades Gastrointestinales , Humanos , Dolor Postoperatorio/prevención & control , Dolor Postoperatorio/tratamiento farmacológico , Estudios Prospectivos , Ropivacaína/uso terapéutico , Toracoscopía/efectos adversos , Toracoscopía/métodos
5.
Fitoterapia ; 170: 105657, 2023 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-37604244

RESUMEN

Four new phenolic compounds, including two naphthalenes, musizin-8-O-ß-D-(6'-O-malonyl-3''-methoxy)glucopyranoside (1) and 2-acetyl-3-methyl-1,4-naphtho-quinone-8-O-ß-D-glucopyranoside (2), one chromone, (2'R)-7-hydroxy-2-(2'-hydroxypropyl)-5-methyl acetate chromone (3), and one xanthone, 2,8-dimethyl-3,6-dihydroxyxanthone (4) were isolated from the roots of Rumex dentatus L. (Polygonaceae). In addition, five known including four naphthalenes (5-8) and one chromone (9) were also obtained. Their structures were determined by means of extensive spectroscopic analysis and acidic hydrolysis. Compound 1 showed moderate antifungal activity against Epidermophyton floccosum, with inhibitory rate of 39.539 ± 0.412% at a concentration of 100 µM.


Asunto(s)
Polygonaceae , Rumex , Estructura Molecular , Polygonaceae/química , Raíces de Plantas/química , Naftalenos
6.
RSC Adv ; 13(16): 11037-11043, 2023 Apr 03.
Artículo en Inglés | MEDLINE | ID: mdl-37033442

RESUMEN

Panax notoginseng (PN) is a well-known traditional Chinese medicine, with dammarane-type triterpenoid saponins characterized as major component and active ingredients, together with amino acids, flavonoids, polysaccharides, and polyacetylenes. The roots of PN are susceptible to root rot disease, which causes a huge loss and changes in the chemical components of this precious resource. In this study, sub-fractions of rot PN root extracts were preliminarily found to have admirable cytotoxicity on two human cancer cells. Further bioassay-guided isolation discovered nine new non-triterpenoids, including two novel N-methylacetamido-1-oxotetrahydropyrimidine alkaloids (1, 2), five 2H-furanones or 2H-pyranones (3-7), and two polyacetylenic alcohols (8, 9). Their structures were illuminated by extensive spectroscopic data, calculated ECD, and X-ray diffraction analysis. Among them, 3-7 were considered to be transformed from panaxatriol through the intermediates (8, 9). The new alkaloids (1, 2) displayed noteworthy cytotoxicity against five human cancer cells with IC50 values ranging from 14 to 24 µM. In silico target prediction and molecular docking studies showed that 1 and 2 may interact with EGFR, and were verified by the experimental inhibitory effect on EGFR tyrosine kinase.

7.
Contrast Media Mol Imaging ; 2022: 7511345, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36072628

RESUMEN

Background: Recently, inflammation has become a major threat to human health. Studies have confirmed that some Chinese traditional medicine ingredients may effectively interfere with the expression of inflammatory mediators through epigenetic modification, showing a great potential of the application. Objective: To investigate the role of the PPAR/DNMT3A pathway in the reversal of galangin-mediated inflammatory lung injury, promote the development of new anti-inflammatory drugs, reduce the side effects of chemical synthetic drugs on the body, and prove the effectiveness and safety of galangin in inhibiting inflammatory response and injury. Methods: 120 rats were randomly divided into 6 groups: (Group 1) LPS group; (Group 2) LPS + galangin group; (Group 3) LPS + galangin + GW9662 group; (Group 4) LPS + galangin + DNMT3A siRNA group; (Group 5) LPS + galangin + siRNA negative group; (Group 6) control group. The model of inflammatory lung injury was established by intrathecal instillation of LPS in the first five groups and NS in the control group. SD survival rate was recorded every 24 hours after modeling, lasting for 168 hours. The lung tissues were taken 168 hours after the establishment of the model. The pathological morphology of lung tissue was observed after the staining under the light microscope, and the lung dry/wet weight ratio was calculated after drying. After NS was perfused into lung tissue, the lavage fluid was collected and the levels of IL-6 and TNF-a were measured by ELISA. The contents of PPAR, DNMT3A, phosphorylated p65, and ERK in monocytes were detected by the WB method, and the binding contents of p65 and AP-1 in the promoter regions of IL-6 and TNF-a genes were detected by the Chip-qPCR method. Results: Intraperitoneal injection of galangin could inhibit the synthesis of alveolar inflammatory factors (TFs) in the SD model of lung injury induced by LPS, reduce the degree of pathological injury of lung tissue, and improve the survival rate of the SD model. GW9662 can completely reverse the protective effect, while DNMT3A interference can only partially block its protective effect. In addition, galangin could significantly inhibit the LPS-induced expression of p65 and AP-1 in alveolar monocytes and their binding content in the promoter region of inflammatory genes by activating PPAR/DNMT3A pathway. GW9662 could completely reverse the inhibitory effect of galangin. DNMT3A interference could restore the binding content of transcription factors at the promoter of the inflammatory gene but had no significant effect on its synthesis. Conclusion: Galangin can interfere with the binding of transcription factors to inflammatory gene promoters through the methylation modification induced by PPAR/DNMT3A pathway, so as to inhibit the synthesis of inflammatory molecules and reverse inflammatory lung injury.


Asunto(s)
Lesión Pulmonar Aguda , Flavonoides , Lesión Pulmonar Aguda/inducido químicamente , Lesión Pulmonar Aguda/tratamiento farmacológico , Lesión Pulmonar Aguda/metabolismo , Animales , Flavonoides/efectos adversos , Interleucina-6/metabolismo , Lipopolisacáridos , Metilación , Receptores Activados del Proliferador del Peroxisoma/metabolismo , ARN Interferente Pequeño/metabolismo , Ratas , Factor de Transcripción AP-1/metabolismo
8.
Nat Prod Bioprospect ; 12(1): 21, 2022 Jun 16.
Artículo en Inglés | MEDLINE | ID: mdl-35710954

RESUMEN

Rumex L., a genus in Polygonaceae family with about 200 species, is growing widely around the world. Some Rumex species, called "sorrel" or "dock", have been used as food application and treatment of skin diseases and hemostasis after trauma by the local people of its growing areas for centuries. To date, 29 Rumex species have been studied to contain about 268 substances, including anthraquinones, flavonoids, naphthalenes, stilbenes, diterpene alkaloids, terpenes, lignans, and tannins. Crude extract of Rumex spp. and the pure isolates displayed various bioactivities, such as antibacterial, anti-inflammatory, antitumor, antioxidant, cardiovascular protection and antiaging activities. Rumex species have important potential to become a clinical medicinal source in future. This review covers research articles from 1900 to 2022, fetched from SciFinder, Web of Science, ResearchGate, CNKI and Google Scholar, using "Rumex" as a search term ("all fields") with no specific time frame set for the search. Thirty-five Rumex species were selected and summarized on their geographical distribution, edible parts, traditional uses, chemical research and pharmacological properties.

9.
J Healthc Eng ; 2022: 5961267, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-35345656

RESUMEN

During the training process, the aerobics athletes gradually increase their technical movements, the appreciation of the movements has been gradually improved, and the injuries of the athletes themselves have also gradually become serious. Based on CT image analysis, we study the protective effect of amino acids on aerobics athletes' muscle injury after endurance exercise. There are three major substance metabolism disorders in patients with muscle sclerosis, which are mainly manifested as decreased glucose tolerance and insulin resistance. Some patients develop muscle-derived diabetes. At the same time, the synthesis of lipids such as cholesterol and apolipoproteins decreases, the production of ketone bodies increases and the body uses more ketones for energy. The BCAA/AAA factor refers to the branched-chain amino acid/aromatic amino acid (BCAA/AAA) value. In amino acid metabolism, plasma albumin decreased significantly, the ratio of amino acids was unbalanced, and BCAA/AAA decreased, which was more likely to induce muscular encephalopathy. Using computer tomography (CT) to study the protective effect of amino acids on muscle injury, 32 aerobics athletes were randomly divided into an intervention group (Ig) and a control group (CG), each with 16 people. After 64-slice spiral CT scanning of muscles and three-dimensional reconstruction, the intervention group and the control group participated in aerobic endurance training 3 weeks in advance to establish a muscle microinjury model. The intervention group took the preprepared BCAA, while the control group did not take it. After three weeks of training, there will be one hour and three hours of aerobics competition. We need to detect changes in blood glucose (BS), creatine kinase (SCK), lactate dehydrogenase (LD), alanine (ALA), and alanine aminotransferase (AA) before and after exercise and 1 hour after exercise and record AVS athletes' pain analysis table. We successfully established the muscle injury model, letting all athletes' VAS score in 6-8 points; after 1 hour of exercise, the measurement results were the same as those of 2 hours. Therefore, after endurance training, the blood glucose content of the intervention group gradually decreased and returned to the original level after 2 hours of exercise, while the control group was lower than the level of exercise after 2 hours of exercise; the content of alanine in the two groups decreased more after 2 hours of exercise; the results of serum creatine kinase in the intervention group were higher than those in the control group after exercise. In the intervention group, lactate dehydrogenase increased rapidly at 2 hours after exercise; the alanine aminotransferase in the intervention group increased after exercise, but there was no significant change in the control group. It is also concluded that the longer the exercise time and the more energy consumption, the more effective the branched-chain amino acids supplement will be. The obtained imaging data can provide a more intuitive and accurate basis for the scientific selection of athletes, and amino acids can promote the synthesis of hormones, accelerate the synthesis of proteins and other products, reduce the content of creatine kinase in the blood, and protect the rapid recovery of muscle damage.


Asunto(s)
Aminoácidos , Glucemia , Alanina/metabolismo , Alanina/farmacología , Alanina Transaminasa , Aminoácidos/metabolismo , Aminoácidos de Cadena Ramificada/metabolismo , Aminoácidos de Cadena Ramificada/farmacología , Atletas , Computadores , Creatina Quinasa/metabolismo , Creatina Quinasa/farmacología , Humanos , Lactato Deshidrogenasas/metabolismo , Músculo Esquelético/diagnóstico por imagen , Músculos/metabolismo , Tomografía , Tomografía Computarizada por Rayos X
10.
Fitoterapia ; 157: 105133, 2022 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-35114336

RESUMEN

Six diterpenoids including three ent-kauranes (1-2, 4) and three cleistanthanes (3, 5-6) were isolated from the roots and stems of Phyllanthus acidus (L.) Skeels. Of them, (16S)-ent-16,17,18-tri-hydroxy-19-nor-kaur-4-en-3-one (1), phyllanthone A (2), and 6-hydroxycleistanthol (3) are new compounds, while the ent-kaurane diterpenoids were reported from the titled plant for the first time. Their structures were elucidated on the basis of the extensive spectroscopic analyses. Compounds 2 and 4-6 displayed cytotoxic potential with IC50 values ranging from 1.96 to 29.15 µM. They also showed moderate anti-inflammatory activities (IC50 = 6.30-12.05 µM). Particularly, the new ent-kaurane 2 displayed cytotoxic potential against HL-60 (IC50 = 2.00 µM) and MCF-7 (IC50 = 3.55 µM) cells, and anti-inflammatory activity (IC50 = 6.47 µM).


Asunto(s)
Diterpenos de Tipo Kaurano/toxicidad , Diterpenos/toxicidad , Phyllanthus/química , Extractos Vegetales/toxicidad , Alcaloides/química , Alcaloides/aislamiento & purificación , Alcaloides/toxicidad , Línea Celular Tumoral , Diterpenos/química , Diterpenos de Tipo Kaurano/química , Humanos , Concentración 50 Inhibidora , Espectroscopía de Resonancia Magnética , Estructura Molecular , Extractos Vegetales/síntesis química , Raíces de Plantas/química , Tallos de la Planta/química
11.
Nat Prod Res ; 36(20): 5241-5246, 2022 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-34074201

RESUMEN

Phyllaciduloids E (1) and F (2), two new cleistanthane diterpenoids, were isolated from the leaves of Phyllanthus acidus (L.) Skeels (Phyllanthaceae). Their planar structures were established by spectroscopic analysis and comparison with literature values. The relative configurations of phyllaciduloids E and F were confirmed by DFT-NMR chemical shift calculations and subsequent CP3 probability methods. Phyllaciduloids E and F were evaluated for their cytotoxicity. However, no significant activities were detected at concentrations up to 40 µM.[Formula: see text].


Asunto(s)
Diterpenos , Phyllanthus , Diterpenos/análisis , Diterpenos/farmacología , Estructura Molecular , Phyllanthus/química , Extractos Vegetales/análisis , Hojas de la Planta/química
12.
Food Chem ; 370: 131326, 2022 Feb 15.
Artículo en Inglés | MEDLINE | ID: mdl-34656020

RESUMEN

Theanaphthoquinone (TNQ) is the initial and main oxidation product of theaflavin, a representative black tea pigment. Nevertheless, TNQ is virtually undetected in the high-performance liquid chromatography analysis of black tea leaves using photodiode array detection. To elucidate the degradation mechanism of theaflavin in the black tea production process, this study investigated the reaction of TNQ with epigallocatechin-3-O-gallate (EGCg), which is the most abundant polyphenol in tea leaves. In citrate-phosphate buffer solution at pH 6 and room temperature, TNQ reacted nonenzymatically with EGCg to afford three products, whose structures were determined on the basis of spectroscopic data. The results indicated that the double bond of the ortho-naphthoquinone moiety in TNQ reacted with the autoxidation product of EGCg. This study demonstrates novel reactions occurring in the process of theaflavin degradation, which might be involved in the formation of thearubigins, the major black tea pigments composing oligomeric catechin oxidation products.


Asunto(s)
Biflavonoides , Catequina , Catequina/análogos & derivados ,
13.
Bioorg Chem ; 114: 105125, 2021 09.
Artículo en Inglés | MEDLINE | ID: mdl-34217976

RESUMEN

The young leaves of Phyllanthus acidus (Euphorbiaceae) are commonly used as edible vegetables in Indonesia, Thailand, and India, and their water infusions as dieting aids for people trying to remain slim. However, it is regarded as a poisonous plant in Malaya, and current researches are insufficient to provide a conclusion on its toxicity and safety under large doses. In this study, we firstly found that the refined nonpolar extracts of P. acidus leaves showed significant cytotoxic effect against BEAS-2B and L02 normal cell lines with IC50 values of 2.15 and 1.64 mg/mL, respectively. Further bioactivity-guided isolation produced four new rare dichapetalins (pacidusins A-D) from the most active fraction. Their structures including absolute configurations were elucidated by extensive spectroscopic data and X-ray diffraction analysis. All the isolated dichapetalins exhibited moderate cytotoxicity against, BEAS-2B and L02 normal cell lines with IC50 values ranging from 12.44 to 22.55 µM, as well as five human cancer cell lines with IC50 values ranging from 3.38 to 22.38 µM. Furthermore, the content of the main dichapetalins in the leaves were determined by analytical HPLC, which showed that the leaves contained a very high amount of the four isolated dichapetalins with a total yield of 0.488 mg/g of dry plant material. These toxic dichapetalins may lead to adverse health effects in higher doses. Our findings indicate that the dichapetalin containing leaves may not be suitable for consumption in large quantities as food, but demonstrate their potency as anti-cancer agents for new drug discovery.


Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Phyllanthus/química , Extractos Vegetales/farmacología , Hojas de la Planta/química , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Línea Celular , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Estructura Molecular , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Relación Estructura-Actividad
14.
Hortic Res ; 8(1): 121, 2021 Jun 01.
Artículo en Inglés | MEDLINE | ID: mdl-34059652

RESUMEN

Coptis chinensis Franch, a perennial herb, is mainly distributed in southeastern China. The rhizome of C. chinensis has been used as a traditional medicine for more than 2000 years in China and many other Asian countries. The pharmacological activities of C. chinensis have been validated by research. Here, we present a de novo high-quality genome of C. chinensis with a chromosome-level genome of ~958.20 Mb, a contig N50 of 1.58 Mb, and a scaffold N50 of 4.53 Mb. We found that the relatively large genome size of C. chinensis was caused by the amplification of long terminal repeat (LTR) retrotransposons. In addition, a whole-genome duplication event in ancestral Ranunculales was discovered. Comparative genomic analysis revealed that the tyrosine decarboxylase (TYDC) and (S)-norcoclaurine synthase (NCS) genes were expanded and that the aspartate aminotransferase gene (ASP5) was positively selected in the berberine metabolic pathway. Expression level and HPLC analyses showed that the berberine content was highest in the roots of C. chinensis in the third and fourth years. The chromosome-level reference genome of C. chinensis provides important genomic data for molecular-assisted breeding and active ingredient biosynthesis.

15.
J Ethnopharmacol ; 275: 114135, 2021 Jul 15.
Artículo en Inglés | MEDLINE | ID: mdl-33892063

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Terminalia chebula (TC), a well-known Indian Ayurvedic medicine introduced into China in the Sui and Tang Dynasties, has been recorded and used medicinally as Fructus Chebulae, together with its variety tomentella (TCT) in the Chinese Pharmacopoeia. They have been also used commonly for the treatment of diabetes mellitus by Tibetan medicine. AIM OF THE STUDY: To investigate the main bioactive and therapeutic principles in the fruits of TCT, based on the extensive evaluation of their anti-inflammatory and hypoglycemic activities. MATERIALS AND METHODS: The TCT fresh fruits were analyzed by HPLC and separated further by column chromatography and preparative HPLC. The isolated compounds were identified by extensive spectroscopic analyses, including 1D/2D NMR, MS, UV, IR and ECD. Anti-inflammatory activity was evaluated by inhibition of NO production in RAW264.7 cells. The specific iNOS (PDB ID: 3E7G) structure was prepared by Discovery Studio 4.0, and the molecular docking simulation was performed on GOLD (version 5.2.2). Hypoglycemic activity was measured using the substrate solution of 4-nitrophenyl-α-d-glucopyranoside enzyme and buffer solution. RESULTS: The HPLC analysis method of polyphenols in the fruits of TCT was established, and 13 main chromatographic peaks were identified, including six hydrolyzable tannins (2, 4-7, 10-11), three simple phenols (12-14), and one oleanane pentacyclic triterpene, arjungenin. Extensive chromatographic separation of TCT fresh fruits yielded 14 compounds, including one new natural hydrolyzable tannin, 2,3-(S)-HHDP-6-O-galloyl-d-glucose (1). The known compounds were identified as 10 hydrolyzable tannins (2-11) and three simple phenols (12-14). Compounds 10 (IC50 = 36.43 ± 0.21 µM), 11 (IC50 = 42.28 ± 0.09 µM) displayed stronger NO inhibitory activity than the positive control L-NMMA (IC50 = 42.34 ± 0.66 µM), while 2, 4, and 9 showed moderate inhibitory activity against NO production. Further molecular docking simulation of specific iNOS on 10 and 11, as well as five previously isolated lignans 15-19 showed that there were no obvious rules between docking results and the in vitro NO inhibitory activity for hydrolyzable tannins (10 and 11), while the mechanism of anti-inflammatory activity for lignans was related to the substitution of conjugated aldehyde groups. Moreover, most of the hydrolyzable tannins (1-2, 4-5, 9-11) and simple phenol (12) displayed stronger inhibitory effects on α-glucosidase than the positive control, quercetin (IC50 = 6.118 ± 0.071 µM), with IC50 values ranging from 0.079 to 16.494 µM. Among these bioactive isolates, the hydrolyzable tannins 2, 4-5, and 9-11, and simple phenol 12 are major chemical components in TCT fruit. CONCLUSIONS: The results showed that lignans and hydrolyzed tannins are the main active ingredients of TCT fruits, responsible for the traditional treatment of sore throat and cough. Moreover, hydrolyzed tannins and simple phenolic compounds with potential hypoglycemic activity are closely related to the ethno-pharmacological uses of TCT fruits on diabetes in Tibetan medicine.


Asunto(s)
Antiinflamatorios/farmacología , Hipoglucemiantes/farmacología , Fenoles/farmacología , Extractos Vegetales/farmacología , Terminalia/química , Animales , Antiinflamatorios/análisis , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Frutas/química , Inhibidores de Glicósido Hidrolasas/farmacología , Taninos Hidrolizables/análisis , Taninos Hidrolizables/química , Taninos Hidrolizables/farmacología , Hipoglucemiantes/análisis , Hipoglucemiantes/química , Hipoglucemiantes/aislamiento & purificación , Técnicas In Vitro , Lignanos/análisis , Lignanos/química , Lignanos/farmacología , Ratones , Simulación del Acoplamiento Molecular , Óxido Nítrico Sintasa de Tipo II/antagonistas & inhibidores , Óxido Nítrico Sintasa de Tipo II/química , Fenoles/análisis , Fenoles/química , Fenoles/aislamiento & purificación , Extractos Vegetales/análisis , Extractos Vegetales/química , Células RAW 264.7 , Triterpenos/análisis , Triterpenos/química , Triterpenos/farmacología , alfa-Glucosidasas/metabolismo
16.
Phytochemistry ; 184: 112656, 2021 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-33524854

RESUMEN

Three previously undescribed pyridyl-steroidal glycoalkaloids, solanindiosides A‒C, one rare 23S,26R-hydroxylated spirostanoid saponin, and two steroidal alkaloid aglycones, solanindins A and B, derived from the acid hydrolysis of solanindiosides A‒C, were isolated from the fruits of Solanum violaceum, together with five known analogues, including two rare steroidal glycosides, two lignans and a diterpene. Structurally, they comprise a 16ß-methoxy-23-deoxy-22,26-epimino-cholest-type skeleton moiety, and a 16ß-methoxy-3,23-dideoxy-22,26-epimino-cholest-3,5-dien derivative. The hitherto undescribed structures were established on the basis of extensive spectroscopic analyses. Configurations of sugar moieties were resolved by chemical derivations. Solanindiosides A‒C, (22R,23S,25R,26R)-spirost-5-ene-3ß,23,26-triol3-O-ß-d-xylopyranosyl-(1→3)-ß-d-glucopyranoside, solanindins A and B, and (1S,2S)-1-(4-hydroxy-3-methoxyphenyl)-2-[2-methoxy-4-[(2S,3R,4R)-tetrahydro-4-[(4-hydroxy-3-methoxyphenyl)methyl]-3-(hydroxymethyl)-2-furanyl]phenoxy]-1,3-propanediol were evaluated for their cytotoxic and antibacterial activities. (1S,2S)-1-(4-hydroxy-3-methoxyphenyl)-2-[2-methoxy-4-[(2S,3R,4R)-tetrahydro-4-[(4-hydroxy-3-methoxyphenyl)methyl]-3-(hydroxymethyl)-2-furanyl]phenoxy]-1,3-propanediol showed the most potent cytotoxic activity against MCF-7 cells (IC50 = 4.386 ± 0.098 µM), while solanindin B displayed some inhibitory effects against Staphylococcus aureus Rosenbach with MIC50 value of 37.32 ± 0.793 µM. In addition, (1S,2S)-1-(4-hydroxy-3-methoxyphenyl)-2-[2-methoxy-4-[(2S,3R,4R)-tetrahydro-4-[(4-hydroxy-3-methoxyphenyl)methyl]-3-(hydroxymethyl)-2-furanyl]phenoxy]-1,3-propanediol induced dose dependent apoptosis effect in MCF-7 cells.


Asunto(s)
Saponinas , Solanum , Frutas , Glicósidos , Saponinas/farmacología , Esteroides
17.
Nat Prod Res ; 35(21): 3540-3547, 2021 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-31979989

RESUMEN

A novel highly oxygenated norbisabolane sesquiterpene, namely phyllanthacidoid U (1), along with nine known sesquiterpenes (2-10) was isolated from the roots and stems of Phyllanthus acidus (L.) Skeels (Phyllanthaceae), collected from Xishuangbanna, Yunnan province, China. Their structures were elucidated by means of extensive spectroscopic analysis and by comparison of their data with reported values in literatures. Instead of the C-13 ester O-glycosyl found mostly in the titled plant growing in Thailand, compound 1 possessed a rare N-ß-glucosamine-2-N-acetate moiety linked directly to the carbonyl at C-13 through an amido bond. Moreover, the acyl group at C-10 in 1 was (Z)-2-(2-hydroxyethyl)-pent-2-enedioyl group, instead of benzoic or p-hydroxybenzoic moieties found commonly in the reported norbisabolane sesquiterpenes. The known sesquiterpene 5 displayed stronger anti hepatitis B virus (HBV) activity with IC50 values of 1.69 ± 0.22 and 2.79 ± 0.69 µM towards HBV surface antigen (HBsAg) and HBV excreted antigen (HBeAg) secretion, respectively.


Asunto(s)
Phyllanthus , Sesquiterpenos , China , Antígenos e de la Hepatitis B , Virus de la Hepatitis B , Estructura Molecular , Extractos Vegetales
18.
Fitoterapia ; 148: 104793, 2021 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-33276011

RESUMEN

Phytochemical investigation on the nonpolar extracts of P. acidus leaves afforded three new cleistanthane diterpenoids, named phyllanacidins A-C (1-3), in addition to three known ones (4-6). Among them, compounds 2 and 3 represent the first examples of 17-nor cleistanthane diterpenoids. Their structures including absolute configurations were elucidated on the basis of extensive spectroscopic data and single crystal X-ray diffraction analysis. All the isolated cleistanthane diterpenoids were evaluated for their cytotoxic activities against five human cancer cell lines. Compounds 4-6 exhibited moderate cytotoxicity with IC50 values ranging from 16.11 to 30.82 µM.


Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Diterpenos/farmacología , Phyllanthus/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Línea Celular Tumoral , China , Diterpenos/aislamiento & purificación , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Estructura Molecular , Fitoquímicos/aislamiento & purificación , Fitoquímicos/farmacología , Hojas de la Planta/química
19.
Nurs Open ; 7(5): 1536-1543, 2020 09.
Artículo en Inglés | MEDLINE | ID: mdl-32802374

RESUMEN

Aim: This study aimed to investigate the current situation of the spiritual health of maintenance haemodialysis (MHD) patients in China and analyse the influencing factors. Methods: A total of 418 patients who underwent maintenance haemodialysis in three grade A tertiary hospitals were selected. The influencing factors were evaluated with demographic questionnaire, the Functional Assessment of Chronic Illness Therapy-Spiritual Well-Being (FACIT-Sp-12), Family APGAR Index, Herth Hope Index (HHI) and Acceptance of Illness Scale (AIS). Results: Spiritual health was positively correlated with the HHI, Family APGAR and AIS scores. Nationality, HHI score, Family APGAR score and AIS score were independent influencing factors of spiritual health. MHD patients had a moderate level of spiritual health. Nationality, hope, family function and acceptance of illness were significant predictors of spiritual health. Patients who have higher hope levels, better family functioning and better illness acceptance may maintain better spiritual health.


Asunto(s)
Diálisis Renal , Espiritualidad , China/epidemiología , Estudios Transversales , Humanos , Encuestas y Cuestionarios
20.
J Agric Food Chem ; 68(30): 7955-7963, 2020 Jul 29.
Artículo en Inglés | MEDLINE | ID: mdl-32628847

RESUMEN

As a subgroup of flavoalkaloids, N-ethyl-2-pyrrolidinone substituted flavan-3-ols are reported to possess various biological activities that may play important roles in the beneficial healthcare functions of tea. The HPLC and LC-MS analyses showed the existence of N-ethyl-2-pyrrolidinone substituted flavan-3-ols in 'Jin-Ya', which is a Yunnan black tea produced only from the buds of the tea plant Camellia sinensis var. assamica. Further phytochemical study on this precious black tea led to the identification of 8 flavoalkaloids, 1-8, along with 11 known flavan-3-ols (9-14) and flavonol glycosides (15-19). The new compounds, (-)-6-(5″S)-N-ethyl-2-pyrrolidinone-epiafzelechin (1), (-)-8-(5″R)-N-ethyl-2-pyrrolidinone-epiafzelechin-3-O-gallate (2a), and (-)-8-(5″S)-N-ethyl-2-pyrrolidinone-epiafzelechin-3-O-gallate (2b), were identified based on extensive spectroscopic analysis. Flavoalkaloids 2-6 showed inhibitory activity on α-glucosidase with IC50 values ranging from 2.09 to 8.47 µM, compared to those of quercetin and acarbose (IC50 = 6.87 and 228.9 µM, respectively). Moreover, compounds 2, 3, and 6 displayed an inhibitory effect on acetyl-cholinesterase with IC50 values of 14.23, 33.79, and 34.82 µM, respectively, compared to tacrine (IC50 = 0.223 µM).


Asunto(s)
Alcaloides/química , Camellia sinensis/química , Inhibidores Enzimáticos/química , Extractos Vegetales/química , Acetilcolinesterasa/química , China , Glicósidos/química , Humanos , Cinética , Estructura Molecular , Hojas de la Planta/química , alfa-Glucosidasas/química
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