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1.
Biomed Chromatogr ; 38(2): e5782, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-38016814

RESUMO

Natural medicines play a crucial role in clinical drug applications, serving as a primary traditional Chinese medicine for the clinical treatment of liver fibrosis. Understanding the in vivo metabolic process of the Fuzheng Huayu (FZHY) formula is essential for delving into its material basis and mechanism. In recent years, there has been a growing body of research focused on the mechanisms and component analysis of FZHY. This study aimed to examine the pharmacokinetics of FZHY in healthy volunteers following oral administration. Blood samples were collected at designated time intervals after the oral intake of 9.6-g FZHY tablets. A UHPLC-Q/Exactive method was developed to assess the plasma concentrations of five components post-FZHY ingestion. The peak time for all components occurred within 10 min. The peak concentration (Cmax ) values for amygdalin, schisandrin, and schisandrin A ranged from 3.47 to 28.80 ng/mL, with corresponding AUC(0-t) values ranging from 10.63 to 103.20 ng h/mL. For schisandrin B and prunasin, Cmax values were in the range of 86.52 to 229.10 ng/mL, and their AUC(0-t) values ranged from 375.26 to 1875.54 ng h/mL, indicating significant exposure within the body. These findings demonstrate that the developed method enables rapid and accurate detection and quantification of the five components in FZHY, offering a valuable reference for its clinical study.


Assuntos
Medicamentos de Ervas Chinesas , Humanos , Medicamentos de Ervas Chinesas/farmacocinética , Cirrose Hepática/tratamento farmacológico , Cirrose Hepática/metabolismo , Medicina Tradicional Chinesa/métodos , Administração Oral , Comprimidos
2.
Biosensors (Basel) ; 13(7)2023 Jul 16.
Artigo em Inglês | MEDLINE | ID: mdl-37504133

RESUMO

A highly sensitive unlabeled electrochemical aptasensor based on hydroxylated black phosphorus/poly-L-lysine (hBP/PLL) composite is introduced herein for the detection of malathion. Poly-L-lysine (PLL) with adhesion and coating properties adhere to the surface of the nanosheets by noncovalent interactions with underlying hydroxylated black phosphorus nanosheets (hBP) to produce the hBP/PLL composite. The as-synthesized hBP/PLL composite bonded to Au nanoparticles (Au NPs) firmly by assembling and using them as a substrate for the aptamer with high specificity as a probe to fabricate the sensor. Under optimal conditions, the linear range of the electrochemical aptasensor was 0.1 pM~1 µM, and the detection limit was 2.805 fM. The electrochemical aptasensor has great selectivity, a low detection limit, and anti-interference, which has potential application prospects in the field of rapid trace detection of pesticide residues.


Assuntos
Aptâmeros de Nucleotídeos , Técnicas Biossensoriais , Nanopartículas Metálicas , Nanopartículas Metálicas/química , Malation , Polilisina , Técnicas Eletroquímicas , Ouro/química , Fósforo , Aptâmeros de Nucleotídeos/química , Limite de Detecção
3.
Molecules ; 28(3)2023 Jan 29.
Artigo em Inglês | MEDLINE | ID: mdl-36770956

RESUMO

Paeoniflorin is a glycoside compound found in Paeonia lactiflora Pall that is used in traditional herbal medicine and shows various protective effects on the cardio-cerebral vascular system. It has been reported that the pharmacological effects of paeoniflorin might be generated by its metabolites. However, the bioavailability of paeoniflorin by oral administration is low, which greatly limits its clinical application. In this paper, a paeoniflorin-converting enzyme gene (G6046, GenBank accession numbers: OP856858) from Cunninghamella blakesleeana (AS 3.970) was identified by comparative analysis between MS analysis and transcriptomics. The expression, purification, enzyme activity, and structure of the conversion products produced by this paeoniflorin-converting enzyme were studied. The optimal conditions for the enzymatic activity were found to be pH 9, 45 °C, resulting in a specific enzyme activity of 14.56 U/mg. The products were separated and purified by high-performance counter-current chromatography (HPCCC). Two main components were isolated and identified, 2-amino-2-p-hydroxymethyl-methyl alcohol-benzoate (tirs-benzoate) and 1-benzoyloxy-2,3-propanediol (1-benzoyloxypropane-2,3-diol), via UPLC-Q-TOF-MS and NMR. Additionally, paeoniflorin demonstrated the ability to metabolize into benzoic acid via G6046 enzyme, which might exert antidepressant effects through the blood-brain barrier into the brain.


Assuntos
Cunninghamella , Paeonia , Glucosídeos/metabolismo , Glicosídeos/metabolismo , Cunninghamella/metabolismo , Monoterpenos/química , Benzoatos/metabolismo , Paeonia/química
4.
Curr Med Imaging ; 19(13): 1580-1590, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36799419

RESUMO

BACKGROUND: Infrared thermal imaging technology was used to observe the changes in infrared radiation temperature at acupoints in rats caused by chronic myocardial ischemia injury. OBJECTIVE: This study aims to compare the difference of body surface infrared radiation temperature information of three groups of acupoints: bilateral Neiguan (PC6), bilateral Yanglingquan (GB33), and bilateral Sham Acupoints (SA) in the pathological state of myocardial ischemia injury, and to explore the relationship between acupoints and viscera state. METHODS: SPF adult Wistar male rats (n = 20) were randomly divided into a control (CTL; n = 10) and an isoproterenol group (ISO; n = 10). Chronic myocardial injury was induced in rats by subcutaneous injection of isoproterenol hydrochloride for 14 d. On the second day after the establishment of the model, the serum levels of cardiac troponin (cTnI) and creatine kinase isoenzyme (CK-MB) were measured by enzyme-linked immunosorbent assay (ELISA). The morphological changes of the myocardial tissue in the two groups were observed by hematoxylin-eosin (HE) staining and their pathological scores were evaluated, which was then used to determine the myocardial ischemic injury. Two days before and after the establishment of the model, the electrocardiograms (ECG) of the two groups of rats were recorded by the (ECG) data acquisition system, and the infrared thermal imaging platform was used to detect the temperature of the six acupoints. RESULTS: 1. After subcutaneous injection of isoproterenol hydrochloride for 14 days, the ST segment of the ECG decreased in the ISO group compared with that of the CTL group; 2. Myocardial tissue injury was serious in the ISO group compared to the CTL group; 3. Serum cTn-I and CK-MB were significantly increased (P <0 01) in the ISO group, compared to that in the CTL group; 4. The infrared radiation temperature on the body surface of bilateral Neiguan (PC6) acupoints decreased significantly in the ISO group, compared to that of the CTL group. CONCLUSION: Infrared thermal imaging technology can be used to detect the changes in the energy state of acupoints. Chronic myocardial ischemic injury can cause a decrease in IR temperature on the body surface of bilateral Neiguan (PC6) acupoints, suggesting that visceral diseases can lead to changes in the energy metabolism of acupoints.


Assuntos
Eletroacupuntura , Isquemia Miocárdica , Ratos , Masculino , Humanos , Animais , Ratos Wistar , Isoproterenol/farmacologia , Pontos de Acupuntura , Temperatura , Isquemia Miocárdica/diagnóstico por imagem , Isquemia Miocárdica/metabolismo
5.
Sleep Breath ; 27(4): 1597-1610, 2023 08.
Artigo em Inglês | MEDLINE | ID: mdl-36194363

RESUMO

In western medicine, obstructive sleep apnea hypopnea syndrome (OSAHS) is an increasingly serious public health hazard, which is exacerbated by the obesity epidemic and an aging population. Ancient medical literature of traditional Chinese medicine (TCM) also recorded OSAHS-like symptoms but described the disease from a completely distinct theoretical perspective. The earliest records of snoring in ancient China can be traced back 2500 years. In TCM, the pathogenesis of OSAHS can be attributed mainly to turbid phlegm and blood stasis. Various TCM prescriptions, herbal medicines, and external therapy have also been proposed for the prevention and therapy of OSAHS. Some of these strategies are still used in current clinical practice. This review highlights historical characterizations of OSAHS and the theory of TCM and also explores its therapy in TCM, which may shed light on future OSAHS research. This is the first systematic English review of the role of TCM in the treatment of OSAHS.


Assuntos
Medicina Tradicional Chinesa , Apneia Obstrutiva do Sono , Humanos , Idoso , Polissonografia , Apneia Obstrutiva do Sono/diagnóstico , Apneia Obstrutiva do Sono/epidemiologia , Apneia Obstrutiva do Sono/terapia , Síndrome , Taxa Respiratória , Ronco/epidemiologia , Ronco/terapia
6.
Front Pharmacol ; 13: 1003812, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36532750

RESUMO

Methotrexate (MTX) is a folic acid antagonist, the mechanism of action is to inhibit DNA synthesis, repair and cell proliferation by decreasing the activities of several folate-dependent enzymes. It is widely used as a chemotherapy drug for children and adults with malignant tumors. High-dose methotrexate (HD-MTX) is an effective treatment for extramedullary infiltration and systemic consolidation in children with acute lymphoblastic leukemia (ALL). However, significant toxicity results in most patients treated with HD-MTX, which limits its use. HD-MTX-induced toxicity is heterogeneous, and this heterogeneity may be related to gene polymorphisms in related enzymes of the MTX intracellular metabolic pathway. To gain a deeper understanding of the differences in toxicity induced by HD-MTX in individuals, the present review examines the correlation between HD-MTX-induced toxicity and the gene polymorphisms of related enzymes in the MTX metabolic pathway in ALL. In this review, we conclude that only the association of SLCO1B1 and ARID5B gene polymorphisms with plasma levels of MTX and MTX-related toxicity is clearly described. These results suggest that SLCO1B1 and ARID5B gene polymorphisms should be evaluated before HD-MTX treatment. In addition, considering factors such as age and race, the other exact predictor of MTX induced toxicity in ALL needs to be further determined.

7.
Biosensors (Basel) ; 12(10)2022 Sep 20.
Artigo em Inglês | MEDLINE | ID: mdl-36290913

RESUMO

A label-free fipronil aptasensor was built based on Polylysine-black phosphorus nanosheets composition (PLL-BPNSs) and Au nanoparticles (AuNPs). A PLL-BP modified glassy carbon electrode (GCE) was fabricated by combining BP NSs and PLL, which included a considerable quantity of -NH2. Au nanoparticles (AuNPs) were placed onto the GCE, and PLL-BPNSs bonded to Au NPs firmly by assembling. The thiolated primers were then added and fixed using an S-Au bond, and competitive binding of the fipronil aptamer was utilized for fipronil quantitative assessment. The sensor's performance was evaluated using differential pulse voltammetry (DPV) method. The linear equation is ΔI (µA) = 13.04 logC + 22.35, while linear correlation coefficient R2 is 0.998, and detection limit is 74 pg/mL (0.17 nM) when the concentration of fipronil is 0.1 ng/mL-10 µg/mL. This aptasensor can apply to quantitative detection of fipronil.


Assuntos
Aptâmeros de Nucleotídeos , Técnicas Biossensoriais , Nanopartículas Metálicas , Ouro/química , Aptâmeros de Nucleotídeos/química , Técnicas Biossensoriais/métodos , Nanopartículas Metálicas/química , Fósforo , Polilisina , Eletrodos , Carbono/química , Limite de Detecção , Técnicas Eletroquímicas/métodos
8.
Chin Med ; 17(1): 57, 2022 May 17.
Artigo em Inglês | MEDLINE | ID: mdl-35578250

RESUMO

BACKGROUND: Myocardial fibrosis changes the structure of myocardium, leads to cardiac dysfunction and induces arrhythmia and cardiac ischemia, threatening patients' lives. Electroacupuncture at PC6 (Neiguan) was previously found to inhibit myocardial fibrosis. Long non-coding RNAs (lncRNAs) play a variety of regulatory functions in myocardial fibrosis, but whether electroacupuncture can inhibit myocardial fibrosis by regulating lncRNA has rarely been reported. METHODS: In this study, we constructed myocardial fibrosis rat models using isoproterenol (ISO) and treated rats with electroacupuncture at PC6 point and non-point as control. Hematoxylin-eosin, Masson and Sirius Red staining were performed to assess the pathological changes and collagen deposition. The expression of fibrosis-related markers in rat myocardial tissue were detected by RT-qPCR and Western blot. Miat, an important long non-coding RNA, was selected to study the regulation of myocardial fibrosis by electroacupuncture at the transcriptional and post-transcriptional levels. In post-transcriptional level, we explored the myocardial fibrosis regulation effect of Miat on the sponge effect of miR-133a-3p. At the transcriptional level, we studied the formation of heterodimer PPARG-RXRA complex and promotion of the TGF-ß1 transcription. RESULTS: Miat was overexpressed by ISO injection in rats. We found that Miat can play a dual regulatory role in myocardial fibrosis. Miat can sponge miR-133a-3p in an Ago2-dependent manner, reduce the binding of miR-133a-3p target to the 3'UTR region of CTGF mRNA and improve the protein expression level of CTGF. In addition, it can also directly bind with PPARG protein, inhibit the formation of heterodimer PPARG-RXRA complex and then promote the transcription of TGF-ß1. Electroacupuncture at PC6 point, but not at non-points, can reduce the expression of Miat, thus inhibiting the expression of CTGF and TGF-ß1 and inhibiting myocardial fibrosis. CONCLUSION: We revealed that electroacupuncture at PC6 point can inhibit the process of myocardial fibrosis by reducing the expression of lncRNA Miat, which is a potential therapeutic method for myocardial fibrosis.

9.
J Cardiovasc Transl Res ; 15(5): 1176-1191, 2022 10.
Artigo em Inglês | MEDLINE | ID: mdl-35377129

RESUMO

Angina pectoris is the most common manifestation of coronary heart disease, causing suffering in patients. Electroacupuncture at PC6 can effectively alleviate angina by regulating the expression of genes, whether the alternative splicing (AS) of genes is affected by acupuncture is still unknown. We established a rat model of myocardial ischemia-reperfusion by coronary artery ligation and confirmed electroacupuncture alleviated the abnormal discharge caused by angina pectoris measured in EMG electromyograms. Analysis of the GSE61840 dataset established that AS events were altered after I/R and regulated by electroacupuncture. I/R decreased the expression of splicing factor Nova1 while electroacupuncture rescued it. Further experiments in dorsal root ganglion cells showed Nova1 regulated the AS of the GABRG2, specifically on its exon 9 where an important phosphorylation site is present. In vivo, results also showed that electroacupuncture can restore AS of GABRG2. Our results proved that electroacupuncture alleviates angina results by regulating alternative splicing.


Assuntos
Eletroacupuntura , Isquemia Miocárdica , Traumatismo por Reperfusão Miocárdica , Animais , Ratos , Pontos de Acupuntura , Processamento Alternativo , Angina Pectoris , Traumatismo por Reperfusão Miocárdica/genética , Traumatismo por Reperfusão Miocárdica/prevenção & controle , Receptores de Neurotransmissores , Proteínas de Ligação a RNA/genética
10.
Front Pharmacol ; 12: 735876, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34552493

RESUMO

The serotonin receptor 5-HT1B is widely expressed in the central nervous system and has been considered a drug target in a variety of cognitive and psychiatric disorders. The anti-inflammatory effects of 5-HT1B agonists may present a promising approach for Alzheimer's disease (AD) treatment. Herbal antidepressants used in the treatment of AD have shown functional overlap between the active compounds and 5-HT1B receptor stimulation. Therefore, compounds in these medicinal plants that target and stimulate 5-HT1B deserve careful study. Molecular docking, drug affinity responsive target stability, cellular thermal shift assay, fluorescence resonance energy transfer (FRET), and extracellular regulated protein kinases (ERK) 1/2 phosphorylation tests were used to identify emodin-8-O-ß-d-glucopyranoside (EG), a compound from Chinese medicinal plants with cognitive deficit attenuating and antidepressant effects, as an agonist of 5-HT1B. EG selectively targeted 5-HT1B and activated the 5-HT1B-induced signaling pathway. The activated 5-HT1B pathway suppressed tumor necrosis factor (TNF)-α levels, thereby protecting neural cells against beta-amyloid (Aß)-induced death. Moreover, the agonist activity of EG towards 5-HT1B receptor, in FRET and ERK1/2 phosphorylation, was antagonized by SB 224289, a 5-HT1B antagonist. In addition, EG relieved AD symptoms in transgenic worm models. These results suggested that 5-HT1B receptor activation by EG positively affected Aß-related inflammatory process regulation and neural death resistance, which were reversed by antagonist SB 224289. The active compounds such as EG might act as potential therapeutic agents through targeting and stimulating 5-HT1B receptor for AD and other serotonin-related disorders. This study describes methods for identification of 5-HT1B agonists from herbal compounds and for evaluating agonists with biological functions, providing preliminary information on medicinal herbal pharmacology.

11.
Artigo em Inglês | MEDLINE | ID: mdl-34479180

RESUMO

Depression is a global mental disorder disease and greatly threatened human health. Xiaochaihutang (XCHT) has been used successfully in treatment of depression for many years in China, but the mechanism is unclear. Using the chronic unpredictable mild stress (CUMS) mice model of depression, the present study aimed to reveal possible antidepressant mechanisms of XCHT from the perspective of liver by analyzing hepatic proteomics in mice. Bioinformatics analysis identified 31 differentially expressed proteins (DEPs), including 5 upregulated and 26 downregulated proteins, between the CUMS model and XCHT groups. The bile secretion pathway was found by KEGG pathway analysis of these DEPs. Four of the 31 differentially expressed proteins, including 2 active proteins involved in bile secretion, carbonic anhydrase 2 (CA2) and cystic fibrosis transmembrane conductance regulator (CFTR), were selected to verify their genes. Four genes (Cyp7a1, Fxr, Shp and Ntcp) related to bile acid synthesis and transport were further investigated by quantitative real-time polymerase chain reaction (qRT-PCR). Both biochemical tests and gene studies demonstrated that CUMS affected bile acid synthesis and transport, while XCHT regulated this pathway. The results indicated that there may be a potential relationship between CUMS induced depression and hepatic injury caused by increased bile acid, and also provide a novel insight to understand the underlying anti-depression mechanisms of XCHT.


Assuntos
Depressão/metabolismo , Medicamentos de Ervas Chinesas/farmacologia , Fígado , Proteoma , Estresse Psicológico/metabolismo , Animais , Ácidos e Sais Biliares/metabolismo , Modelos Animais de Doenças , Fígado/química , Fígado/efeitos dos fármacos , Fígado/lesões , Masculino , Camundongos Endogâmicos C57BL , Proteoma/análise , Proteoma/química , Proteômica , Espectrometria de Massas em Tandem/métodos
12.
Artigo em Inglês | MEDLINE | ID: mdl-33747104

RESUMO

The root cause behind the development of chronic obstructive pulmonary disease (COPD) is cigarette smoke that induces the inflammation of the lung tissue and alveolar destruction. Long-term cigarette smoking can lead to deterioration in lung parenchymal function and cause structural changes in the lung, further resulting in pulmonary fibrosis. Rhodiola rosea L., a traditional medicinal perennial herb, is well known for its numerous pharmacological benefits, including anti-inflammation, antioxidant, antifatigue, antidepressive, and antifibrotic properties. Here, we evaluated the pharmacological effects and mechanisms of the Rhodiola rosea L. (RRL) macroporous resin extract on COPD caused by lipopolysaccharide (LPS) and cigarette smoke (CS) in rats. The RRL significantly improved the pathological structure of the lung tissue. Additionally, RRL decreased the infiltration of inflammatory cells and, subsequently, oxidative stress. Furthermore, the RNAseq assay indicated that RRL attenuated the CS and LPS-induced COPD via anti-inflammatory, antifibrotic, and antiapoptotic activities. Western blot analysis substantiated that the RRL resulted in upregulated levels of Nrf2 and HO-1 as well as downregulated levels of IκBα, NF-κB p65, α-SMA, and TGF-ß1. Interestingly, the RRL could protect rats from CS and LPS-induced COPD by inhibiting the ERK1/2 and Smad3 signaling pathways and apoptosis. Thus, the RRL could attenuate CS and LPS-induced COPD through inflammation inhibition and antioxidant and antifibrosis pathways.

13.
Molecules ; 24(12)2019 Jun 18.
Artigo em Inglês | MEDLINE | ID: mdl-31216740

RESUMO

The major objective of this study was to investigate the anti-chronic nonbacterial prostatitis (CNP) mechanism of T. patula by metabolomics and network pharmacology. The study demonstrated that the flavonoids and polysaccharides of T. patula could alleviate prostatitis by improving the level of DHT, reducing the secretion of PSA and TNF-α. Besides, both could enhance Na+/K+-ATPase activity, decrease the O2 consumption, CO2 production, heat production, energy expenditure of rats and promote respiratory exchange ratio of rats. Up to 28 potential biomarkers and 8 key metabolic pathways related to the treatment of CNP were elucidated by the metabolomics analysis, including phenylalanine metabolism, taurine and hypotaurine metabolism, tryptophan metabolism etc. Network pharmacology prediction also reflected the potential mechanism was associated with tryptophan metabolism and energy pathway. Generally, the potential anti-CNP mechanism of flavonoids and polysaccharides of T. patula might be through reducing the expression of inflammation factors, adjusting the level of hormone and regulating the amino acid metabolism, energy metabolism and glucose and lipid metabolism.


Assuntos
Biomarcadores , Metabolômica , Extratos Vegetais/farmacologia , Prostatite/tratamento farmacológico , Prostatite/metabolismo , Tagetes/química , Cromatografia Líquida , Doença Crônica , Metabolismo Energético/efeitos dos fármacos , Humanos , Masculino , Espectrometria de Massas , Redes e Vias Metabólicas/efeitos dos fármacos , Metaboloma , Metabolômica/métodos , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Prostatite/diagnóstico , Prostatite/etiologia
14.
Phytomedicine ; 56: 64-73, 2019 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-30668355

RESUMO

BACKGROUND: Acacia catechu (L.f.) Willd (ACW) and Scutellaria baicalensis Georgi (SBG) are two famous herbs and often used in many traditional Chinese compound prescriptions. In clinical practice, ACW-SBG couple as a famous traditional herb couple, was widely used for treating infantile cough, phlegm and fever which caused by pulmonary infection. Meanwhile, a standardized bioflavonoid composition-UP446 with ACW extract and SBG extract has been used in both special nutritional products and joint care dietary supplements. However, its herb-herb interactions based on absorption, distribution, metabolism and excretion (ADME) study had not been investigated. PURPOSE: The aim of this study was to evaluate potential pharmacokinetic, tissue distribution and excretion interactions between ACW and SBG, and to provide useful information for the development of suitable dosage forms and clinical applications. STUDY DESIGN AND METHODS: A sensitive and reliable LC-MS/MS method was established to the quantification of four major bioactive components in rat biological samples. The method was validated for accuracy, precision, linearity, range, selectivity, lower limit of quantification (LLOQ), recovery, and matrix effect. All validation parameters met the acceptance criteria according to regulatory guidelines. Based on this, we obtained and compared the parameters about pharmacokinetics, tissue distribution and excretion of four major bioactive components in this study. RESULTS: This work revealed that the parameters including plasma pharmacokinetics, tissue distribution and excretion of (+)-catechin (C), (-)-epicatechin (EC), baicalin (BL) and baicalein (BLE) in single administration had significant differences compared co-administration. The results illustrated that interactions between two herbs are related to the effect of competitive gastrointestinal absorption inhibition and drug metabolism by liver metabolic enzymes. Moreover, the alteration of C and EC in the tissue of lung maybe could enhance the pharmacological activity for treating pulmonary infection. CONCLUSION: This is the first report to evaluate the pharmacokinetics, tissue distribution and excretion of co-administration of ACW or SBG to rats and compared its properties of four major bioactive components. The results demonstrate that herb -herb interactions occurred in this herb couple.


Assuntos
Acacia/química , Medicamentos de Ervas Chinesas/farmacocinética , Extratos Vegetais/química , Extratos Vegetais/farmacocinética , Animais , Catequina/análise , Catequina/farmacologia , Cromatografia Líquida , Interações Medicamentosas , Medicamentos de Ervas Chinesas/química , Flavanonas/análise , Flavanonas/farmacocinética , Flavonoides/análise , Flavonoides/farmacocinética , Limite de Detecção , Ratos Sprague-Dawley , Reprodutibilidade dos Testes , Scutellaria baicalensis , Espectrometria de Massas em Tandem/métodos , Distribuição Tecidual
15.
Chin J Integr Med ; 25(3): 210-215, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30159645

RESUMO

OBJECTIVE: To examine the effects of ursolic acid (UA) on mitigating retinoic acid (RA)-induced osteoporosis in rats. METHODS: Fifty female Sprague-Dawley rats were randomly divided into the control group (n=10) and the osteoporosis group (n=40). The 40 osteoporosis rats were induced by 75 mg/(kg•d) RA once daily for 2 weeks, and then were randomly assigned to vehicle control (model), low-, middle-, and high-dose UA [(UA-L, UA-M, UA-H; 30, 60, 120 mg/(kg•d), respectively] groups (10 rats each). UA were administered once daily to the rats from the 3rd weeks for up to 4 weeks by gavage. Bone turnover markers [serum alkaline phosphatase (ALP), osteocalcin (OCN), urine deoxypyridinoline (DPD)] and other parameters, including serum calcium (S-Ca), serum phosphorus (S-P), urine calcium (U-Ca), urine phosphorus (U-P), and bone mineral density (BMD) of the femur, 4th lumbar vertebra and tibia, bone biomechanical properties and trabecular microarchitecture, were measured. RESULTS: The osteoporosis in rats was successfully induced by RA. Compared with the model group, UA-M and UA-H significantly reversed the RA-induced changes in S-P, U-Ca, U-P, ALP, OCN and urine DPD ratio and markedly enhanced the BMD of right femur, 4th lumbar vertebra and tibia (Plt;0.05 or Plt;0.01). Further, biomechanical test and microcomputed tomography evaluation also showed that UA-H drastically improved biomechanical properties and trabecular microarchitecture (Plt;0.05 or Plt;0.01). CONCLUSION: UA could promote bone formation, increase osteoblastic activity and reduce osteoclastic activity in rats, indicating that UA might be a potential therapeutic of RA-induced acute osteoporosis.


Assuntos
Densidade Óssea/efeitos dos fármacos , Osteoporose/tratamento farmacológico , Tretinoína/toxicidade , Triterpenos/uso terapêutico , Animais , Fenômenos Biomecânicos , Remodelação Óssea/efeitos dos fármacos , Feminino , Osteoporose/diagnóstico por imagem , Ratos , Ratos Sprague-Dawley , Triterpenos/farmacologia , Microtomografia por Raio-X , Ácido Ursólico
16.
Food Funct ; 9(12): 6608-6617, 2018 Dec 13.
Artigo em Inglês | MEDLINE | ID: mdl-30500001

RESUMO

Three new stilbenoids (1-3) and 16 known stilbenoids (4-6) and cannabinoids (7-19) were isolated from the leaves of hemp (Cannabis sativa L.). The structures of the three new compounds were identified as α,α'-dihydro-3',4,5'-trihydroxy-4'-methoxy-3-isopentenylstilbene (HM1), α,α'-dihydro-3,4',5-trihydroxy-4-methoxy-2,6-diisopentenylstilbene (HM2), and α,α'-dihydro-3',4,5'-trihydroxy-4'-methoxy-2',3-diisopentenylstilbene (HM3) by 1D and 2D NMR spectroscopy, LC-MS, and HRESIMS. The known α,α'-dihydro-3,4',5-trihydroxy-4,5'-diisopentenylstilbene (5) and combretastatin B-2 (6) were isolated for the first time from C. sativa f. sativa. These isolated compounds exhibited cytotoxic effects on human cancer cells via inhibiting the proliferation of cancer cells and inducing cell death. Among them, compounds 4, 5, 10, 12, 13, 15, and 19 displayed broad-spectrum cytotoxicity, and 1, 7, and 11 displayed selectivity in inhibition efficiency on MCF-7 and A549 cells, which suppressed the proliferation of cancer cells significantly by inducing cell death. The effects of compounds 1-3 on improving reverse cholesterol transport (RCT) were evaluated by isotope-tracing and western blotting. Results showed that the three stilbenoids showed a cytotoxicity above 1.0 mg L-1, especially that of HM3. They could improve [3H]-cholesterol efflux from Raw 264.7 macrophages to high density lipoproteins by enhancing the protein expression of ABCG1 and SR-B1, and HM1 and HM2 showed a significant difference compared with fenofibrate at 1.0 mg L-1. The three stilbenoids could also significantly improve the protein expression of ABCA1. Further study on HepG2 cells indicated that they improve the protein expression of LDLR, SR-B1 and CYP7A1, especially that of HM1 and HM3. However, they showed no significant effect on PCSK9. The above results indicated that these stilbenoids may elevate the transfer of cholesterol to hepatocytes by improving the protein expression of SR-B1 and LDLR, and the synthesis of bile acid by increasing the protein expression of CYP7A1. In conclusion, HM1 showed lower cytotoxicity and higher activity in improving the RCT-related protein expression. Our study suggests that it may be explored as a novel lipid-lowering drug and as a beneficial ingredient in health functional foods and pharmaceuticals.


Assuntos
Canabinoides/farmacologia , Cannabis/química , Colesterol/metabolismo , Medicamentos de Ervas Chinesas/farmacologia , Estilbenos/farmacologia , Membro 1 da Subfamília G de Transportadores de Cassetes de Ligação de ATP/genética , Membro 1 da Subfamília G de Transportadores de Cassetes de Ligação de ATP/metabolismo , Transporte Biológico/efeitos dos fármacos , Canabinoides/química , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Medicamentos de Ervas Chinesas/química , Humanos , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Estrutura Molecular , Folhas de Planta/química , Receptores Depuradores Classe B/genética , Receptores Depuradores Classe B/metabolismo , Estilbenos/química
17.
J Nanosci Nanotechnol ; 18(12): 8133-8141, 2018 12 01.
Artigo em Inglês | MEDLINE | ID: mdl-30189930

RESUMO

The present work aimed to investigate extracellular biosynthesis of silver nanoparticles (AgNPs) mediated by an actinomycete strain and their cytotoxic effects compared with silver ions. The selected strain was identified as Streptomyces coelicoflavus KS-3 by phenotypical characteristics and 16S rRNA analysis. The formation of biosynthesized AgNPs was proved by an absorption peak observed at 437 nm. Transmission electron microscopy (TEM) and dynamic light scattering (DLS) analyses revealed that the prepared AgNPs were spherical or approximately spherical followed by a small amount of truncated triangular, quadrangular and hexagonal with the particle diameters ranging from 2.33 to 91.3 nm. X-ray diffraction (XRD) pattern confirmed that the AgNPs presented a face-centered cubic (FCC) structure of crystalline silver. Energy dispersive of X-ray (EDX) spectrum and Fourier transform infrared spectroscopy (FTIR) analyses verified the existence of biomolecules, such as proteins, that participated in the formation and stabilization of AgNPs. Furthermore, the comparative study on cytotoxic effect of AgNPs indicated that the AgNPs exhibited higher biocompatibility towards human bronchial epithelial (HBE) cells than silver ions and exerted potent cytotoxic effect in a dose-dependent manner against human lung squamous cell carcinoma cells (HTB-182) and human lung adenocarcinoma cells (A549) with the concentrations ranging from 1 to 50 µg/mL.


Assuntos
Nanopartículas Metálicas , Prata , Streptomyces , Adenocarcinoma de Pulmão/tratamento farmacológico , Humanos , Neoplasias Pulmonares/tratamento farmacológico , Compostos Orgânicos , Extratos Vegetais , RNA Ribossômico 16S , Prata/farmacologia , Células Tumorais Cultivadas
18.
Biochem Biophys Res Commun ; 503(2): 998-1003, 2018 09 05.
Artigo em Inglês | MEDLINE | ID: mdl-29936180

RESUMO

Brassica campestris Male Fertility 20 (BcMF20) is a typical zinc-finger transcription factor that was previously isolated from flower buds of Chinese cabbage (Brassica campestris ssp. chinensis). By applying expression pattern analysis, it can be known that BcMF20 was specifically and strongly expressed in tapetum and pollen, beginning from the uninucleate stage, and was maintained during the mature-pollen stage. As BcMF20 was highly conserved in Cruciferae, it can be indicated that this zinc-finger transcription factor is important during the growth of Cruciferae. In this study, 12 C2H2-type zinc-finger TFs which shared high homology with BcMF20 were found from NCBI via BLAST. A new molecular phylogenetic tree was constructed by the comparison between BcMF20 and these 12 C2H2-type zinc-finger TFs with NJ method. By analyzing this phylogenetic tree, the evolution of BcMF20 was discussed. Then, antisense RNA technology was applied in the transgenesis of Arabidopsis thaliana to get the deletion mutants of BcMF20, so that its function during the pollen development can be identified. The results showed: BcMF20 are in the same clade with three genes from Arabidopsis. The inhibition of BcMF20 expression led to smaller amounts of and lower rate in germination of pollen and lower rate in fruit setting in certain transgenetic plants. This also led to the complete collapse of pollen grains. By SEM and TEM, pollen morphology and anther development processes were observed. In the middle uninucleate microspore stage, a relatively thin or even no primexine was formed in microspores. This may result in the malformation of the pollen wall and finally cause the deformity of pollens. Above all, it can be indicated that BcMF20 may act as a part of regulation mechanisms of TAZ1 and MS1. Together they play a role in a genetic pathway in the tapetum to act on proliferation of tapetal cells and keep the normal development of pollens.


Assuntos
Brassica/genética , Germinação , Proteínas de Plantas/genética , Pólen/genética , Fatores de Transcrição/genética , Brassica/crescimento & desenvolvimento , Brassicaceae/genética , Brassicaceae/crescimento & desenvolvimento , Regulação da Expressão Gênica de Plantas , Genes de Plantas , Filogenia , Pólen/crescimento & desenvolvimento , Dedos de Zinco
19.
Oncotarget ; 8(26): 43306-43321, 2017 Jun 27.
Artigo em Inglês | MEDLINE | ID: mdl-28496007

RESUMO

BACKGROUND: The epidemiological evidence for a dose-response relationship between tea consumption and risk of cognitive disorders is sparse. The aim of the study was to summarize the evidence for the association of tea consumption with risk of cognitive disorders and assess the dose-response relationship. METHODS: We searched electronic databases of Pubmed, Embase, and Cochrane Library (from 1965 to Jan 19, 2017) for eligible studies that published in the international journals. A random-effects model was used to pool the most adjusted odds ratios (ORs) and the corresponding 95% confidence intervals (CIs). RESULTS: Seventeen studies involving 48,435 participants were included in our study. The meta-analysis showed that a higher tea consumption was associated with a significant reduction in the risk of cognitive disorders (OR=0.73, 95% CI: 0.65-0.82). When considering the specific types of tea consumption, the significantly inverse association is only found in green tea consumption (OR=0.64, 95% CI: 0.53-0.77) but not in black/oolong tea consumption (OR=0.75, 95% CI: 0.55-1.01). Dose-response meta-analysis indicated that tea consumption is linearly associated with a reduced risk of cognitive disorders. An increment of 100 ml/day, 300 ml/day, and 500 ml/day of tea consumption was associated with a 6% (OR=0.94, 95% CI: 0.92-0.96), 19% (OR=0.81, 95% CI: 0.74-0.88), and 29% (OR=0.71, 95% CI: 0.62-0.82) lower risk of cognitive disorders. CONCLUSIONS: Tea consumption is inversely and linearly related to the risk of cognitive disorders. More studies are needed to further confirm our findings.


Assuntos
Transtornos Cognitivos/etiologia , Chá/efeitos adversos , Idoso , Idoso de 80 Anos ou mais , Transtornos Cognitivos/patologia , Feminino , Humanos , Masculino , Estudos Observacionais como Assunto , Fatores de Risco
20.
Pharmacognosy Res ; 9(2): 151-155, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28539738

RESUMO

BACKGROUND: The morphological identification is an effective and simple quality evaluation method in Chinese drugs, and the traits of mealiness and color were widely used in the commercial market of Chinese drugs. OBJECTIVE: The objective of this study was to explore the correlation between mealiness of herbal drugs and its quality; licorice was selected as an example. MATERIALS AND METHODS: The mealiness of licorice was graded by its weight; meanwhile, the content of glycyrrhizic acid and liquiritin was determined by high-performance liquid chromatography-diode-array detection method; the content of polysaccharides, soluble sugars, pectin, total starch, amylose, and amylopectin was measured by colorimetric method; and the number and diameter of starch granule were observed by microscope. RESULTS: The results showed that the mealiness of licorice which collected from wild and cultivated plants is positively correlated with the content of glycyrrhizic acid, liquiritin, the ratio of amylose to total starch, and the number of starch granules whose diameter was over 5 µm. However, the mealiness is negatively correlated with the total starch. Further, the formation mechanism of starch granule was discussed. CONCLUSION: It is for the first time to report the positive correlation between the mealiness and the starch granule size, the ratio of amylose to total starch, which can provide rationality for the quality evaluation using the character of mealiness in herbal medicine. SUMMARY: It is a convenient method to justify the quality of herbal medicine. To explore the correlation between mealiness of herbal drugs and its quality, licorice was selected as an example. The result indicated that the effective constituent is correlated with mealiness of licorice. Abbreviations Used: TCM: Traditional Chinese Medicine.

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