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1.
Genes (Basel) ; 15(3)2024 02 26.
Artigo em Inglês | MEDLINE | ID: mdl-38540360

RESUMO

German chamomile (Matricaria chamomilla L.) and Roman chamomile (Chamaemelum nobile) are the two well-known chamomile species from the Asteraceae family. Owing to their essential oils and higher medicinal value, these have been cultivated widely across Europe, Northwest Asia, North America, and Africa. Regarding medicinal applications, German chamomile is the most commonly utilized variety and is frequently recognized as the "star among medicinal species". The insufficient availability of genomic resources may negatively impact the progression of chamomile industrialization. Chamomile's mitochondrial genome is lacking in extensive empirical research. In this study, we achieved the successful sequencing and assembly of the complete mitochondrial genome of M. chamomilla and C. nobile for the first time. An analysis was conducted on codon usage, sequence repeats within the mitochondrial genome of M. chamomilla and C. nobile. The phylogenetic analysis revealed a consistent positioning of M. chamomilla and C. nobile branches within both mitochondrial and plastid-sequence-based phylogenetic trees. Furthermore, the phylogenetic analysis also showed a close relationship between M. chamomilla and C. nobile within the clade comprising species from the Asteraceae family. The results of our analyses provide valuable resources for evolutionary research and molecular barcoding in chamomile.


Assuntos
Asteraceae , Genoma Mitocondrial , Matricaria , Óleos Voláteis , Matricaria/genética , Chamaemelum/genética , Filogenia , Genoma Mitocondrial/genética , Asteraceae/genética
2.
Mol Pharm ; 20(8): 4210-4218, 2023 08 07.
Artigo em Inglês | MEDLINE | ID: mdl-37463505

RESUMO

Photothermal therapy, combined with chemotherapy, holds promising prospects for the therapeutic outcome of malignant tumors. However, the synergistic therapeutic effect suffers from low coloading capacity and inefficient synchronous tumor-targeting delivery of chemodrug and photothermal photosensitizers. Herein, we designed a versatile carrier-free nanoplatform to seek improvement for chemo-photothermal therapy. An NIR photosensitizer IR-808 was used for noninvasive cancer imaging, diagnosis, and imaging-guided photothermal therapy. A reduction-sensitive paclitaxel prodrug (PTX-SS-PEG2k) was rationally synthesized by covalently linking paclitaxel with polyethylene glycol 2000 via a disulfide bond. Then, the carrier-free nanoassemblies were constructed with an inner core of IR-808 and an amphiphilic paclitaxel prodrug shell. PTX-SS-PEG2k served as a stabilizer and chemodrug and could facilitate the self-assembly of IR-808 nanoparticles with high coloading efficiency and reduction-sensitive drug release. The versatile nanoplatform exhibited multiple advantages, including high drug payload, reduction-sensitive drug release, tumor-targeting drug delivery, and potent synergistic antitumor effect. We provide a versatile theranostic nanoplatform, which improves the effectiveness of synergetic chemo-photothermal therapy and reduces the off-target toxicity.


Assuntos
Hipertermia Induzida , Nanopartículas , Pró-Fármacos , Pró-Fármacos/química , Terapia Fototérmica , Fototerapia/métodos , Linhagem Celular Tumoral , Paclitaxel , Nanopartículas/química , Liberação Controlada de Fármacos , Doxorrubicina/química , Hipertermia Induzida/métodos
3.
Sci Rep ; 13(1): 793, 2023 01 16.
Artigo em Inglês | MEDLINE | ID: mdl-36646777

RESUMO

A large body of literature has shown that ginseng had a role in diabetes mellitus management. Ginsenosides are the main active components of ginseng. But what ginsenosides can manage in diabetic are not systematic. The targets of these ginsenosides are still incomplete. Our aim was to identify which ginsenosides can manage diabetes mellitus through network pharmacology and molecular docking. To identify the targets of these ginsenosides. In this work, we retrieved and screened ginsenosides and corresponding diabetes mellitus targets across multiple databases. PPI networks of the genes were constructed using STRING, and the core targets were screened out through topological analysis. Gene Ontology and Kyoto Encyclopedia of Genes and Genomes enrichment analyses were performed by using the R language. Finally, molecular docking was performed after bioinformatics analysis for verification. Our research results showed that 28 ginsenosides in ginseng might be against diabetes mellitus by modulating related proteins such as VEGFA, Caspase 3, and TNF-α. Among the 28 ginsenosides, 20(R)-Protopanaxatriol, 20(R)-Protopanaxadiol, and Ginsenoside Rg1 might play a significant role. Kyoto Encyclopedia of Genes and Genomes and Gene Ontology enrichment analysis showed that the management of diabetes mellitus by ginsenosides may be related to the positive regulation of reactive oxygen metabolic processes, associated with the insulin signaling pathway, TNF signaling pathway, and AMPK signaling pathway. Molecular docking results and molecular dynamics simulation showed that most ginsenosides could stably bind to the core target, mainly hydrogen bonding and hydrophobic bond. This study suggests the management of ginseng on diabetes mellitus. We believe that our results can contribute to the systematic study of the mechanism of ginsenosides for the management of diabetes mellitus. At the same time, it can provide a theoretical basis for subsequent studies on the management of ginsenosides in diabetes mellitus.


Assuntos
Diabetes Mellitus , Medicamentos de Ervas Chinesas , Ginsenosídeos , Panax , Farmacologia em Rede , Ginsenosídeos/farmacologia , Ginsenosídeos/uso terapêutico , Simulação de Acoplamento Molecular , Diabetes Mellitus/tratamento farmacológico , Medicina Tradicional Chinesa
4.
Chin J Nat Med ; 20(12): 881-901, 2022 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-36549803

RESUMO

As a steroid skeleton-based saponin, ginsenoside Rh2 (G-Rh2) is one of the major bioactive ginsenosides from the plants of genus Panax L. Many studies have reported the notable pharmacological activities of G-Rh2 such as anticancer, antiinflammatory, antiviral, antiallergic, antidiabetic, and anti-Alzheimer's activities. Numerous preclinical studies have demonstrated the great potential of G-Rh2 in the treatment of a wide range of carcinomatous diseases in vitro and in vivo. G-Rh2 is able to inhibit proliferation, induce apoptosis and cell cycle arrest, retard metastasis, promote differentiation, enhance chemotherapy and reverse multi-drug resistance against multiple tumor cells. The present review mainly summarizes the anticancer effects and related mechanisms of G-Rh2 in various models as well as the recent advances in G-Rh2 delivery systems and structural modification to ameliorate its anticancer activity and pharmacokinetics characteristics.


Assuntos
Antineoplásicos , Ginsenosídeos , Neoplasias , Saponinas , Humanos , Ginsenosídeos/farmacologia , Antineoplásicos/farmacologia , Saponinas/farmacologia , Neoplasias/tratamento farmacológico , Apoptose
5.
Am J Chin Med ; 50(8): 2033-2056, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36222119

RESUMO

Ginsenoside Rg5 (G-Rg5) is a rare ginsenoside isolated from ginseng (Panax ginseng C.A. Meyer), and this compound is increasingly known for its potent pharmacological activities. This study aimed to provide a comprehensive review of the main activities and mechanisms of G-Rg5 by adopting network pharmacological analysis combined with a summary of published articles. The 100 target genes of G-Rg5 were searched through available database, subjected to protein-protein interaction (PPI) network generation and then core screening. The results showed that G-Rg5 has promising anticancer and neuroprotective effects. By summarizing these two pharmacological activities, we found that G-Rg5 exerts its therapeutic effects mainly through PI3K/AKT, MAPK signaling pathways, and the regulation of apoptosis and cell cycle. And these results were corroborated by KEGG analysis. Likewise, molecular docking of the related proteins was performed, and the binding energies were all less than [Formula: see text]7.0[Formula: see text]kJ/mol, indicating that these proteins had excellent binding capacity with G-Rg5. The network pharmacology results revealed many potential G-Rg5 mechanisms, which need to be further explored. We expect that the network pharmacology approach and molecular docking techniques can help us gain a deeper understanding of the therapeutic mechanisms of different ginsenosides and even the ginseng plant, for further developing their therapeutic potential as well as clinical applications.


Assuntos
Ginsenosídeos , Panax , Ginsenosídeos/farmacologia , Ginsenosídeos/uso terapêutico , Fosfatidilinositol 3-Quinases/metabolismo , Neuroproteção , Simulação de Acoplamento Molecular , Farmacologia em Rede , Panax/química
6.
Anim Nutr ; 7(4): 1105-1114, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34738041

RESUMO

Clostridium butyricum has been widely considered an antibiotic substitute in recent years. It can promote growth performance, improve the immune response and enhance the intestinal barrier function of the host. In the present study, 1-d-old Arbor Acres (AA) broilers were fed C. butyricum (1 × 109 cfu/kg) for 28 d. The transcriptomic characteristics of epithelial cells of the cecal mucosa were determined by RNA-sequence, and the cecal microbiota composition was explored by 16S ribosomal RNA gene sequencing. The changes in the intestinal mucosa of broilers were then analyzed by tissue staining. Gene Ontology (GO) annotations identified substance transport and processes and pathways that might participate in intestinal development and cell viability. Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway analysis revealed that the differentially expressed genes are involved in numerous pathways related to amino acid and vitamin metabolism and antioxidant and defensive functions, among others. The relative expression of some genes associated with intestinal barrier function (claudins 2, 15, 19, and 23, tight junction proteins 1, 2, and 3 and mucin 1) was significantly increased in the treatment group (P < 0.05 or P < 0.01). Moreover, the proportion of Firmicutes was higher in the C. butyricum-treated group, whereas the proportion of Proteobacteria was higher in the control group. At the genus level, the relative abundances of Butyricicoccus and Lactobacillus, among other bacteria, were increased after C. butyricum supplementation. The tissue staining analysis showed that the cecal mucosa of broilers was significantly ameliorated after the addition of C. butyricum (P < 0.05 or P < 0.01). These results showed that dietary supplementation with C. butyricum can enhance the antioxidant capacity, mucosal barrier function, and stabilize the cecal microbiota, resulting in improving the growth performance.

7.
Am J Chin Med ; 49(7): 1739-1756, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34461812

RESUMO

Although the protective effect of ginsenoside on cisplatin-induced renal injury has been extensively studied, whether ginsenoside interferes with the antitumor effect of cisplatin has not been confirmed. In this paper, we verified the main molecular mechanism of 20(R)-ginsenoside Rg3 (R-Rg3) antagonizing cisplatin-induced acute kidney injury (AKI) through the combination of in vivo and in vitro models. It is worth mentioning that the two cell models of HK-2 and HepG2 were used simultaneously for the first time to explore the effect of the activation site of tumor-associated protein p53 on apoptosis and tumor suppression. The results showed that a single injection of cisplatin (20 mg/kg) led to weight loss, the kidney index of the mice increased, and creatinine (CRE) and blood urea nitrogen (BUN) levels in mice sharply increased. Continuous administration of R-Rg3 at doses of 10 and 20 mg/kg for 10 days could significantly alleviate this symptom. Similarly, R-Rg3 treatment reduced oxidative stress damage caused by cisplatin. Moreover, R-Rg3 could observably reduce the apoptosis and inflammatory infiltration of renal tubular cells induced by cisplatin. We used western blotting analysis to demonstrate that R-Rg3 restored cisplatin-induced AKI might be related to PI3K/AKT and NF-[Formula: see text]B mediated apoptosis and inflammation pathways. In the meantime, we also verified that R-Rg3 could activate different sites of p53 to control renal cell apoptosis induced by cisplatin without affecting its antitumor effect.


Assuntos
Injúria Renal Aguda/induzido quimicamente , Injúria Renal Aguda/tratamento farmacológico , Cisplatino/efeitos adversos , Ginsenosídeos/farmacologia , NF-kappa B/metabolismo , Fosfatidilinositol 3-Quinases/metabolismo , Proteínas Proto-Oncogênicas c-akt/metabolismo , Animais , Antineoplásicos/efeitos adversos , Apoptose/efeitos dos fármacos , Linhagem Celular , Modelos Animais de Doenças , Humanos , Masculino , Camundongos , Camundongos Endogâmicos ICR , Estresse Oxidativo/efeitos dos fármacos
8.
Nanomedicine ; 34: 102382, 2021 06.
Artigo em Inglês | MEDLINE | ID: mdl-33771706

RESUMO

Invasive infections caused by antibiotic-resistant Staphylococcus aureus have posed a great threat to human health. To tackle this problem, a cationic liposomal Curcumin (C-LS/Cur) was developed and its effect against antibiotic-resistant S. aureus was investigated in this study. As expected, C-LS/Cur exhibited greater bactericidal capacity compared with its counterparts, probably because the negatively charged S. aureus favors electrostatic interactions rather than intercalation with cationic liposomal vesicles at the beginning of endocytic process, thereby effectively delivering Cur to its targets. We confirmed this hypothesis by monitoring zeta potential variation, collecting visual evidences through CLSM, FCM and TEM, and determining binding kinetics by BLI. Moreover, an excellent therapeutic efficacy of C-LS/Cur against invasive murine infection was also observed, which was due to the enhanced accumulation and retention in the targets. Therefore, cationic liposomes have great potential for the clinical application in the treatment of invasive antibiotic-resistant S. aureus infections.


Assuntos
Lipossomos , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Infecções Estafilocócicas/tratamento farmacológico , Cátions , Endocitose , Humanos , Staphylococcus aureus Resistente à Meticilina/isolamento & purificação , Testes de Sensibilidade Microbiana
9.
Kaohsiung J Med Sci ; 36(9): 732-740, 2020 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-32374939

RESUMO

Cisplatin, as one of the most effective chemotherapeutic agents, its clinical use is limited by serious side effect of nephrotoxicity. Cisplatin-induced nephrotoxicity is closely related to apoptosis induction and activation of caspase. The present study aimed to explore the potential protective effect of ginsenoside Rk1 (Rk1), a rare ginsenoside generated during steaming ginseng, on cisplatin-induced nephrotoxicity and the underlying mechanisms in human embryonic kidney 293 (HEK-293) cells. Our results showed that the reduced cell viability induced by cisplatin could significantly recover by Rk1. Furthermore, glutathione (GSH) as an oxidative index, was elevated and the lipid peroxidation product malondialdehyde (MDA) was significantly decreased after Rk1 treatment compared to the cisplatin group. Additionally, Rk1 can also decrease the ROS fluorescence expression and increase the protein levels of nuclear factor erythroid 2-related factor 2 (Nrf2) and heme oxygenase-1 (HO-1) compared to the cisplatin group, which suggested a suppression of oxidative response. More importantly, the cisplatin-induced elevated protein levels of Bax, cleaved caspase-3, cleaved caspase-9, and decreased protein level of Bcl-2 were reversed after treatment with Rk1. Our results elucidated the possible protective mechanism of Rk1 for the first time, which may involve in its anti-oxidation and anti-apoptosis effects.


Assuntos
Antineoplásicos/toxicidade , Antioxidantes/farmacologia , Cisplatino/toxicidade , Regulação da Expressão Gênica/efeitos dos fármacos , Ginsenosídeos/farmacologia , Antioxidantes/isolamento & purificação , Caspase 3/genética , Caspase 3/metabolismo , Caspase 9/genética , Caspase 9/metabolismo , Cisplatino/antagonistas & inibidores , Ginsenosídeos/isolamento & purificação , Glutationa/agonistas , Células HEK293 , Heme Oxigenase-1/genética , Heme Oxigenase-1/metabolismo , Humanos , Malondialdeído/antagonistas & inibidores , Fator 2 Relacionado a NF-E2/genética , Fator 2 Relacionado a NF-E2/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Panax/química , Proteínas Proto-Oncogênicas c-bcl-2/genética , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , Espécies Reativas de Oxigênio/antagonistas & inibidores , Espécies Reativas de Oxigênio/metabolismo , Transdução de Sinais , Proteína X Associada a bcl-2/genética , Proteína X Associada a bcl-2/metabolismo
10.
Nat Prod Res ; 34(18): 2559-2565, 2020 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-30450965

RESUMO

A novel acylated quercetin glycoside, floralpanasenoside A (1) and five known flavonoid glycosides, panasenoside (2), quercetin 3-O-(2''-ß-D-glucopyranosyl)-ß-D- galactopyranoside (3), trifolin (4) kaempferol 7-O-α-L-rhamnoside (5), and afzelin (6) were isolated from the flower buds of Panax ginseng. Their structures were established by spectroscopic data and comparison with the literature values. Four of the six isolated compounds including 1 (IC50 = 62.4) exhibited α-glucosidase inhibitory activity with IC50 values lower than acarbose (385.2 µM). The molecular docking study indicated that 1 bound to the active site of α-glucosidase with numerous hydrogen bond interactions.


Assuntos
Flores/química , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Glicosídeos/química , Panax/química , Quercetina/química , Flavonoides/química , Flavonoides/isolamento & purificação , Flores/metabolismo , Inibidores de Glicosídeo Hidrolases/farmacologia , Glicosídeos/isolamento & purificação , Concentração Inibidora 50 , Quempferóis/isolamento & purificação , Simulação de Acoplamento Molecular , Panax/metabolismo , Extratos Vegetais/química , Quercetina/isolamento & purificação , alfa-Glucosidases/metabolismo
11.
J Agric Food Chem ; 67(31): 8617-8625, 2019 Aug 07.
Artigo em Inglês | MEDLINE | ID: mdl-31293160

RESUMO

Inhibiting starch digestion can effectively control postprandial blood sugar level. In this study, the in vitro digestion differences among the mixtures of five polyphenols (i.e., procyanidins [PAs], catechin [CA], tannic acid [TA], rutin [RU], and quercetin [QU]) and starch were analyzed through an in vitro simulation test of starch digestion. The interaction characteristics of these five polyphenols with α-amylase and α-glucosidase were investigated in terms of the inhibition effect, dynamics, fluorescence quenching, and circular dichroism (CD). The results revealed that the rapidly digestible starch (RDS) contents decreased, while the resistant starch (RS) contents increased. All five polyphenols inhibited the α-amylase activity through the noncompetitive approach but inhibited the α-glucosidase activity through the competitive approach. Five polyphenols combined with α-amylase spontaneously by using the hydrophobic effect. The interaction of PAs and QU with α-glucosidase were recognized as van der Waals forces and H bonding, whereas CA and TA interacted with α-glucosidase through the hydrophobic effect. All five polyphenols can cause conformational changes in enzymes.


Assuntos
Extratos Vegetais/química , Polifenóis/química , Amido/química , Animais , Digestão , Inibidores Enzimáticos/química , Inibidores Enzimáticos/metabolismo , Proteínas Fúngicas/química , Proteínas Fúngicas/metabolismo , Cinética , Modelos Biológicos , Extratos Vegetais/metabolismo , Polifenóis/metabolismo , Amido/metabolismo , Suínos , Leveduras/enzimologia , alfa-Amilases/química , alfa-Amilases/metabolismo , alfa-Glucosidases/química , alfa-Glucosidases/metabolismo
12.
Zhongguo Zhong Yao Za Zhi ; 44(12): 2519-2531, 2019 Jun.
Artigo em Chinês | MEDLINE | ID: mdl-31359719

RESUMO

This project is to investigate the chemical constituents of ginsenosides from the flower buds of Panax ginseng. The compounds were isolated by using a variety of chromatographic methods including Diaion HP-20,silica gel,MCI gel and semi-preparative HPLC chromatography. Their structures were identified by NMR,and MS data. As a result,32 compounds were isolated from the extract of P. ginseng flower buds,and identified as ginsenoside Rk_3( 1),ginsenoside Rh_4( 2),ginsenoside Rh_8( 3),pseudoginsenoside Rc_1( 4),ginsenoside Rc( 5),ginsenoside Rb_2( 6),ginsenoside Rg_6( 7),20( E)-ginsenoside F_4( 8),ginsenoside Rb_1( 9),vinaginsenoside R_(16)( 10),ginsenoside Rh_6( 11),vinaginsenoside R_3( 12),5,6-didehydro-ginsenoside Rd( 13),vinaginsenoside R_4( 14),vinaginsenoside R_8( 15),ginsenoside Rf( 16),notoginsenoside E( 17),ginsenoside Ⅲ( 18),3-O-ß-D-glucopyranosyl-3ß,7ß,12ß,20 S-tetrahydroxydammar-5( 6),24-diene-20-O-ß-D-glucopyranoside( 19),20( S)-ginsenoside Rg_2( 20),20( R)-ginsenoside Rg_2( 21),notoginsenoside R_2( 22),ginsenoside F_2( 23),quinquenoside I( 24),ginsenoside M_1( 25),quinquenoside L_(10)( 26),ginsenoside Rh_5( 27),ginsenoside Rg_5( 28),ginsenoside Rk_1( 29),20( R)-ginsenoside Rg_3( 30),oleanolic acid 3-O-ß-D-glucopyranosyl-( 1→2)-ß-D-( 6'-methyl ester)-glucuronopyranoside( 31) and ginsenoside MC( 32). Among them,compounds 10,12,13,15,19,22,24,31 and 32 were isolated from P. ginseng for the first time,and compound 19 was a genuine ginsenoside firstly obtained by separation and identification,with NMR data that were also reported. Compounds 1-3,7,8,23,25-30 were isolated from P. ginseng flower buds for the first time.


Assuntos
Flores/química , Ginsenosídeos/análise , Panax/química , Saponinas/análise , Cromatografia Líquida de Alta Pressão , Espectroscopia de Ressonância Magnética
13.
Steroids ; 143: 1-5, 2019 03.
Artigo em Inglês | MEDLINE | ID: mdl-30543815

RESUMO

Three pairs of ginsenoside epimers, including three new compounds (2, 3 and 5), were isolated from the flower buds of Panax ginseng. The structures of the isolated compounds were elucidated on the basis of considerable spectroscopic analyses and comparison with the reported data. All six compounds were evaluated for their cytotoxicties against three human cancer cell lines, HL-60, MGC80-3 and Hep-G2. Compounds 1, 3, and 6 with S configurations at C-24 or C-20 showed moderate inhibitory activities with IC50 values of 25.32, 18.76, and 38.64 µM in HL-60 cells, respectively. Our findings showed that different configurations of these isolated ginsenosides had a significant impact on the antitumor activity, and S epimers were higher than R.


Assuntos
Antineoplásicos/química , Antineoplásicos/farmacologia , Flores/química , Ginsenosídeos/química , Ginsenosídeos/farmacologia , Panax/química , Linhagem Celular Tumoral , Humanos , Hidrólise , Estereoisomerismo
14.
Biomed Res Int ; 2018: 8628531, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30105254

RESUMO

Polyploidization is an effective means of improving the active components and quality of secondary metabolism in medicinal plants. In the present study, we compared the immunostimulatory effects of crude polysaccharides from tetraploid and diploid Echinacea purpurea. The results showed that the carbohydrate contents of crude polysaccharide of tetraploid E. purpurea (CPE4) and diploid E. purpurea (CPE2) were 85.51% and 44.65%, respectively. 1H-nuclear magnetic resonance (NMR) spectroscopy and gel-permeation chromatography (GPC) analyses showed no major differences in the overall structure and molecular weight of polysaccharides between CPE4 and CPE2. However, some differences in the relative content of the same polysaccharides group were observed between CPE4 and CPE2. In in vitro tests, EP4 could stimulate lymphocyte proliferation and secretion of cytokines maximally at the concentration of 0.0312 mg/mL, and EP2 could stimulate lymphocyte proliferation and secretion of cytokines maximally at the concentration of 0.125 mg/mL. In in vivo tests, EP4 was more effective at promoting the proliferation of lymphocytes and secretion of cytokines in mice immunosuppressed by cyclophosphamide than EP2 at the same concentration. Taken together, these data demonstrated that the relative content of the partial polysaccharides group is increased, and the immunoregulatory effect is enhanced in tetraploid E. purpurea.


Assuntos
Adjuvantes Imunológicos/farmacologia , Echinacea/química , Extratos Vegetais/farmacologia , Polissacarídeos/farmacologia , Animais , Diploide , Echinacea/genética , Feminino , Masculino , Camundongos , Tetraploidia
15.
Curr Drug Deliv ; 15(3): 424-435, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29219057

RESUMO

BACKGROUND: Ethosomes, a novel type of percutaneous drug delivery carrier with a lipid bilayer structure, penetrate the skin barrier due to their deformability and malleability, and presence of ethanol that fluidizes lipids in the skin. In order to further enhance the delivery of drugs through the skin, penetration enhancers are widely used. OBJECTIVE: The objective of this work was to develop an optimized formulation of lornoxicam ethosomal gels, investigate skin permeability with the addition of penetration enhancers, and evaluate the invivo pharmacodynamics of these formulations. METHODS: Lornoxicam ethosomes were prepared by the ethanol injection method and optimized using the orthogonal design method. Lornoxicam ethosomal gels with enhancers were prepared and optimized using in-vitro transdermal delivery experiments. Experiments on lornoxicam ethosomal gels containing various enhancers such as azone, menthol, lauryl alcohol, and oleic acid were conducted using vertical Franz diffusion cells to measure the percutaneous permeability of the different formulations. Furthermore, the in-vivo analgesic effects of the optimized lornoxicam ethosomal gels were examined using the hot-plate and acetic acid-induced writhing tests. Anti-inflammatory activity was investigated using the dimethylbenzene-induced mouse ear swelling method. RESULTS: The results showed that compared to other formulations, the optimized lornoxicam ethosomal gels with 5 % menthol significantly increased transdermal penetration. Meanwhile, the optimized lornoxicam ethosomal gels showed remarkably anti-nociceptive and anti-inflammatory activity compared with the plain lornoxicam gels. CONCLUSION: These results suggest that the optimized ethosomal gel formulated in this study is a promising lornoxicam carrier in transdermal delivery systems to enhance anti-nociceptive and antiinflammatory efficiency.


Assuntos
Analgésicos/administração & dosagem , Anti-Inflamatórios não Esteroides/administração & dosagem , Mentol/administração & dosagem , Piroxicam/análogos & derivados , Ácido Acético , Analgésicos/química , Analgésicos/farmacocinética , Analgésicos/uso terapêutico , Animais , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/farmacocinética , Anti-Inflamatórios não Esteroides/uso terapêutico , Colesterol/química , Composição de Medicamentos , Sistemas de Liberação de Medicamentos , Edema/induzido quimicamente , Edema/tratamento farmacológico , Etanol/química , Feminino , Géis , Temperatura Alta/efeitos adversos , Lecitinas/química , Lipossomos , Mentol/química , Mentol/farmacocinética , Mentol/uso terapêutico , Camundongos Endogâmicos BALB C , Dor/tratamento farmacológico , Dor/etiologia , Piroxicam/administração & dosagem , Piroxicam/química , Piroxicam/farmacocinética , Piroxicam/uso terapêutico , Absorção Cutânea , Xilenos
16.
Molecules ; 22(12)2017 Dec 10.
Artigo em Inglês | MEDLINE | ID: mdl-29232875

RESUMO

Ultrasound-assisted extraction (UAE), using petroleum ether as the solvent, was systematically applied to extract main macamides and macaenes from Maca hypocotyls. Extraction yield was related with four variables, including ratio of solution to solid, extraction temperature, extraction time, and extraction power. On the basis of response surface methodology (RSM), the optimal conditions were determined to be the ratio of solution to solid as 10:1 (mL/g), the extraction temperature of 40 °C, the extraction time of 30 min, and the extraction power of 200 W. Based on the optimal extraction method of UAE, the total contents of ten main macamides and two main macaenes of Maca cultivated in twenty different areas of Tibet were analyzed by HPLC and UHPLC-ESI-Q-TOF-MS/MS. This study indicated that UAE was able to effectively extract macamides alkaloids from Maca hypocotyls. Quantitative analysis showed that geographical origins, not ecotypes, played a more important role on the accumulation of active macamides in Maca.


Assuntos
Lepidium/química , Extratos Vegetais/química , Cromatografia Líquida de Alta Pressão , Estrutura Molecular , Espectrometria de Massas por Ionização por Electrospray , Espectrometria de Massas em Tandem , Temperatura , Tibet
17.
Molecules ; 22(3)2017 Mar 10.
Artigo em Inglês | MEDLINE | ID: mdl-28287442

RESUMO

The present study was designed to simultaneously isolate the less polar ginsenosides from the flower buds of Panax ginseng (FBPG). Five ginsenosides, including a pair of new 20-methoxyl isomers, were extracted from FBPG and purified through a five-step integrated strategy, by combining ultrasonic extraction, Diaion Hp-20 macroporous resin column enrichment, solid phase extraction (SPE), reversed-phase high-performance liquid chromatography (RP-HPLC) analysis and preparation, and nuclear magnetic resonance (NMR) analysis. The quantification of the five ginsenosides was also discussed by a developed method with validations within acceptable limits. Ginsenoside Rg5 showed content of about 1% in FBPG. The results indicated that FBPG might have many different ginsenosides with diverse chemical structures, and the less polar ginsenosides were also important to the quality control and standardization of FBPG.


Assuntos
Flores/química , Ginsenosídeos/química , Ginsenosídeos/isolamento & purificação , Panax/química , Cromatografia Líquida de Alta Pressão , Isomerismo , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Extratos Vegetais/química , Reprodutibilidade dos Testes , Sensibilidade e Especificidade , Extração em Fase Sólida
18.
Molecules ; 21(3): 315, 2016 Mar 09.
Artigo em Inglês | MEDLINE | ID: mdl-27005606

RESUMO

In this paper, the isolation, purification and quantification of ginsenoside F5 and F3 isomeric compounds from crude extracts of flower buds of Panax ginseng (CEFBPG) was investigated by reversed-phase high-performance liquid chromatography (RP-HPLC) for the first time. The satisfied separation at analytical scale was achieved using a Zorbax Eclipse XDB C-18 column with a ternary mobile phase of acetonitrile-water-phosphoric acid (28:71:1) at a flow rate of 1.0 mL/min within 40 min. UV detection was set at 203 nm. Ginsenoside F5 and F3 was 4.21 mg and 5.13 mg in 1 g flower buds of P. ginseng (FBPG), respectively. The preparation of ginsenoside F5 and F3 at semi-preparative scale was performed by using a Daisogel C-18 column and gradient elution system of acetonitrile-water (32:68 → 28:72) at a flow rate of 10 mL/min with a sample load of 20-30 mg, and yielded ginsenosides in purity of more than 96%. Their structures were characterized by NMR and high resolution electrospray ionization mass spectrometry (HRESIMS). All the method validations showed acceptable limits. The results indicate a new source to obtain ginsenoside F5 and F3, and show that the method developed here appears to be reliable for simultaneously preparing them from CEFBPG.


Assuntos
Misturas Complexas/química , Flores/química , Ginsenosídeos/química , Panax/química , Cromatografia Líquida de Alta Pressão , Cromatografia de Fase Reversa , Ginsenosídeos/isolamento & purificação , Isomerismo , Espectroscopia de Ressonância Magnética , Espectrometria de Massas por Ionização por Electrospray , Água/química
19.
Int J Clin Exp Pathol ; 8(6): 6169-80, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-26261494

RESUMO

Polygonatum sibiricum polysaccharide (PSP) is a traditional Chinese medicine and is widely used to treat many diseases for hundreds of years conventionally. This study was to access the effects of PSP on the osteogenic differentiation of bone marrow mesenchymal stem cells (BMSCs) in the mice. Cells collected from BALB/C mice in the bone marrow were isolated and cultured with osteogenic medium (OM) with different concentrations of PSP. The proliferation and morphological changes of BMSCs were observed using an inverted microscope. Flow cytometric analysis was used to identify the BMSCs. MTT test was performed to analyze the proliferation and viability of the cells. ELISA was used to determine the expression levels of alkaline phosphatase (ALP), osteocalcin (OC), N-terminal propeptide of type I procollagen (PINP) and bone morphogenetic protein-2 (BMP-2). Immunocytochemistry and western blot were respectively used to determine the expressions of bone sialoprotein (BSP) and SPARC/osteonectin (OSN). The growth curves of the proliferation and differentiation of the Control, OM, 17ß-E2 and PSP groups were increased. Compared to the Control and OM groups, the expression levels of ALP, OC, PINP and BMP-2 were significantly increased in the PSP induced group (P<0.05). Immunocytochemistry and western blot showed that BSP and SPARC were increased after induction of PSP compared to the OM group (P<0.05). The study demonstrates that PSP promotes the proliferation and enhances the viability of BMSCs during osteogenic differentiation. Therefore, PSP may be a potential treatment of osteoporosis in the clinic.


Assuntos
Conservadores da Densidade Óssea/farmacologia , Células da Medula Óssea/efeitos dos fármacos , Diferenciação Celular/efeitos dos fármacos , Células-Tronco Mesenquimais/efeitos dos fármacos , Osteoblastos/efeitos dos fármacos , Osteogênese/efeitos dos fármacos , Extratos Vegetais/farmacologia , Polygonatum , Polissacarídeos/farmacologia , Animais , Biomarcadores/metabolismo , Conservadores da Densidade Óssea/isolamento & purificação , Células da Medula Óssea/metabolismo , Proliferação de Células/efeitos dos fármacos , Forma Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Relação Dose-Resposta a Droga , Células-Tronco Mesenquimais/metabolismo , Camundongos Endogâmicos BALB C , Osteoblastos/metabolismo , Fenótipo , Fitoterapia , Extratos Vegetais/isolamento & purificação , Plantas Medicinais , Polygonatum/química , Polissacarídeos/isolamento & purificação , Fatores de Tempo
20.
J Asian Nat Prod Res ; 14(7): 634-9, 2012.
Artigo em Inglês | MEDLINE | ID: mdl-22582827

RESUMO

A new natural product, 10-hydroxyrutaecarpine (1), and a rarely new glycosidic alkaloid, rutaecarpine-10-O-rutinoside (2), along with the known compounds rutaecarpine (3), evodiamine, wuzhuyuamide-I, and dehydroevodiamine were isolated from the butanol fraction of 70% ethanol aqueous extract of the dried and nearly ripe fruits of Euodia rutaecarpa (Juss.) Benth. Their structures were elucidated on the basis of their spectroscopic data.


Assuntos
Medicamentos de Ervas Chinesas/isolamento & purificação , Evodia/química , Alcaloides Indólicos/isolamento & purificação , Quinazolinas/isolamento & purificação , Alcaloides , Medicamentos de Ervas Chinesas/química , Frutas/química , Alcaloides Indólicos/química , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Quinazolinas/química
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