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1.
Zhongguo Zhong Yao Za Zhi ; 49(2): 412-419, 2024 Jan.
Artigo em Chinês | MEDLINE | ID: mdl-38403317

RESUMO

Thirteen compounds were isolated and identified from 70% ethanol extract of the roots of Gentiana macrophylla by multi-chromatographic methods, including microporous resin, silica gel, and C_(18) reversed-phase column chromatography, as well as HPLC as follows: macrophylloside G(1), macrophylloside D(2), 5-formyl-2,3-dihydroisocoumarin(3),(+)-medicarpin(4),(+)-syringaresinol(5), liquiritigenin(6),(3R)-sativanone(7),(3R)-3'-O-methylviolanone(8), 4,2',4'-trihydroxychalcone(9), latifolin(10), gentioxepine(11), 6α-hydroxycyclonerolidol(12), and ethyl linoleate(13). Compound 1 was a new benzopyran glycoside. Compounds 4, 6-10, 12, and 13 were isolated for the first time from Gentiana plants. Compounds 1 and 2 showed promising hepatoprotective activity against D-GalN-induced AML12 cell damage at the concentration of 10 µmol·L~(-1), and compound 2 exhibited more significant activity than silybin at the same concentration.


Assuntos
Glicosídeos Cardíacos , Éteres , Gentiana , Gentiana/química , Glicosídeos/farmacologia , Benzopiranos , Glucosídeos
2.
Chin J Nat Med ; 22(2): 161-170, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-38342568

RESUMO

Our continued works on the chemical constituents of Ginkgo biloba (G. biloba) leaves has led to the isolation of two novel phenylbutenoids (1, 2), along with five previously unidentified terpene glycosides (3-7). Among them, compounds 1 and 2 represent unique (Z)-phenylbutenoids, 3-6 are megastigmane glycosides, and 7 is identified as a rare bilobanone glycoside (Fig. 1). This study marks the first reported isolation of phenylbutenoid and bilobanone glycoside from G. biloba. The chemical structures of these compounds were elucidated through extensive spectroscopic analysis, including HR-ESI-MS and various 1D and 2D NMR experiments. Furthermore, the absolute configurations of these molecules were determined using Mosher's method, ECD experiments, and Cu-Kα X-ray crystallographic analyses.


Assuntos
Glicosídeos Cardíacos , Glicosídeos , Glicosídeos/química , Ginkgo biloba/química , Terpenos/química , Folhas de Planta/química , Extratos Vegetais/química
3.
Neuroscience ; 541: 77-90, 2024 Mar 16.
Artigo em Inglês | MEDLINE | ID: mdl-38278474

RESUMO

Synapse formation following the generation of postsynaptic dendritic spines is essential for motor learning and functional recovery after brain injury. The C-terminal fragment of agrin cleaved by neurotrypsin induces dendritic spine formation in the adult hippocampus. Since the α3 subunit of sodium-potassium ATPase (Na/K ATPase) is a neuronal receptor for agrin in the central nervous system, cardiac glycosides might facilitate dendritic spine formation and subsequent improvements in learning. This study investigated the effects of cardiac glycoside digoxin on dendritic spine turnover and learning performance in mice. Golgi-Cox staining revealed that intraperitoneal injection of digoxin less than its IC50 in the brain significantly increased the density of long spines (≥2 µm) in the cerebral cortex in wild-type mice and neurotrypsin-knockout (NT-KO) mice showing impairment of activity-dependent spine formation. Although the motor learning performance of NT-KO mice was significantly lower than control wild-type mice under the control condition, low doses of digoxin enhanced performance to a similar degree in both strains. In NT-KO mice, lower digoxin doses equivalent to clinical doses also significantly improved motor learning performance. These data suggest that lower doses of digoxin could modify dendritic spine formation or recycling and facilitate motor learning in compensation for the disruption of neurotrypsin-agrin pathway.


Assuntos
Glicosídeos Cardíacos , Espinhas Dendríticas , Camundongos , Animais , Espinhas Dendríticas/metabolismo , Digoxina/farmacologia , Agrina , Camundongos Knockout , Adenosina Trifosfatases
4.
Phytochemistry ; 219: 113990, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38219854

RESUMO

Ten undescribed cardiac glycosides, strasperosides A-J, together with twelve known analogues, were isolated from Streblus asper Lour. Their structures were elucidated on the basis of spectroscopic analysis, electronic circular dichroism data, and chemical methods. These cardiac glycosides showed diversity in steroid skeleton and sugar moiety. Strasperosides A and B are a pair of unusual stereoisomers featuring different orientation of the lactone motif. Ten cardiac glycosides demonstrated potent antiviral effects on HSV-1 in vitro with the IC50 values from 0.19 ± 0.08 to 1.03 ± 0.25 µM and the therapeutic indices from 66.61 ± 5.08 to 326.75 ± 11.75.


Assuntos
Glicosídeos Cardíacos , Moraceae , Glicosídeos Cardíacos/farmacologia , Glicosídeos Cardíacos/química , Extratos Vegetais/química , Moraceae/química , Antivirais/química , Glicosídeos/farmacologia
5.
Int J Mol Sci ; 25(2)2024 Jan 19.
Artigo em Inglês | MEDLINE | ID: mdl-38279268

RESUMO

Nymphoides peltata has been used as a medicinal herb in traditional medicines to treat strangury, polyuria, and swelling. The phytochemical investigation of the MeOH extract of N. peltata roots led to the isolation of three iridoid glycosides and three coumarin glycoside derivatives, which were characterized as menthiafolin (1), threoninosecologanin (2), callicoside C (3), and scopolin (4), as well as two undescribed peltatamarins A (5) and B (6). The chemical structures of the undescribed compounds were determined by analyzing their 1 dimensional (D) and 2D nuclear magnetic resonance (NMR) spectra and using high-resolution (HR)-electrospray ionization mass spectroscopy (ESI-MS), along with the chemical reaction of acid hydrolysis. The wound healing activities of the isolated compounds 1-6 were evaluated using a HaCaT cell scratch test. Among the isolates, scopolin (4) and peltatamarin A (5) promoted HaCaT cell migration over scratch wounds, and compound 5 was the most effective. Furthermore, compound 5 significantly promoted cell migration without adversely affecting cell proliferation, even when treated at a high dose (100 µM). Our results demonstrate that peltatamarin A (5), isolated from N. peltata roots, has the potential for wound healing effects.


Assuntos
Glicosídeos Cardíacos , Magnoliopsida , Plantas Medicinais , Glicosídeos/farmacologia , Glicosídeos/química , Glicosídeos Iridoides/química , Cicatrização , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Cumarínicos/farmacologia
6.
Nat Prod Res ; 38(5): 759-767, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-37005002

RESUMO

Four new glycosides, named amplexicosides A-D (1-4), and five known compounds: benzyl 2-[ß-D-glucopyranosyl-(1→6)-ß-D-glucopyranosyloxy]-benzoate (5), benzyl 2-neohesperidosyloxy-6-hydroxybenzoate (6), chrysandroside A (7), chrysandroside B (8) and camelliquercetiside C (9) were isolated from the branches and leaves of Camellia amplexicaulis (Pit.) Cohen-Stuart. Their structures were elucidated using HR-ESI-MS and 1D- and 2D-NMR spectra and compared to reported NMR data. All of the isolated compounds were screened in an α-glucosidase assay. Compounds 4, 8, and 9 significantly inhibited α-glucosidase with respective IC50 values of 254.9 ± 4.2, 304.8 ± 11.9 and 228.1 ± 16.4 µM.


Assuntos
Camellia , Glicosídeos Cardíacos , Glicosídeos/farmacologia , Glicosídeos/química , alfa-Glucosidases , Estrutura Molecular , Inibidores de Glicosídeo Hidrolases/farmacologia , Inibidores de Glicosídeo Hidrolases/química
7.
Nat Prod Res ; 38(6): 1016-1023, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-37194669

RESUMO

A novel bioactive flavan glycoside was isolated by solvent extraction method with the help of Soxhlet apparatus from the methanolic extract of Tradescantia spathacea Sw. Flavan glycoside having molecular formula C20H22O10, melting point 175-1780C, molecular weight by ESI-MS m/z (M + H]+ 423, optical rotation was[α]21D-45.1(c 0.20 methanol). Its structure was determined (-)-epicatechin 7-O-alpha-L-arabinopyranoside. Various color reactions, chemical degradation (like acid hydrolysis, permethylation, and enzymatic hydrolysis), UV-Visible spectrophotometry, Fourier transforms infrared spectroscopy, electrospray ionization mass spectrometry, and nuclear magnetic resonance spectroscopy were used to establish the structure of compound (-)-(-)-epicatechin 7-O-alpha-L-arabinopyranoside.. A flavan glycoside was also tested with a DPPH assay method for antioxidant activity by using Ascorbic acid as standard. DPPH radical scavenging test data demonstrate that a flavan glycoside possesses potent antioxidant activity so this flavan glycoside can be utilized as a potent antioxidant agent.


Assuntos
Glicosídeos Cardíacos , Catequina , Commelinaceae , Tradescantia , Antioxidantes/farmacologia , Glicosídeos/química , Extratos Vegetais/química , Espectrometria de Massas por Ionização por Electrospray
8.
Leukemia ; 38(1): 67-81, 2024 01.
Artigo em Inglês | MEDLINE | ID: mdl-37904054

RESUMO

Myelomonocytic and monocytic acute myeloid leukemia (AML) subtypes are intrinsically resistant to venetoclax-based regimens. Identifying targetable vulnerabilities would limit resistance and relapse. We previously documented the synergism of venetoclax and cardiac glycoside (CG) combination in AML. Despite preclinical evidence, the repurposing of cardiac glycosides (CGs) in cancer therapy remained unsuccessful due to a lack of predictive biomarkers. We report that the ex vivo response of AML patient blasts and the in vitro sensitivity of established cell lines to the hemi-synthetic CG UNBS1450 correlates with the ATPase Na+/K+ transporting subunit alpha 1 (ATP1A1)/BCL2 like 1 (BCL2L1) expression ratio. Publicly available AML datasets identify myelomonocytic/monocytic differentiation as the most robust prognostic feature, along with core-binding factor subunit beta (CBFB), lysine methyltransferase 2A (KMT2A) rearrangements, and missense Fms-related receptor tyrosine kinase 3 (FLT3) mutations. Mechanistically, BCL2L1 protects from cell death commitment induced by the CG-mediated stepwise triggering of ionic perturbation, protein synthesis inhibition, and MCL1 downregulation. In vivo, CGs showed an overall tolerable profile while impacting tumor growth with an effect ranging from tumor growth inhibition to regression. These findings suggest a predictive marker for CG repurposing in specific AML subtypes.


Assuntos
Glicosídeos Cardíacos , Leucemia Mieloide Aguda , Humanos , Leucemia Mieloide Aguda/tratamento farmacológico , Leucemia Mieloide Aguda/genética , Leucemia Mieloide Aguda/patologia , Compostos Bicíclicos Heterocíclicos com Pontes/farmacologia , Sulfonamidas/farmacologia , Tirosina Quinase 3 Semelhante a fms/metabolismo , Linhagem Celular Tumoral , ATPase Trocadora de Sódio-Potássio/metabolismo , ATPase Trocadora de Sódio-Potássio/uso terapêutico , Proteína bcl-X/metabolismo
9.
J Biochem ; 175(3): 253-263, 2024 Mar 04.
Artigo em Inglês | MEDLINE | ID: mdl-37948630

RESUMO

Cardiac glycosides (CGs) have been used for decades to treat heart failure and arrhythmic diseases. Recent non-clinical and epidemiological findings have suggested that CGs exhibit anti-tumor activities. Therefore, CGs may be repositioned as drugs for the treatment of cancer. A detailed understanding of the anti-cancer mechanisms of CGs is essential for their application to the treatment of targetable cancer types. To elucidate the factors associated with the anti-tumor effects of CGs, we performed transcriptome profiling on human multiple myeloma AMO1 cells treated with periplocin, one of the CGs. Periplocin significantly down-regulated the transcription of MYC (c-Myc), a well-established oncogene. Periplocin also suppressed c-Myc expression at the protein levels. This repression of c-Myc was also observed in several cell lines. To identify target proteins for the inhibition of c-Myc, we generated CG-resistant (C9) cells using a sustained treatment with digoxin. We confirmed that C9 cells acquired resistance to the inhibition of c-Myc expression and cell proliferation by CGs. Moreover, the sequencing of genomic DNA in C9 cells revealed the mutation of D128N in α1-Na/K-ATPase, indicating the target protein. These results suggest that CGs suppress c-Myc expression in cancer cells via α1-Na/K-ATPase, which provides further support for the anti-tumor activities of CGs.


Assuntos
Glicosídeos Cardíacos , Humanos , Glicosídeos Cardíacos/farmacologia , Linhagem Celular , Proliferação de Células , Perfilação da Expressão Gênica , Adenosina Trifosfatases
10.
Fitoterapia ; 172: 105740, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-37939734

RESUMO

Three new phenolic glycosides (1-3) and a new lignan glycoside (4), together with five known compounds (5-9) were isolated from the ethanol extract of the aerial part of Gaultheria leucocarpa var. yunnanensis (Franch.) T.Z.Hsu & R.C.Fang. Their structures were determined on the basis of spectroscopic techniques, experimental and calculated ECD spectra, acid hydrolysis, and enzymatic hydrolysis experiments. All the isolates were evaluated for their anti-inflammatory and antioxidant activities. Compounds 7 and 8 exhibited inhibitory effects against the LPS-induced production of NO with IC50 of 63.71 and 10.66 µM, respectively, compared to L-NMMA having an IC50 of 6.95 µM. Besides, compound 7 also represented significant DPPH radical scavenging activity with EC50 of 18.75 µM, comparable with vitamin C (EC50 = 15.77 µM).


Assuntos
Glicosídeos Cardíacos , Gaultheria , Lignanas , Glicosídeos/química , Lignanas/farmacologia , Gaultheria/química , Estrutura Molecular , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química
11.
Nat Prod Res ; 38(1): 10-15, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-35862620

RESUMO

Phytochemical investigation of methanolic extract of L. rubiginosa using modern chromatographic techniques has led to the isolation of three new triterpenoid saponins, lepiginosides A-C (1-3), a new farnesyl glycoside, lepiginoside D (4), together with lepisantheside B (5) and gleditsoside C (6). The characterization and structural elucidation of the isolated compounds were established by extensive spectroscopic data analysis and comparison with literature data. Moreover, the antibacterial activity against seven bacteria, but none is active.


Assuntos
Glicosídeos Cardíacos , Sapindaceae , Saponinas , Triterpenos , Glicosídeos/farmacologia , Saponinas/química , Sapindaceae/química , Triterpenos/química , Estrutura Molecular
12.
Nat Prod Res ; 38(1): 43-51, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-35876051

RESUMO

Phytochemical investigation of Bignonia binata leaves led to the isolation of three new compounds: including a glycoside of simple alcohol, namely binatoside (2), 3,4-dihydroxy-N-methyl piperidin-2-one (7), and a phenyl ethanoid glycoside, namely bignanoside C (8), alongside with five known compounds; including a glycoside of simple alcohol; (2S) propane-1,2-diol 1-O-(6-O-caffeoy1)-ß-D-glucopyranoside (1), phenyl ethanoids; leucosceptoside A (3) and plantainoside C (4), and iridoids; ipolamiide (5) and strictoloside (6). The structure of the isolated compounds was elucidated by various spectroscopic methods, including 1 D and 2 D NMR experiments, HR-ESI-MS as well as by comparison with the literature.


Assuntos
Bignoniaceae , Glicosídeos Cardíacos , Glicosídeos/química , Espectroscopia de Ressonância Magnética , Folhas de Planta/química , Bignoniaceae/química , Estrutura Molecular
13.
Nat Prod Res ; 38(1): 146-151, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-35879853

RESUMO

A new megastigmane glycoside, (1R,5R,6S,7E)-megastigman-3,9-dione-7-en-6,11-diol 11-O-ß-D-glucopyranoside (1), and a new organic acid glycoside, methyl (4 R)-4-O-ß-D-glucopyranosyl-decanoate (2), together with eight known compounds (3-10), were isolated from the aerial parts of Artemisia halodendron Turcz. ex Bess. (Asteraceae). Their chemical structures were elucidated by 1 D and 2 D NMR and HR-ESI-MS spectra and DP4+ probability analysis. Among the identified compounds, compounds 5, 6 and 10 were isolated from the family Asteraceae, and compounds 3, 4 and 7-9 were identified from the genus Artemisia for the first time. All of the compounds were evaluated for their anticomplementary activity against the classical pathway (CP) and the alternative pathway (AP). Compounds 7 and 9 showed anticomplementary activity with the CH50 values of 0.31 ± 0.08 and 0.50 ± 0.09 mM, respectively.


Assuntos
Artemisia , Glicosídeos Cardíacos , Glicosídeos/farmacologia , Glicosídeos/química , Artemisia/química , Norisoprenoides/farmacologia , Norisoprenoides/química , Glucosídeos/química , Estrutura Molecular
14.
Virology ; 589: 109915, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-37931588

RESUMO

A small molecule screen identified several cardiotonic steroids (digitoxin and ouabain) and the ionophore monensin as potent inhibitors of HCoV-229E, HCoV-OC43, and SARS-CoV-2 replication with EC50s in the low nM range. Subsequent tests confirmed antiviral activity in primary cell models including human nasal epithelial cells and lung organoids. Addition of digitoxin, ouabain, or monensin strongly reduced viral gene expression as measured by both viral protein and RNA accumulation. Furthermore, the compounds acted post virus entry. While the antiviral activity of digitoxin was dependent upon activation of the MEK and JNK signaling pathways but not signaling through GPCRs, the antiviral effect of monensin was reversed upon inhibition of several signaling pathways. Together, the data demonstrates the potent anti-coronavirus properties of two classes of FDA approved drugs that function by altering the properties of the infected cell, rendering it unable to support virus replication.


Assuntos
Glicosídeos Cardíacos , Coronavirus Humano 229E , Humanos , Glicosídeos Cardíacos/farmacologia , Monensin/farmacologia , Ouabaína/farmacologia , Digitoxina/farmacologia , Antivirais/farmacologia
15.
Int Immunopharmacol ; 127: 111368, 2024 Jan 25.
Artigo em Inglês | MEDLINE | ID: mdl-38103408

RESUMO

Zika virus (ZIKV) is a mosquito-borne virus first reported from humans in Nigeria in 1954. The first outbreak occurred in Micronesia followed by an outbreak in French Polynesia and another in Brazil when the virus was associated with numerous cases of severe neurological manifestations such as Guillain-Barre syndrome in adults and congenital zika syndrome in fetuses, particularly congenital microcephaly. Innate immunity is the first line of defense against ZIKV through triggering an antiviral immune response. Along with innate immune responses, a sufficient balance between anti- and pro-inflammatory cytokines and the amount of these cytokines are triggered to enhance the antiviral responses. Here, we reviewed the complex interplay between the mediators and signal pathways that coordinate antiviral immune response and inflammation as a key to understanding the development of the underlying diseases triggered by ZIKV. In addition, we summarize current and new therapeutic strategies for ZIKV infection, highlighting cardiotonic steroids as antiviral drugs for the development of this agent.


Assuntos
Glicosídeos Cardíacos , Infecção por Zika virus , Zika virus , Adulto , Animais , Humanos , Infecção por Zika virus/tratamento farmacológico , Infecção por Zika virus/epidemiologia , Inflamação/tratamento farmacológico , Inflamação/complicações , Imunidade Inata , Citocinas , Antivirais/uso terapêutico
16.
Int J Mol Sci ; 24(23)2023 Dec 04.
Artigo em Inglês | MEDLINE | ID: mdl-38069442

RESUMO

The flavonoid glycoside apiin (apigenin 7-O-[ß-D-apiosyl-(1→2)-ß-D-glucoside]) is abundant in apiaceous and asteraceous plants, including celery and parsley. Although several enzymes involved in apiin biosynthesis have been identified in celery, many of the enzymes in parsley (Petroselinum crispum) have not been identified. In this study, we identified parsley genes encoding the glucosyltransferase, PcGlcT, and the apiosyltransferase, PcApiT, that catalyze the glycosylation steps of apiin biosynthesis. Their substrate specificities showed that they were involved in the biosynthesis of some flavonoid 7-O-apiosylglucosides, including apiin. The expression profiles of PcGlcT and PcApiT were closely correlated with the accumulation of flavonoid 7-O-apiosylglucosides in parsley organs and developmental stages. These findings support the idea that PcGlcT and PcApiT are involved in the biosynthesis of flavonoid 7-O-apiosylglucosides in parsley. The identification of these genes will elucidate the physiological significance of apiin and the development of apiin production methods.


Assuntos
Apium , Glicosídeos Cardíacos , Glicosídeos/química , Petroselinum/química , Glicosiltransferases/genética , Flavonoides/química
17.
Cells ; 12(24)2023 12 11.
Artigo em Inglês | MEDLINE | ID: mdl-38132136

RESUMO

Inflamed and infected tissues can display increased local sodium (Na+) levels, which can have various effects on immune cells. In macrophages, high salt (HS) leads to a Na+/Ca2+-exchanger 1 (NCX1)-dependent increase in intracellular Na+ levels. This results in augmented osmoprotective signaling and enhanced proinflammatory activation, such as enhanced expression of type 2 nitric oxide synthase and antimicrobial function. In this study, the role of elevated intracellular Na+ levels in macrophages was investigated. Therefore, the Na+/K+-ATPase (NKA) was pharmacologically inhibited with two cardiac glycosides (CGs), ouabain (OUA) and digoxin (DIG), to raise intracellular Na+ without increasing extracellular Na+ levels. Exposure to HS conditions and treatment with both inhibitors resulted in intracellular Na+ accumulation and subsequent phosphorylation of p38/MAPK. The CGs had different effects on intracellular Ca2+ and K+ compared to HS stimulation. Moreover, the osmoprotective transcription factor nuclear factor of activated T cells 5 (NFAT5) was not upregulated on RNA and protein levels upon OUA and DIG treatment. Accordingly, OUA and DIG did not boost nitric oxide (NO) production and showed heterogeneous effects toward eliminating intracellular bacteria. While HS environments cause hypertonic stress and ionic perturbations, cardiac glycosides only induce the latter. Cotreatment of macrophages with OUA and non-ionic osmolyte mannitol (MAN) partially mimicked the HS-boosted antimicrobial macrophage activity. These findings suggest that intracellular Na+ accumulation and hypertonic stress are required but not sufficient to mimic boosted macrophage function induced by increased extracellular sodium availability.


Assuntos
Anti-Infecciosos , Glicosídeos Cardíacos , Humanos , Sódio/metabolismo , Glicosídeos Cardíacos/farmacologia , Ouabaína/farmacologia , Macrófagos/metabolismo , Cloreto de Sódio/farmacologia , Cloreto de Sódio na Dieta , Cafeína/farmacologia , Anti-Infecciosos/farmacologia , Anti-Infecciosos/metabolismo
18.
Zhongguo Zhong Yao Za Zhi ; 48(22): 6058-6065, 2023 Nov.
Artigo em Chinês | MEDLINE | ID: mdl-38114212

RESUMO

The poor solubility of insoluble components of traditional Chinese medicine(TCM) is an important factor restricting the development of its preparations. Natural polysaccharides of TCM can be used as functional components to increase the solubility of insoluble components. Epimedium flavonoid secondary glycoside components(EFSGC) have been shown to have positive effects on the prevention and treatment of osteoporosis, but they exhibit poor solubility. Therefore, the strategy of solubilizing EFSGC with TCM polysaccharides was adopted, and its effect on the permeability and stability of EFSGC was evaluated in this study. Based on the equilibrium solubility experiment of EFSGC, it was found that Panax notoginseng crude polysaccharide(PNCP) had the best solubilization effect on EFSGC among the ten kinds of TCM polysaccharides, which increased the solubility of EFSGC from 0.8 mg·mL~(-1) to 13.3 mg·mL~(-1). It should be noted that after the solubilization of EFSGC by preparation technology, the effects on permeability and stability should be considered. Therefore, this study also investigated these two properties. The results showed that PNCP increased the effective transmittance of EFSGC from 50.5% to 71.1%, which could increase the permeability of EFSGC significantly. At the same time, it could improve the stability of EFSGC in the simulated gastric juice environment. In order to explain the solubilization mechanism of PNCP on EGSGC, critical micelle concentration, particle size, potential, differential scanning calorimetry, and infrared spectroscopy were analyzed. It was preliminarily inferred that the mechanism was as follows: PNCP and EFSGC could self-assemble into aggregates for solubilization by intermolecular hydrogen bonding interaction in water. In summary, PNCP can not only improve the solubility of EFSGC but also improve its permeability and stability. This study lays the foundation for the application of TCM polysaccharides as a functional component to solubilize insoluble components.


Assuntos
Glicosídeos Cardíacos , Epimedium , Medicina Tradicional Chinesa , Flavonoides/química , Glicosídeos , Epimedium/química , Solubilidade , Polissacarídeos/química
19.
Arh Hig Rada Toksikol ; 74(4): 292-295, 2023 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-38146758

RESUMO

Natural cardiac glycosides have positive inotropic heart effects but at high, toxic doses they can cause life-threatening cardiac arrhythmias. Here we present the first Croatian case of a 16-year-old girl who attempted suicide by eating dried oleander leaves, which contain natural cardiac glycosides, and her treatment with a specific antidote. The girl presented with an oedema of the uvula indicating local toxicity, severe bradycardia, first-degree atrioventricular block, drowsiness, and vomiting. Having taken her medical history, we started treatment with atropine, intravenous infusion of dextrose-saline solution and gastroprotection, but it was not successful. Then we introduced digoxin-specific Fab antibody fragments and within two hours, the patient's sinus rhythm returned to normal. Cases of self-poisoning with this oleander are common in South-East Asia, because it is often used as a medicinal herb, and digoxin-specific Fab fragments have already been reported as effective antidote against oleander poisoning there. Our case has taught us that it is important to have this drug in the hospital pharmacy both for digitalis and oleander poisoning.


Assuntos
Glicosídeos Cardíacos , Nerium , Intoxicação por Plantas , Humanos , Feminino , Adolescente , Tentativa de Suicídio , Antídotos/uso terapêutico , Digoxina/uso terapêutico , Glicosídeos Cardíacos/uso terapêutico , Intoxicação por Plantas/tratamento farmacológico , Intoxicação por Plantas/etiologia , Fragmentos Fab das Imunoglobulinas/uso terapêutico , Ingestão de Alimentos
20.
Nihon Yakurigaku Zasshi ; 158(6): 465-468, 2023.
Artigo em Japonês | MEDLINE | ID: mdl-37914325

RESUMO

Na+,K+-ATPases are essential for maintaining the membrane potential in almost all cells, and their catalytic subunits have four isoforms (α1-α4). Volume-regulated anion channel (VRAC) plays an important role in the cell death signaling pathway in addition to its fundamental role in cell volume maintenance. First, we introduce that disruption of actin filaments cause the dysfunction of VRAC, which elicits resistance to cisplatin in the cancer cells. Next, we summarize the cardiac glycosides-induced signaling pathway mediated by the crosstalk between Na+,K+-ATPase α1-isoform (α1NaK) and VRAC in the membrane microdomain of the cancer cells. In this mechanism, sub-micromolar concentrations of cardiac glycosides bind to the receptor-type α1NaK, and generate VRAC activities concomitantly with a deceleration of cancer cell proliferation. Finally, we summarize the pathophysiological function of α3NaK, which is abnormally expressed in the intracellular vesicles of cancer cells. The cancer cell can survive even under loss of anchorage because they have the avoidance mechanism for anoikis. On cancer cell detachment, we found that intracellular α3NaK is translocated to the plasma membrane and this event contributes to the survival of the cells. Interestingly, cardiac glycosides inhibited the α3NaK translocation and cell survival. Our findings may open up new opportunities for the development of cancer medicines.


Assuntos
Glicosídeos Cardíacos , Neoplasias , Humanos , ATPase Trocadora de Sódio-Potássio/metabolismo , Glicosídeos Cardíacos/farmacologia , Membrana Celular , Íons/metabolismo , Transdução de Sinais , Neoplasias/tratamento farmacológico , Neoplasias/metabolismo
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