RESUMO
OBJECTIVE@#To observe the effect of amygdalin on liver fibrosis in a liver fibrosis mouse model, and the underlying mechanisms were partly dissected in vivo and in vitro.@*METHODS@#Thirty-two male mice were randomly divided into 4 groups, including control, model, low- and high-dose amygdalin-treated groups, 8 mice in each group. Except the control group, mice in the other groups were injected intraperitoneally with 10% carbon tetrachloride (CCl4)-olive oil solution 3 times a week for 6 weeks to induce liver fibrosis. At the first 3 weeks, amygdalin (1.35 and 2.7 mg/kg body weight) were administered by gavage once a day. Mice in the control group received equal quantities of subcutaneous olive oil and intragastric water from the fourth week. At the end of 6 weeks, liver tissue samples were harvested to detect the content of hydroxyproline (Hyp). Hematoxylin and eosin and Sirius red staining were used to observe the inflammation and fibrosis of liver tissue. The expressions of collagen I (Col-I), alpha-smooth muscle actin (α-SMA), CD31 and transforming growth factor β (TGF-β)/Smad signaling pathway were observed by immunohistochemistry, quantitative real-time polymerase chain reaction and Western blot, respectively. The activation models of hepatic stellate cells, JS-1 and LX-2 cells induced by TGF-β1 were used in vitro with or without different concentrations of amygdalin (0.1, 1, 10 µmol/L). LSECs. The effect of different concentrations of amygdalin on the expressions of liver sinusoidal endothelial cells (LSECs) dedifferentiation markers CD31 and CD44 were observed.@*RESULTS@#High-dose of amygdalin significantly reduced the Hyp content and percentage of collagen positive area, and decreased the mRNA and protein expressions of Col-I, α-SMA, CD31 and p-Smad2/3 in liver tissues of mice compared to the model group (P<0.01). Amygdalin down-regulated the expressions of Col-I and α-SMA in JS-1 and LX-2 cells, and TGFβ R1, TGFβ R2 and p-Smad2/3 in LX-2 cells compared to the model group (P<0.05 or P<0.01). Moreover, 1 and 10 µmol/L amygdalin inhibited the mRNA and protein expressions of CD31 in LSECs and increased CD44 expression compared to the model group (P<0.05 or P<0.01).@*CONCLUSIONS@#Amygdalin can dramatically alleviate liver fibrosis induced by CCl4 in mice and inhibit TGF-β/Smad signaling pathway, consequently suppressing HSCs activation and LSECs dedifferentiation to improve angiogenesis.
Assuntos
Ratos , Masculino , Camundongos , Animais , Fator de Crescimento Transformador beta/metabolismo , Amigdalina/uso terapêutico , Células Endoteliais/metabolismo , Azeite de Oliva/uso terapêutico , Ratos Wistar , Proteínas Smad/metabolismo , Cirrose Hepática/metabolismo , Fígado , Fator de Crescimento Transformador beta1/metabolismo , Transdução de Sinais , Colágeno Tipo I/metabolismo , Tetracloreto de Carbono , Células Estreladas do FígadoRESUMO
This study focused on the separation, characterization, content determination, and antiviral efficacy research on colloidal particles with different sizes in Maxing Shigan Decoction(MXSG). The mixed colloidal phase of MXSG was initially separated into small colloidal particle segment(S), medium colloidal particle segment(M), and big colloidal particle segment(B) using ultrafiltration. Further fine separation was performed using size-exclusion chromatography. Dynamic light scattering(DLS) and transmission electron microscopy(TEM) were employed to characterize the size and morphology of the separated colloidal particles. UPLC-MS/MS was used to determine the content of ephedrine, amygdalin, glycyrrhizic acid, and the EDTA complexometric titration was used to measure the calcium(Ca~(2+)) content in different colloidal phases. Finally, a respiratory syncytial virus(RSV) infection mouse model was established using intranasal administration. The experimental groups included a blank group, a model group, a ribavirin group, an MXSG group, an S group, an M group, and a B group. Oral administration was given for treatment, and pathological changes in mouse lung tissue and organ indices were evaluated. The results of the study showed that the distribution of ephedrine, amygdalin, glycyrrhizic acid, and Ca~(2+) content was not uniform among different colloidal segments. Among them, the B segment had the highest proportions of the three components, except for Ca~(2+), accounting for 46.35%, 53.72%, and 92.36%, respectively. Size-exclusion chromatography separated colloidal particles with uniform morphology in the size range of 100-500 nm. Compared to the S and M segments, the B segment showed an increased lung index inhibition rate(38.31%), spleen index, and thymus index in RSV-infected mice, and it improved the infiltration of inflammatory cells and lung injury in the lung tissue of mice. The complex components in MXSG form colloidal particles of various sizes and morphologies through heating, and small-molecule active components such as ephedrine, amygdalin, glycyrrhizic acid, and Ca~(2+) participate in the assembly to varying degrees. The main material basis for the antiviral effect of MXSG is the colloidal particles with certain particle sizes formed by the assembly of active components during the heating process.
Assuntos
Camundongos , Animais , Amigdalina/química , Medicamentos de Ervas Chinesas/química , Ácido Glicirrízico/análise , Efedrina/análise , Cromatografia Líquida , Espectrometria de Massas em Tandem , Antivirais/farmacologiaRESUMO
Abstract Trichinellosis is a zoonosis results from eating raw or semi-cooked meat of infected animals. Medicinal plants have been used lately as alternatives and/or combined therapies to resolve some drawbacks of the current regimens. This work analyzed the effect of albendazole monotherapy on Trichinella spiralis experimental infection (group A), in comparison to P. granatum and amygdalin extracts +cobalamin (group B), plus its combination with albendazole (group C). The study revealed that the extracts alone or combined with albendazole had an inferior effect to albendazole monotherapy regarding number of adult worms (40.83 ±3.82, 18.67 ±1.86 and 16.83 ±2.32, respectively). However, their effect was more obvious in muscle phase combined with albendazole, achieving the lower number of larvae/mL tissue homogenate (22.33 ±3.27 in comparison to 39.67 ±2.58 achieved by albendazole monotherapy). The extracts exerted a significant immunomodulatory effect by reducing the local CD4+ expression in the intestine as well as in muscle phase (1.15 ±0.25 and 3.80 ±0.65 in comparison to 4.97 ±0.37 and 12.20 ±0.87 with albendazole monotherapy, respectively). So, these extracts improved the therapeutic efficacy of albendazole, specifically in muscle phase and counteracted the inflammatory reaction caused by albendazole monotherapy, thus extensively alleviating the resulting myositis.
Resumo Trichinellosis é uma zoonose resultante da ingestão de carne crua ou semicozida de animais infectados. As plantas medicinais têm sido usadas, ultimamente, como alternativas e/ou terapias combinadas, para resolver algumas desvantagens dos regimes atuais. Este trabalho analisou o efeito da monoterapia albendazole na infecção experimental por Trichinella spiralis (grupo A), em comparação com extratos de P. granatum e amígdalina +cobalamina (grupo B), além de sua combinação com albendazol (grupo C). O estudo revelou que os extratos sozinho ou combinado com albendazol teve efeito inferior à monoterapia albendazol em relação ao número de vermes adultos (40,83 ±3,82, 18,67 ±1,86 e 16,83 ±2,32, respectivamente). No entanto, seu efeito foi mais óbvio na fase muscular combinado com o albendazol, alcançando o menor número de larvas/mL homogeneizado de tecido (22,33 ±3,27 em comparação com 39,67 ±2,58 obtidos pela monoterapia albendazol). Os extratos exerceram um efeito imunomodulatório significativo, ao reduzir a expressão local CD4+ no intestino, bem como na fase muscular (1,15 ±0,25 e 3,80 ±0,65 em comparação com 4,97 ±0,37 e 12,20 ±0,87 com monoterapia albendazol, respectivamente). Assim, esses extratos melhoraram a eficácia terapêutica do albendazol, especificamente na fase muscular e neutralizaram a reação inflamatória causada pela monoterapia albendazol, aliviando extensivamente a miosite resultante.
Assuntos
Animais , Triquinelose/tratamento farmacológico , Triquinelose/veterinária , Trichinella spiralis , Punica granatum , Amigdalina , Miosite/veterinária , Vitamina B 12 , Extratos Vegetais , Albendazol , Modelos Animais de Doenças , LarvaRESUMO
To discuss the effect of deterioration on the quality of Armeniacae Semen Amarum by observing the changes of macroscopic characteristics, active components and rancidness degrees of Armeniacae Semen Amarum in deterioration process. The traditional macroscopic identification was used to observe, identify and classify the morphologic and organleptic characteristics of Armeniacae Semen Amarum. The contents of amygdalin and fatty oil(two representatives of active components) were detected by HPLC and general rule 0713 in Chinese Pharmacopoeia, respectively. Acid value and peroxide value of the samples were selected as the representative indices of different rancidness degrees, and the general rule 2303 was adopted as the method for quantitative analysis. Then principal component analysis(PCA), partial least square analysis discrimination analysis(PLS-DA) were further utilized to establish the discriminative models of samples with different rancidness degrees, and also to screen out the largest contribution factors. In sensory evaluation, Armeniacae Semen Amarum samples were divided into three groups: non-rancid, slightly-rancid, and noticeably-rancid. The color of seed coat, cotyledon and surface of noticeably-rancid samples was deepened, and the odor differed much from non-rancid samples. Average content of amygdalin and fatty oil in non-rancid samples was 4.12% and 67.77%, respectively, both meeting the requirements of Chinese Pharmacopoeia; and decreased to some extent in slightly-rancid samples. However, the content of amygdalin sharply dropped to 0.074% in noticeably-rancid samples. The acid value and peroxide value were increased significantly with the intensifying of the rancidness degree, from only 1.363 and 0.016 74 in non-rancid samples to 1.865 and 0.023 70 in slightly-rancid samples, even doubled in noticeably-rancid samples(2.167 and 0.033 82). The discriminative models established by PCA and PLS-DA could complete the task of distinguishing the non-rancid samples from noticeably-rancid ones. The contribution degree of amygdalin content as one of the input attributes of discriminative model was higher than 1. Rancidness affected the quality of Armeniacae Semen Amarum, resulting in appearance changes, decrease in content of active components, and increase in acid value and peroxide value. Obviously, noticeably-rancid samples were non-conforming to Chinese Pharmacopoeia and no longer suitable for medicinal use. Rancidness can significantly reduce the quality of Armeniacae Semen Amarum, and even could possibly produce toxicity, which should attach more attention.
Assuntos
Amigdalina , Cromatografia Líquida de Alta Pressão , Medicamentos de Ervas Chinesas , SêmenRESUMO
Abstract We report an unexpected difficult airway in a patient with unrecognized lingual tonsillar hypertrophy. A 54-year-old hypertensive woman presented for resection of a mediastinal mass under general anesthesia (GA). After induction, mask ventilation was impossible. Laryngeal mask airway (LMA) was used, achieving suboptimal ventilation. Fiberoptic intubation through LMA was attempted but tube advancement was hindered by a protrudingmass. Finally, intubation was achieved using the Frova introducer. After completion of the surgery, the patient was transferred, intubated, to the postanesthesia care unit. Ear, nose, and throat assessment concluded that the mass was a hyper-trophied lingual tonsil. Unexpected lingual tonsillar hypertrophy can complicate GA, making mask ventilation, and even intubation impossible. It is considered a frequent cause of unexpected difficult airway. Diagnosis cannot be made by standard airway physical examination. Once recognized, fiberoptic intubation is mandatory in subsequent surgeries.
Resumen Presentamos el caso de una vía aérea difícil imprevista debido a hipertrofia de la amígdala lingual no conocida. Mujer de 54 años, hipertensa, que ingresa para resección de masa mediastínica bajo anestesia general. Tras la inducción, la ventilación mediante mascarilla facial resultó imposible. Se coloca mascarilla laríngea (ML) y se consigue ventilación de forma subóptima. Se intenta intubación guiada por fibroscopia a su través, pero se objetiva masa protruyente que impide la progresión del tubo. Finalmente se intuba mediante introductor Frova. Tras finalizar la cirugía, la paciente se traslada intubada a la Unidad de Reanimación Postanestésica (URPA). Se realiza evaluación por otorrinolaringología (ORL), que concluye que la masa corresponde a una amígdala lingual hipertrófica. La hipertrofia de la amígdala lingual puede complicar la anestesia, dificultando la ventilación e intubación. Se considera una causa frecuente de vía aérea difícil imprevista. El diagnóstico no puede realizarse mediante exploración anestésica estándar. Una vez conocida, las intubaciones siguientes deben ser guiadas por fibroscopia.
Assuntos
Humanos , Feminino , Pessoa de Meia-Idade , Faringe , Amigdalina , Hipertrofia , Otolaringologia , Língua , Tonsila Palatina , Ventilação , Máscaras LaríngeasRESUMO
This study aimed to establish characteristic chromatogram and content determination method for Chan Taoren formula granules,evaluate the production processes of Chan Taoren formula granules based on the correlation of characteristic chromatogram and the transfer rate of D-amygdalin,and clarify the key control points. The optimized analytical method was carried out on a Waters CORTECS C18 column(4. 6 mm×150 mm,2. 7 μm) with acetonitrile-0. 1% phosphoric acid aqueous solution as the mobile phase at a flow rate of 0. 6 m L·min-1. The detection wavelength was 207 nm,and the column temperature was 20 ℃ . As compared with the standard decoction of Chan Taoren,there were five characteristic peaks in the decoction pieces,extracts,concentrates,spray-dried powders and formula granules,basically consistent in relative retention time and peak pattern; in addition,the transfer rate of D-amygdalin from Chan Taoren pieces to the formula granules was within the transfer rate range of standard decoction. The average transfer rate of D-amygdalin was 56.65%,72.85%,94.58% and 99.29% respectively in the extraction,concentration,spray drying and granulation processes. Therefore,the factors affecting D-amygdalin in the extraction process were further studied. The results showed that D-amygdalin was easily converted to L-amygdalin in the water extraction process,leading to a low transfer rate of D-amygdalin in this process.D-amygdalin was unstable under alkaline conditions and prone to isomerization. Both liquid to solid ratio and extraction time had significant effects on the extraction rate of D-amygdalin. In this study,the key links in the production process of Chan Taoren formula granules was clarified based on the characteristic chromatogram and the quantity transmission of D-amygdalin,which provided a theoretical basis for production and quality control.
Assuntos
Amigdalina , Cromatografia Líquida de Alta Pressão , Medicamentos de Ervas Chinesas , Controle de Qualidade , ÁguaRESUMO
Amarogentin is an efficacious Chinese herbal medicine and a component of the bitter apricot kernel. It is commonly used as an expectorant and supplementary anti-cancer drug. β-Glucosidase is an enzyme that hydrolyzes the glycosidic bond between aryl and saccharide groups to release glucose. Upon their interaction, β-glucosidase catalyzes amarogentin to produce considerable amounts of hydrocyanic acid, which inhibits cytochrome C oxidase, the terminal enzyme in the mitochondrial respiration chain, and suspends adenosine triphosphate synthesis, resulting in cell death. Hydrocyanic acid is a cell-cycle-stage-nonspecific agent that kills cancer cells. Thus, β-glucosidase can be coupled with a tumor-specific monoclonal antibody. β-Glucosidase can combine with cancer-cell-surface antigens and specifically convert amarogentin to an active drug that acts on cancer cells and the surrounding antibodies to achieve a killing effect. β-Glucosidase is injected intravenously and recognizes cancer-cell-surface antigens with the help of an antibody. The prodrug amarogentin is infused after β-glucosidase has reached the target position. Coupling of cell membrane peptides with β-glucosidase allows the enzyme to penetrate capillary endothelial cells and clear extracellular deep solid tumors to kill the cells therein. The Chinese medicine amarogentin and β-glucosidase will become an important treatment for various tumors when an appropriate monoclonal antibody is developed.
Assuntos
Humanos , Amigdalina , Usos Terapêuticos , Anticorpos Monoclonais , Usos Terapêuticos , Antineoplásicos , Usos Terapêuticos , Peptídeos Penetradores de Células , Usos Terapêuticos , Iridoides , Usos Terapêuticos , Pró-Fármacos , Usos Terapêuticos , beta-Glucosidase , Usos TerapêuticosRESUMO
Amygdalin, D-mandelonitrile-beta-D-glucoside-6-beta-glucoside, belongs to aromatic cyanogenic glycoside group derived from rosaceous plant seed. Mounting evidence has supported the anti-cancer effects of amygdalin. However, whether amygdalin indeed acts as an anti-tumor agent against breast cancer cells is not clear. The present study aimed to investigate the effect of amygdalin on the proliferation of human breast cancer cells. Here, we show that amygdalin exerted cytotoxic activities on estrogen receptors (ER)-positive MCF7 cells, and MDA-MB-231 and Hs578T triple-negative breast cancer (TNBC) cells. Amygdalin induced apoptosis of Hs578T TNBC cells. Amygdalin downregulated B-cell lymphoma 2 (Bcl-2), upregulated Bcl-2-associated X protein (Bax), activated of caspase-3 and cleaved poly ADP-ribose polymerase (PARP). Amygdalin activated a pro-apoptotic signaling molecule p38 mitogen-activated protein kinases (p38 MAPK) in Hs578T cells. Treatment of amygdalin significantly inhibited the adhesion of Hs578T cells, in which integrin alpha5 may be involved. Taken together, this study demonstrates that amygdalin induces apoptosis and inhibits adhesion of breast cancer cells. The results suggest a potential application of amygdalin as a chemopreventive agent to prevent or alleviate progression of breast cancer, especially TNBC.
Assuntos
Humanos , Adenosina Difosfato Ribose , Amigdalina , Apoptose , Proteína X Associada a bcl-2 , Neoplasias da Mama , Caspase 3 , Integrina alfa5 , Linfoma de Células B , Células MCF-7 , Proteínas Quinases p38 Ativadas por Mitógeno , Plantas , Receptores de Estrogênio , Neoplasias de Mama Triplo NegativasRESUMO
The study aims to develop an LC-MS/MS method for the simultaneous determination of amygdalin and paeoniflorin in urine samples, and to investigate their urinary excretion characteristics in healthy volunteers after intravenous infusion administration of Huoxue-Tongluo lyophilized powder for injection (HTLPI). The urine samples were extracted by methanol, and then separated on a Hedera ODS-2 column with a mobile phase of acetonitrile and 5 mmol · L(-1) ammonium acetate buffer solution containing 0.05% formic acid (20:80). Electrospray ionization source was applied and operated in the positive ion mode using MRM. The method exhibited good linearity over the concentration range of 0.03 -40 µg · mL(-1). The values on both the occasions (intra- and inter-day) were all within 15% at three concentration levels. No matrix effect and carry-over effect were observed. Amygdalin and paeoniflorin were stable in human urine under different storage conditions. Approximately 79.6% of the administered amount of amygdalin was excreted unchanged in urine within 24 h and which was 48.4% for paeoniflorin. The developed LC-MS/MS method can be applied to evaluate the urinary excretion of amygdalin and paeoniflorin.
Assuntos
Humanos , Amigdalina , Urina , Cromatografia Líquida , Medicamentos de Ervas Chinesas , Glucosídeos , Urina , Monoterpenos , Urina , Espectrometria de Massas em TandemRESUMO
The effect of amygdalin joint hydroxysafflor yellow A (HSYA) on the endplate chondrocytes derived from intervertebral discs of rats induced by IL-1beta and the possible mechanism were studied and explored. Chondrocytes were obtained from endplate of one-month SD rat intervertebral discs and cultured primary endplate chondrocytes. After identification, they were divided into normal group, induced group, amygdalin group, HSYA group and combined group. CCK-8 kit was adopted to detect the proliferation of the endplate chondrocytes. FCM was measured to detect the apoptosis. Real-time PCR method was adopted to observe the mRNA expression of Aggrecan, Col 2 alpha1, Col 10 alpha1, MMP-13 and the inflammatory cytokines IL-1beta. The protein expression of Col II, Col X was tested through immunofluorescence. Compared with the normal group, the proliferation of the endplate chondrocytes decreased while the apoptosis increased (P < 0.05). With down regulation of the mRNA expressions of Aggrecan, Col 2 alpha1 and up regulation of the mRNA expressions of Col 10 alpha1, MMP-13, IL-1beta (P < 0.05), the protein expression of Col II decreased while the protein expression of Col X increased. Compared with the induced group, amygdalin group, HSYA group, the combined group could inhibit the apoptosis and promote the proliferation (P < 0.05). They could increase the mRNA expressions of Aggrecan and Col 2 alpha1 while decrease the mRNA expressions of Col 10 alpha1, MMP-13 and IL-1beta (P < 0.05). They could also enhance the protein expression of Col II while reduce the protein expression of Col X. The effect of the combined group was significantly better than that of amygdalin and HSYA. Amygdalin joint HSYA could inhibit the degeneration of the endplate chondrocytes derived from intervertebral discs of rats induced by IL-1beta and better than the single use of amygdalin or HSYA.
Assuntos
Animais , Ratos , Amigdalina , Farmacologia , Apoptose , Células Cultivadas , Chalcona , Farmacologia , Condrócitos , Colágeno , Metabolismo , Sinergismo Farmacológico , Interleucina-1beta , Disco Intervertebral , Biologia Celular , Quinonas , FarmacologiaRESUMO
Ten compounds were isolated from the 70% ethanol extract of linseed meal (Linum usitatissimum L) through a combination of various chromatographic techniques, including silica gel, macroporous adsorbent resin, Sephadex LH-20, and preparative HPLC. On the basis of spectroscopic data analysis, they were elucidated as 1-methylethyl-2-O-beta-D-glucopyranosyl-(1" --> 6')-beta-D-glucopyanoside (1), linustatin (2), neolinustatin (3), lotaustralin (4), linamarin (5), deoxyguanosine (6), deoxyadenosine (7), (+)-pinoresinol-4'-O-beta-D-glucopyranoside (8), 4-O-beta-D-glucopyranosylvanillyl alcohol (9) and tachioside (10), separately. Among them, compound 1 is a new compound, and compounds 6, 8 and 10 were isolated from the linseed meal for the first time.
Assuntos
Amigdalina , Química , Desoxiadenosinas , Química , Desoxiguanosina , Química , Linho , Química , Glucosídeos , Química , Glicosídeos , Química , Lignanas , Química , Estrutura Molecular , Nitrilas , Química , Plantas Medicinais , Química , Sementes , QuímicaRESUMO
<p><b>OBJECTIVE</b>To establish an HPLC method for the determination of ephedrine hydrochloride, D-pseudo-ephedrine and amygdalin in Xiao'er Pingchuan Qutan granule.</p><p><b>METHOD</b>Pheny ether chromatographic column (4.6 mm x 250 mm, 5 microm) was adopted, with acetonitrile-0.1% phosphoric acid (containing 0.1% three ethylamine) (3:97) as the mobile phase. The UV detection wavelength was at 210 nm, with the flow rate of 1 mL x min(-1), and column temperature was at 35 degrees C.</p><p><b>RESULT</b>The linearity of ephedrine hydrochloride, D-pseudo-ephedrine and amygdalin ranged between 0.078 60-3.144 microg (r = 1.000 0), 0.103 4-2.068 microg (r = 0.999 7) and 0.430 5-3.157 microg (r = 0.999 8), respectively. Their average recoveries were 98.46% (RSD 1.1%), 103.0% (RSD 1.5%) and 97.15% (RSD 2.1%), respectively.</p><p><b>CONCLUSION</b>The method is simple, stable and reliable that it can be used to determine the content of ephedrine hydrochloride, D-pseudo-ephedrine and amygdalin in Xiao'er Pingchuan Qutan granule.</p>
Assuntos
Amigdalina , Química , Cromatografia Líquida de Alta Pressão , Medicamentos de Ervas Chinesas , Química , Efedrina , Química , Modelos Lineares , Pseudoefedrina , Química , Reprodutibilidade dos Testes , Fatores de TempoRESUMO
Armeniacae semen (AS) has been considered a toxic herb in the Korean medicine as it contains hydrogen cyanide and amygdalin, especially in its endocarp. Therefore, prebrewed AS that is devoid of endocarp has been traditionally used. In the present study, amygdalin content of the prebrewed AS was significantly lower (2.73 +/- 0.32 microg/ml; p < 0.01) than the content in the extract that contained the endocarps (28.50 +/- 6.71 microg/ml); amygdalin content corresponded to 10% of the extract in the present study. Because of single oral dose toxicity of prebrewed AS according to the recommendation of Korea Food and Drug Administration Guidelines (2009-116, 2009), which was based on single oral dose toxicity study of prebrewed AS, mortality due to toxic principles was significantly reduced. In this study, 2,000 mg/kg of prebrewed AS led to death of 1 female rat and 1 male rat at the end of 2 hr of administration. Based on these results, the 50% lethal dose in both male and female rats was determined to be 9279.5 mg/kg. Seizure, loss of locomotion, and increases in respiration and heart rate were observed as prebrewed AS treatment-related toxicological signs; these signs were restrictedly manifested in the prebrewed AS (2,000 mg/kg)-treated rats. In addition, no changes were observed in body weight, organ weight, gross features, and histopathological parameters with 2,000 mg/kg of AS in both male and female rats. These findings serve as direct evidence that amygdalin in AS is the toxic principle, which can be reduced by the traditional prebrewing method involving the exclusion of endocarp.
Assuntos
Animais , Feminino , Humanos , Masculino , Ratos , Amigdalina , Peso Corporal , Frequência Cardíaca , Cianeto de Hidrogênio , Coreia (Geográfico) , Locomoção , Tamanho do Órgão , Respiração , Convulsões , Sêmen , United States Food and Drug AdministrationRESUMO
Background: Angiogenesis contributes to different physiological and pathological conditions. The aim of this study was to investigate for the first time the antiangiogenic effects of amygdalin on the cultured endothelial cells of diabetic rats. Materials and Methods: A total of 20 streptozotocin-induced diabetic rats were divided into two equal groups of control and amygdalin-treated animals. Eight weeks after the induction of diabetes, amygdalin was injected intraperitoneally (3 mg/kg) to the rats of the treatment group. One day later, rats were sacrificed; the aortic arteries were excised and cut as 2 mm rings. Each aortic ring was incubated in a cell-culture well for 7 days. The process of angiogenesis was monitored by counting the number of microvessels and primary microtubules in each well. Results: Optic microscopy showed proliferation and migration of new endothelial cells to the fibrin gels. The endothelial cells produced primary microtubules which gradually made several branches and finally made a vascular matrix. The number of the primary microtubules and microvessels were significantly lower in the amygdalin-treated vs. control group (P < 0.01). Conclusion: Therefore, amygdalin exerts inhibitory effects on angiogenesis in aortic rings of diabetic rats and may pave a new way for treatment of unfavorable angiogenic conditions.
Assuntos
Amigdalina/administração & dosagem , Animais , Proliferação de Células/efeitos dos fármacos , Células Cultivadas , Cianetos/administração & dosagem , Diabetes Mellitus Experimental , Células Endoteliais/efeitos dos fármacos , Masculino , Neovascularização Fisiológica/efeitos dos fármacos , Ratos , Ratos Sprague-DawleyRESUMO
<p><b>OBJECTIVE</b>To investigate pharmacokinetic parameters of peoniflorin, albiflorin and amygdaloside after administration of Guizhi Fuling capsule in beagle dogs.</p><p><b>METHOD</b>Plasma was collected from forelimb vein of Beagle dogs after oral administration of Guizhi Fuling capsule. HPLC-MS/MS method was used to determine the concentrations of constituents in plasma. The pharmacokinetic parameters were analyzed by program DAS 2.0.</p><p><b>RESULT</b>The limit of quantitation of peoniflorin, albiflorin and amygdaloside were 0.25, 2.64, 0.04 microg x L(-1), respectively. After administrated with different doses, half-life of peoniflorin in dogs were 4.33, 3.62 h, albiflorin were 6.16, 5.91 h, amygdaloside were 2.43, 1.32 h. The AUC(0-t) of all components were related to dose.</p><p><b>CONCLUSION</b>The pharmacokinetic course of peoniflorin, albiflorin and amygdaloside can be described by two-compartment model, and these components have high expose.</p>
Assuntos
Animais , Cães , Masculino , Administração Oral , Amigdalina , Sangue , Área Sob a Curva , Benzoatos , Sangue , Hidrocarbonetos Aromáticos com Pontes , Sangue , Cápsulas , Farmacocinética , Cromatografia Líquida de Alta Pressão , Métodos , Medicamentos de Ervas Chinesas , Farmacocinética , Glucosídeos , Sangue , Meia-Vida , Monoterpenos , Espectrometria de Massas em Tandem , MétodosRESUMO
<p><b>OBJECTIVE</b>To evaluate effect of amygdalin on expression of four biomarkers in the animal model of pulmonary fibrosis induced by bleomycin.</p><p><b>METHODS</b>Rats were given one dose (5 mg/kg) of bleomycin in bleomycin-treated groups, amygdalin-treated groups and saline in controls by intratracheal instillation exposed surgically. The amygdalin-treated groups rats were treated with intraperitoneal injection of amygdalin (15 mg x kg(-1) x day(-1)). The rats were sacrificed 7, 14 and 28 days after bleomycin administration. Polarized light microscopy and Image-Pro Plus detected I and III collagen expressed in Paraffin-embedded lung sections stained with Sirius red. Surface-enhanced laser desorption-ionization time-of-flight mass spectrometry (SELDI-TOF MS) with weak cationic proteinchip (CM10) detected differentially expressed proteins in the pooled serum samples of all groups.</p><p><b>RESULTS</b>Consistent fibrotic responses were found in all bleomycin and amygdalin-tread groups. On the 7th, 14th and 28th day after bleomycin or saline instillation, four differentially expressed proteins were detected in the pooled serum of all groups rats, consisting of 4 proteins with mass/charge ratio of 3530.7, 7043.5, 8332.6 and 9068.0, respectively. Compared with control groups, protein peaks intensity ratio with mass/charge ratio of 3530.7 on 7, 28 d and 7043.5, 8332.6 and 9068.0 on 7, 14 and 28 d was > 2 in bleomycin-treated groups. Compared with amygdalin-treated groups, protein peaks intensity with mass/charge ratio of 3530.7 at 7, 14, 28 d had no change almost, but protein peaks intensity ratio with mass/charge ratio of 7043.5 at 7 d, 8332.6 on 28 d and 9068.0 on 14 d was > 2 in bleomycin-tread groups. All the four protein peaks intensity had no change almost at other point.</p><p><b>CONCLUSION</b>Amygdalin may reduce the bleomycin-induced increase of differentially expressed protein peak intensities in rat serum.</p>
Assuntos
Animais , Masculino , Ratos , Amigdalina , Farmacologia , Biomarcadores , Sangue , Bleomicina , Proteínas Sanguíneas , Metabolismo , Fibrose Pulmonar , Sangue , Ratos WistarRESUMO
<p><b>OBJECTIVE</b>To study the influence of processing on metabolism of the main component of bitter almond-amygdalin in rat.</p><p><b>METHOD</b>The blood was collected at different times after amygdalin given by injection and oral, bitter almond and its processed production given by oral respectively, and then detected by both HPLC and HPLC-MS(n) methods after extraction pretreatment.</p><p><b>RESULT</b>After injection, amygdalin was absorbed in prototype to blood rapidly, while the other three kinds of medicine given by oral were all not detected the prototype of amygdalin, but two metabolites were detected which were isomers of prunasin confirmed by mass spectrometry. The metabolic pathway of prunasin in processed bitter almond group was markedly different from the bitter almond group.</p><p><b>CONCLUSION</b>Processing has a significant effect on bitter almond metabolic processes in rats.</p>
Assuntos
Animais , Feminino , Masculino , Ratos , Amigdalina , Metabolismo , Prunus , Química , Ratos Sprague-DawleyRESUMO
<p><b>OBJECTIVE</b>To explore the method and significance for studying active anti-liver fibrosis ingredients consisted Chinese medicine compound prescription based on Chinese medicine theory.</p><p><b>METHODS</b>Optimized prescription was screened out, adopting uniform block design with 4-factor 8-level table and regression analysis, through applying the four known effective ingredients (cordyceps sinensis polysaccharide, salvianolic acid B, amygdaloside and gypenosides) of Fuzheng Huayu Capsule (FZHYC, a new Chinese medine anti-liver fibrosis drug) to two rat liver fibrosis models established separately by dimethylnitrosamine (DMN) and CCl4, and taking the liver content of hydroxyproline (Hyp) as the screen index. Then a further study for comparing and verifying the efficacy of the obtained optimized prescription was conducted on the two former models respectively by observing the changes of Hyp content in liver, serum ALT activity and fibrosis pathology after medication, controlled by the original FZHYC and the recipe assembled by all the four ingredients.</p><p><b>RESULTS</b>Two optimized prescriptions (OPA and OPB) were screened out separately in the studies conducted on the two models. Both of them were consisted of cordyceps sinensis polysaccharide, Amygdaloside and Gypenosides, but different in constituent ratio, i.e., the ratio in OPA was 60 : 80: 50, and that in OPB, 20: 160: 50. Verifying study showed both OPA and OPA were significantly effective, with the efficacy equivalent to that of FZHYC (P>0.05). However, when they were used in combining with salvianolic acid B (the cutout ingredient in the screening), the efficacy lowered surely.</p><p><b>CONCLUSIONS</b>Uniform design is a valuable method in the compatibility research of Chinese Medicine drugs' composition. To assemble a new compound recipe reasonably based on the prescription of traditional compound recipe could make its effect equivalent to that of the original prescription. Ingredients or constituents in a prescription, either presented synergistic or antagonistic effects, are not randomly stacked together, and they should be orderly assembled in intrinsic rules of qualitative and quantitative changing.</p>
Assuntos
Animais , Masculino , Ratos , Amigdalina , Combinação de Medicamentos , Desenho de Fármacos , Medicamentos de Ervas Chinesas , Usos Terapêuticos , Gynostemma , Cirrose Hepática , Tratamento Farmacológico , Extratos Vegetais , Ratos Wistar , Análise de RegressãoRESUMO
Resistance to antibacterial agents and sensivity reaction to such chemical compounds are the main reasons for investigators to develop new antibiotics from herbal sources. Antimicrobial effects of Metanolic extract of 12 herbal species Pistacia atlantica, Amygdalus scoparia, Cuscuta epthymum, Ephedra procera, Salsola boryosm, Sameraria armena, Scabiosa olivier, Scorzonera tortuosissima, Lepyrodielis holosteoidea, Vaccaria pyramidata, Sonchus oleraceam and Silene conoidema on 6 bacterial strains Staphylococcus aureas, Staphylococcus epidermidis, Echerichia colt, Kelebsiella pneumonia, Pseudomonas aeroginos and Bacillus subtilis were, separately, studied using Cylinder-plate method. In this laboratory study, methanolic extracts of herbal strains were prepared by maceration and after concentrating the extracts were dried. Then the concentrations of 50, 25, 12.5, 6.25 and 3.125 mg/ml of the extracts were prepared using 1:1 solution of DMSO/methanol. The standard bacteria with certain concentration [0.5 MacFarland] were inoculated on to the Muller-Hinton agar medium. Prepared extracts were dropped into cylinders and 18-24 hours after incubation and penetration of extract into the culture medium, the antibacterial effects and growth inhibitory zone [mm] were measure and values were expressed as [Mean +/- SEM]. The least and the most amount of effective concentration were 3.125 mg/ml and 50 mg/ml, respectively. The most inhibitory diameter belonged to methanolic extract of Amygdalus scoparia on Staphylococcus epidermidis which was equal to 19 +/- 0.3mm. Metanolic extracts of herbal species of Pistacia atlantica, Amygdalus scoparia and Ephedra procera had the most antibacterial effects compared to gentamicin as positive control. Regarding the side effects of the synthetic drugs and also benefits of such herbal extracts, extracts of these herbs as antibacterial agents after further investigations seems to be useful
Assuntos
Plantas Medicinais , Resistência Microbiana a Medicamentos , Extratos Vegetais , Salsola , Pistacia , Amigdalina , Cuscuta , Ephedra , Sonchus , Vaccaria , SileneRESUMO
Amygdalin is known as vitamain B17, and it was called laetrile. Amygdalin is composed of two molecules of glucose, one molecule of benzaldehyde which induces an analgesic action, and one molecule of hydrocyanic acid which is an anti-neoplastic compound. Amygdalin had been used to treat cancers and relieve pain. In order to evaluate whether the analgesic action of amygdalin is related with descending pain control system, we performed patch clamp study. In the present study, the modulatory effects of amygdalin on glycine- and glutamate-induced ion currents in periaqueductal gray (PAG) neurons were investigated using the nystatin-perforated patch clamp method. Continuous application of lipopolysaccharides (LPS) on PAG neurons resulted in increased glycine-induced ion current, and in decreased glutamate-induced ion current. In contrast, continuous application of amygdalin with LPS resulted in decreased glycine-induced ion current increased by LPS, and increased glutamate- induced ion current decreased by LPS in concentration- and time-dependent fashion. These results demonstrate that amygdalin modulates neuronal activity of PAG by modulation of glycine and glutamate. Based on the present results, it can be suggested that amygdalin participates in the regulation of the descending pain control system in the level of PAG neurons. The present study demonstrated that activation of the descending pain control system is one of the possible analgesic mechanisms of amygdalin.