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ObjectiveTo establish a rat model of diabetic wound by feeding on a high-fat and high-sugar diet combined with intraperitoneal injection of streptozotocin （STZ） and surgical preparation of full-thickness skin defects， observe the effect of cinnamaldehyde on the wound healing of diabetes rats， and explore the therapeutic mechanism of cinnamaldehyde in improving wound healing of diabetes rats based on the PTEN-induced putative kinase （PINK1）/Parkin pathway-mediated mitochondrial autophagy. MethodForty-eight male SD rats were randomly divided into blank group （n=12） and diabetes group （n=36）. The diabetes group was further randomly divided into model group， cinnamaldehyde group， and Beifuxin group， with 12 rats in each group. The blank group and the model group received routine disinfection with physiological saline after creating the wounds， while the cinnamaldehyde group received topical application of polyethylene glycol 400 （PEG 400） gel containing 4 μmol·L-1 cinnamaldehyde， and the Beifuxin group received topical application of Beifuxin gel. Dressings were changed once daily. The wound healing rate of each group was observed. On the 7th and 14th days after intervention， the wound tissues of the rats were collected. Hematoxylin and eosin （HE） staining was performed to observe the pathological changes in the local tissues. Immunohistochemistry （IHC） was used to detect the expression of interleukin-6 （IL-6）， tumor necrosis factor-α （TNF-α）， vascular endothelial growth factor （VEGF）， and collagen fibers. Immunofluorescence （IF） and Real-time polymerase chain reaction （Real-time PCR） were used to detect the protein， and mRNA expression of PINK1， Parkin， microtubule-associated protein 1 light chain 3 Ⅱ （LC3 Ⅱ）. ResultAfter intraperitoneal injection of STZ， compared with the blank group， the random blood glucose values of rats in the diabetic group increased significantly （P<0.01）， all higher than 16.7 mmol·L-1， and persistently hyperglycemic for some time after modeling. Compared with the blank group， the model group showed poor growth and healing of granulation tissue in the wounds， and the wound healing rate decreased （P<0.01）. On the 7th day after intervention， the blank group had squamous epithelial coverage on the wounds. Compared with the blank group， the model group only had a small amount of scab at the wound edges， with a large number of infiltrating inflammatory cells in the wounds. The protein expression levels of IL-6 and TNF-α in the tissues increased （P<0.01）， and the protein and mRNA levels of PINK1， Parkin， and LC3Ⅱ decreased （P<0.01）. On the 14th day after the intervention， the granulation tissue in the wounds of the blank group was mature and well-healed. Compared with the blank group， the model group still had infiltrating inflammatory cells and red blood cell exudation. The protein expression levels of VEGF and collagen fibers in the tissues decreased （P<0.01）， and the protein and mRNA expression levels of PINK1， Parkin， and LC3Ⅱ increased （P<0.01）. Compared with the model group， the cinnamaldehyde group and the Beifuxin group showed better wound healing， with increased wound healing rates （P<0.01）. On the 7th day after intervention， the protein expression levels of IL-6 and TNF-α in the tissues decreased （P<0.01）， and the protein and mRNA expression levels of PINK1， Parkin， and LC3Ⅱ increased （P<0.01）. On the 14th day after intervention， the protein expression levels of VEGF and collagen fibers in the tissues increased （P<0.01）， and the protein and mRNA expression levels of PINK1， Parkin， and LC3Ⅱ decreased （P<0.01）. ConclusionCinnamaldehyde can promote the wound healing of diabetes rats by increasing the wound healing rate， reducing the levels of inflammatory factors IL-6 and TNF-α， and increasing the levels of VEGF and collagen fibers. Its mechanism may be related to the regulation of the PINK1/Parkin signaling pathway， activation of mitochondrial autophagy， inhibition of inflammatory responses， and promotion of angiogenesis and collagen synthesis， thereby promoting the wound healing of diabetes rats.
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The present study aims to evaluate the effectiveness of Cinnamon (Cinnamomum verum) derive bioactive compound viz.trans-cinnamaldehyde, cinnamyl alcohol, and cinnamic acid on inhibition of Bacillus licheniformis ?-amylase (BLA) and pancreatic porcine ?-amylase (PPA) activity. The inhibition extent of each of the compounds was determined along with their inhibition kinetics and compared with standard inhibitor-acarbose (Synthetic anti-diabetic agent). The IC50 values for trans-cinnamaldehyde with respect to BLA and PPAwere observed to 5.38 ?g mL?1 and 3.76 ?g mL?1, respectively. The IC50 value of acarbose was estimated to be 6.2 ?g mL?1 for both the amylases. The maximum percent enzyme inhibition of 75.8 (at 10.75 µg mL?1) and 71.6 (5.38 µg mL?1) were observed in case of BLA and PPA, respectively, using trans-cinnamaldehyde. Cinnamyl alcohol and cinnamic acid on the other hand were observed to show no specific inhibitory effect on the both the ?-amylases even at high concentrations. Catalytic efficiency (Vmax/Km) of both the amylases was observed to decrease significantly in presence of trans-cinnamaldehyde compared to acarbose. Overall, trans-cinnamaldehyde was observed as a better inhibitor of ?-amylase compared to known synthetic inhibitor-acarbose. Thus, trans-cinnamaldehyde could effectively be used for controlling hyperglycemia and diabetes mellitus.
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OBJECTIVE To prepare cinnamaldehyde （CA） loaded liposomes bilayer-modified by bovine serum albumin （BSA）/chitosan （CTS）（BSA/CTS-Lip-CA） in order to improve the sustained-release effect and storage stability of the nanoparticles. METHODS Firstly，cinnamaldehyde loaded liposomes （Lip-CA）and blank liposomes （Lip-Blank）were prepared by thin film dispersion method. Then chitosan modified cinnamaldehyde loaded liposome （CTS-Lip-CA）and BSA/CTS-Lip-CA were obtained by electrostatic adsorption. Finally ， the prepared liposomes were characterized ， and their in vitro release characteristics and storage stability were investigated. RESULTS The particle size of BSA/CTS-Lip-CA was （177.8±4.0）nm and the Zeta potential was （－15.6±1.5）mV；they were in spherical shape ；FTIR analysis showed that the modification of BSA and CTS had no effect on the internal structure of liposomes. The results of in vitro drug release characteristics showed that the cumulative release of Lip-CA ，CTS-Lip-CA and BSA/CTS-Lip-CA within 10 hours were 82.9％，74.1％ and 72.9％ respectively. The results of storage stability showed that after 30 days of storage ，the particle sizes of Lip-CA ，CTS-Lip-CA and BSA/ CTS-Lip-CA were （134.2±2.1），（151.7±0.4），（164.8±1.5）nm；the retention rates of model drug CA were 65.4％，82.5％ and 90.2％ respectively. CONCLUSIONS BSA/CTS-Lip-CA is successfully prepared. It has a certain sustained-release effect and can improve the storage stability of the drug to a certain extent.
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Objective To revise the qualitative and quantitative determination methods of Xuanxi Rongjin powder. Methods TLC was used to qualitatively identify Chuanxiong and Chuanshanlong. The content of cinnamaldehyde in the preparation was determined by HPLC with KR100-5C18 column (250 mm×4.6 mm, 5μm). The mobile phase was acetonitrile-water (35:65) and the detection wavelength was 290 nm. Results TLC can qualitatively identify Chuanxiong and Chuanshanlong. Cinnamaldehyde has a good linear relationship in the range of 0.0489~0.3260 µg/ml (r=1.00), The average recovery was 95.71% (RSD=1.78%). Conclusion The method has high sensitivity, good specificity, simple operation and good reproducibility.
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This study was aimed to explore the comparative efficacy of cinnamon bark extract, cinnamaldehyde and kaempferol against acetaminophen (APAP)-induced oxidative stress. Cinnamon bark extract, cinnamaldehyde and kaempferol were utilized or in-vivo analysis. From the results of in-vitro screening tests, cinnamon ethanolic extract was selected for in-vivo study in mouse model. For this, Balb/c albino mice were treated with cinnamon ethanolic extract (200 mg/kg), cinnamaldehyde (10 mg/kg) and kaempferol (10 mg/kg) orally for 14 days followed by single intraperitoneal administration of APAP during 8 hours. Blood and organ samples were collected for biochemical and histopathological analysis. The results showed that cinnamon bark ethanolic extract, cinnamaldehyde and kaempferol ameliorated APAP-induced oxidative stress and organ toxicity in mice. In conclusion, cinnamaldehyde and kaempferol possess comparable antioxidant potential even at 20-times less dose as compared to cinnamon bark ethanolic extract suggesting therapeutic potential in oxidative stress-related disorders.
Este estudio tuvo como objetivo explorar la eficacia comparativa del extracto de corteza de canela, cinamaldehído y kaempferol contra el estrés oxidativo inducido por acetaminofén (APAP). Se utilizaron extracto de corteza de canela, cinamaldehído y kaempferol para el análisis in vivo. De los resultados de las pruebas de detección in vitro, se seleccionó el extracto etanólico de canela para estudio in vivo en modelo de ratón. Para ello, los ratones albinos Balb/c fueron tratados con extracto etanólico de canela (200 mg/kg), cinamaldehído (10 mg/kg) y kaempferol (10 mg/kg) por vía oral durante 14 días, seguido de la administración intraperitoneal única de APAP durante 8 horas. Se recogieron muestras de sangre y órganos para análisis bioquímicos e histopatológicos. Los resultados mostraron que el extracto etanólico de la corteza de canela, el cinamaldehído y el kaempferol mejoraron el estrés oxidativo inducido por APAP y la toxicidad orgánica en ratones. En conclusión, el cinamaldehído y el kaempferol poseen un potencial antioxidante comparable, incluso a una dosis 20 veces menor en comparación con el extracto etanólico de la corteza de canela, lo que sugiere un potencial terapéutico en los trastornos relacionados con el estrés oxidativo.
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Animals , Mice , Acrolein/analogs & derivatives , Plant Extracts/administration & dosage , Cinnamomum zeylanicum/chemistry , Oxidative Stress/drug effects , Kaempferols/chemistry , Antioxidants/administration & dosage , Acrolein/chemistry , Chromatography, High Pressure Liquid , Disease Models, Animal , Phytochemicals , Kidney/drug effects , Kidney/pathology , Liver/drug effects , Liver/pathology , Acetaminophen/toxicity , Mice, Inbred BALB CABSTRACT
Abstract This study aimed to chemically characterize the essential oils (EOs) of Cinnamomum zeylanicum (cinnamon) and Eremanthus erythropappus (candeia) and evaluate their acaricidal activity, together with that of their major compounds and cinnamyl acetate derivative, against Rhipicephalus microplus. Essential oil compounds were identified through gas chromatography. The larval packet test (LPT) at concentrations ranging from 0.31 to 10.0 mg/mL and the adult immersion test (AIT) at concentrations between 2.5 and 60.0 mg/mL were performed. (E)-cinnamaldehyde and α-bisabolol were the major compounds in cinnamon (86.93%) and candeia (78.41%) EOs, respectively. In the LPT, the EOs of cinnamon and candeia and the compounds (E)-cinnamaldehyde, α-bisabolol and cinnamyl acetate resulted in 100% mortality at concentrations of 2.5, 2.5, 5.0, 10.0 and 10.0 mg/mL respectively. In the AIT, percentage control values > 95% were observed for cinnamon and candeia EOs, (E)-cinnamaldehyde and α-bisabolol at the concentrations of 5.0, 60.0, 20.0, and 20.0 mg/mL, respectively, whereas cinnamyl acetate showed low activity. We conclude that EOs and their compounds showed high acaricidal activity, whereas the acetylated derivative of (E)-cinnamaldehyde presented less acaricidal activity on R. microplus engorged females.
Resumo Este estudo teve como objetivo caracterizar quimicamente os óleos essenciais (OE) de Cinnamomum zeylanicum (canela) e Eremanthus erythropappus (candeia) e avaliar sua atividade acaricida, juntamente com a de seus principais compostos e do derivado de acetato de cinamila, sobre Rhipicephalus microplus. Os compostos do óleo essencial foram identificados por cromatografia gasosa. Foram realizados o Teste de Pacote de Larvas (TPL), em concentrações variando de 0,31 a 10,0 mg/mL, e o Teste de Imersão de Adultos (TIA), em concentrações entre 2,5 e 60,0 mg/mL. (E)-cinnamaldeído e α-bisabolol foram os principais compostos nos OE da canela (86,93%) e da candeia (78,41%), respectivamente. No TPL, os OEs de canela e candeia, e os compostos (E)-cinnamaldeído, α-bisabolol e acetato de cinamila resultaram em 100% de mortalidade nas concentrações de 2,5, 2,5, 5,0, 10,0 e 10,0 mg/mL, respectivamente. No TIA, valores percentuais de controle >95% foram observados para OE de canela e candeia, (E)-cinnamaldeído e α-bisabolol nas concentrações de 5,0, 60,0, 20,0 e 20,0 mg/mL, respectivamente, enquanto o acetato de cinamila apresentou baixa atividade. Conclui-se que os OEs e seus compostos apresentaram alta atividade acaricida, enquanto o derivado acetilado do (E)-cinnamaldeído apresentou menor atividade acaricida em fêmeas ingurgitadas de R. microplus.
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Animals , Oils, Volatile/pharmacology , Rhipicephalus , Acaricides/pharmacology , Cinnamates , Cinnamomum zeylanicum , LarvaABSTRACT
OBJECTIVE@#To evaluate the effect and safety of cinnamaldehyde on immunosuppressed mice with invasive pulmonary candidiasis.@*METHODS@#An immunosuppressed BALB/c mouse model was established by intraperitoneal administration of cyclophosphamide (200 mg/kg) once daily for 2 days. The immunosuppressed mouse with invasive pulmonary candidiasis model was further established by nasal perfusion of Candida albicans suspension. In the cinnamaldehyde treatment group, immunosuppressed mice with invasive pulmonary candidiasis were orally given cinnamaldehyde 240 mg/(kg·d) for 14 consecutive days. Fluconazole and 0.9% saline were used as the positive and negative controls, respectively. The mice in the cinnamaldehyde safety evaluation group were orally administered cinnamaldehyde 480 mg/(kg·d) for 42 days to observe the safety of the drug. Microscopic identification, fungal culture, histopathological examination, and (1,3)-beta-D-glucans detection were conducted to analyze the effect of cinnamaldehyde on C. albicans.@*RESULTS@#The fungal clearance rate in the cinnamaldehyde treatment group was higher than that in the fluconazole control group (80.00% vs. 56.67%, P<0.05). The level of (1,3)-β-D-glucan in the cinnamaldehyde treatment group was lower than that in the fluconazole positive control group (1160.62 ±89.65 pg/mL vs. 4285.87 ± 215.62 pg/mL, P<0.05). The survival rate of mice in the cinnamaldehyde safety evaluation group was 100%, and no significant pathological changes of kidney, lung and liver were observed.@*CONCLUSIONS@#Cinnamaldehyde was effective and safe in treating immunosuppressed BALB/c mice with invasive pulmonary candidiasis. It would be a potentially novel drug for anti-candidiasis infection.
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Objective:To explore the potential target and mechanism of Wumeiwan in the treatment of lung metastasis of breast cancer by network pharmacological analysis and experimental verification. Method:The databases of active ingredients and targets of Wumeiwan were established through Traditional Chinese Medicine Systems Pharmacology（TCMSP） Database and Analysis Platform，and the targets of lung metastasis of breast cancer were established through the GeneCards database and Online Mendelian Inheritance in Man（OMIM） database，and the data of Chinese medicine targets and disease targets were matched. Cytoscape 3.6.0 software was used to establish the network analysis of traditional Chinese medicine-active ingredients-therapeutic targets，and the interaction relationship between key target proteins was analyzed by STRING database. Target gene ontology（GO） analysis and Kyoto Encyclopedia of Genes and Genomes（KEGG） signal pathway enrichment analysis were performed by using the Biological Information Annotation Database. Result:A total of 108 possible important targets for Wumeiwan in the treatment of lung metastasis of breast cancer were found，including interleukin 6（IL6），cysteine aspartate-specific protease-3（CASP3），vascular endothelial growth factor A（VEGFA），epidermal growth factor receptor（EGFR），mitogen-activated protein kinase（MAPK8）， and others. GO enrichment analysis yielded 29 cell components（CC），1 218 biological processes（BP） and 125 molecular functions（MF） related to lung metastasis of breast cancer，and KEGG enrichment analysis yielded 118 pathways related to lung metastasis of breast cancer（<italic>P<</italic>0.05），including MAPK signaling pathway and apoptosis pathway. <italic>In vitro</italic> experiments showed that cinnamaldehyde， the active ingredient of Wumeiwan， could induce apoptosis，inhibit proliferation and migration of MCF7 cells，partially validating the predicted results of network pharmacology to a certain extent. Conclusion:The therapeutic effect of Wumeiwan on lung metastasis of breast cancer may be multi-target，multi-pathway and multi-mechanism. The results of this study provide more evidence for the clinical application of Wumeiwan.
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Evaluation of the drug ligand interactions between the C. cassia bio-compounds with the SAP-1 in C. albicans to explore the inhibitory medicinal potential of C. cassia bio-compounds by a computational approach is performed in the present investigation. Antimicrobial assay was done using agar well diffusion method with the crude aqueous and ethanolic extracts of the dried barks of C. cassia against C. albicans. 2D & 3D structures of the active bio-compounds of C. cassia were optimized and the 3D structure of SAP-1 was retrieved from the PDB data bank. In-silico inhibitory potential of the selected C. cassia biocompounds against SAP-1 was done by Auto Dock 2.0 and was visualized with Accelrys discovery studio visualizing tool with the assessment of the molecular properties of the ligands against SAP-1 by molinspiration calculations and further assessment for their drug likeliness. In-vitro analysis showed a promising anti-fungal activity of C. cassia extracts against C. albicans. Cinnamoyl E-acetate and Eugenyl acetate seem to possess promising inhibitory effect to target SAP-1 with a least binding energy of –5.33 and -5.21 Kcal/mol with four hydrogen bonds respectively. Molinspiration assessments showed zero violations for all the C. cassia compounds with the TPSA scores of <140 Å towards the best oral bioavailability. The findings of the study emphasize that cinnamaldehyde, cinnamoyal acetate and eugenol from C. cassia seem to possess a promising inhibitory effect against SAP-1 of C. albicans suggesting the medicinal value of the spice against SAP-1
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Background: Cinnamon is one of the best known spices used as an herbal medicine. Cinnamaldehyde (CNM) the volatile oil, which was present in the essential oil of the bark, is the important constituents of cinnamon. Cinnamon has been investigated for its various effects like peptic ulcer protection, antioxidant property, inhibition of tau aggregation, anti-inflammatory activity, effect on cardiovascular system, anti-nociceptive activity, hepato-protective effects, hypolipidemic and antidiabetic activites. The present study was aimed to evaluate the anxiolytic effect of CNM per se and its interaction with diazepam in swiss albino mice.Methods: Anxiolytic activity was evaluated by elevated plus maze method. A group of 36 healthy mice of either sex weighing 20-30 grams were divided at random into six groups (n=6). CNM and diazepam were dissolved in tween twenty 20% to maintain uniformity of the solvent and given orally. Group I was given twenty 20% (10 ml/kg, p.o.), group II diazepam (0.5 mg/kg, p.o.), group III diazepam (1 mg/kg, p.o.), group IV cinnamaldehyde (100 mg/kg, p.o.), group V cinnamaldehyde (200 mg/kg, p.o.), group VI cinnamaldehyde and diazepam (100 mg/kg and 0.5 mg/kg, p.o.).Results: Cinnamaldehyde per se showed no anxiolytic effect at any dose (p<0.05). The standard drug diazepam has shown significant anxiolytic activity on elevated plus maze. Whereas combination of diazepam 0.5 mg/kg and cinnamaldehyde 100 mg/kg showed significant increase in the time spent in open arms as compared to all groups (p<0.05).Conclusions: CNM per se did not show any effect on anxiety but enhanced the action of diazepam when co-administered.
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To observe the efficacy of cinnamaldehyde on dextran sulfate sodium(DSS)-induced ulcerative colitis(UC) with Can-dida albicans(Ca) colonization and its effect on dectin-1/TLRs/NF-κB signaling pathway in mice. C57 BL/6 mice were randomly divided into normal group, DSS group, DSS+Ca group, cinnamaldehyde group and mesalazine group. Mice in DSS+Ca group were given Ca(1×10~8 CFU per mouse) through intragastrical administration for 4 consecutive days and then distilled water with 3.0% DSS for 7 consecutive days. In cinnamaldehyde group and mesalazine group, in addition to the induction method of the DSS+Ca group, mice were given 75 mg·kg~(-1) cinnamaldehyde and 200 mg·kg~(-1) mesalazine accompanied with 3.0% DSS for 7 consecutive days, respectively. Mice in normal group and DSS group were correspondingly administered with distilled water. The general conditions of the mice were observed daily, the diseased activity index(DAI) score was calculated, and fungal loads of feces were detected by plate method. The mice were sacrificed on day 12, colon length was measured, colon mucosa damage index(CMDI) score was calculated, and histopathological analysis was carried out by HE staining. Anti-saccharomces cerevisiae antibody(ASCA) and β-1,3-glucan in serum, and TNF-α, IL-1β, IL-6, IL-8, IL-10 in serum and colon tissue were detected by ELISA. The contents of β-1,3-glucan and macrophage infiltration in colon tissues were examined by immunofluorescence staining. The protein expressions of dectin-1, TLR2, TLR4 and NF-κB were detected by Western blot and immunohistochemistry staining. The results showed that cinnamaldehyde could significantly improve the general conditions of UC mice with Ca colonization, decrease DAI and histopathological scores, reduce intestinal mucosal congestion, erosion and colon shortening, decrease Ca load in mouse feces and tissues, down-regulate the contents of ASCA and β-1,3-glucan in serum, reduce the contents of TNF-α, IL-1β, IL-6, IL-8 and increase IL-10 in serum and colon tissues, inhibit macrophages infiltration and down-regulate the protein expression of dectin-1, TLR2, TLR4 and NF-κB in colon tissue. These results suggested that cinnamaldehyde had a therapeutic effect on UC mice with Ca colonization, which might be related to the inhibition of Ca proliferation, the regulation of dectin-1/TLRs/NF-κB signaling pathways and the coordination of the balance between pro-inflammatory and anti-inflammatory factors.
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Animals , Mice , Acrolein , Candida albicans , Colitis, Ulcerative , Colon , Dextran Sulfate , Disease Models, Animal , Lectins, C-Type , NF-kappa B , Signal TransductionABSTRACT
Objective To study the chemical constituents and cytotoxic activity of Dendrobium wardianum. Methods The compounds were separated and purified by various column chromatography techniques and semi-preparative liquid chromatography, and the structures were then identified by NMR, MS and TLC. And the cytotoxic activity of compounds 3, 6, 8, 9, 11, 14, 15 were detected by MTS assay. Results Sixteen compounds were isolated from D. wardianum. They were identified as amotin (1), aduncin (2), E-ferulic acid eicosyl ester (3), E-ferulic acid docosyl ester (4), tetracosyl p-coumarate (5), 4-hydroxy-3-methoxy cinnamaldehyde (6), dihydroconiferyl alcohol (7), 3,7-dimethoxy-5-hydroxy-1,4-phenanthrenequinone (8), 3-ethoxy-5-hydroxy-7- methoxy-1,4-phenanthrenequinone (9), 4-methoxy-9,10-dihydrophilic-2,7-diol (10), 5,7,4’-trihydroxy dihydroflavone (11), 5,7,4’- trihydroxy-3’,5’-dimethoxy dihydroflavone (12), tricin (13), 3,5,4’-trimethoxy-4-hydroxybibenzyl (14), 3,5,3’-trimethoxy-4’- hydroxybibenzyl (15) and 3,3’-dimethoxy-4,5’-dihydroxybibenzyl (16). Compounds 6 and 8 have tumor growth inhibitory activity on tumor growth in vitro. Conclusion Compounds 3, 5, 6 are isolated from Dendrobium for the first time, and 10, 11, 14, 15 are isolated from D. wardianum for the first time. The active components of D. wardianum need to be further explored.
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Objective: To analyze and predict the Q-marker of Cinnamomi Ramulus in Danggui Sini Decoction based on fingerprint and network pharmacology. Methods: The fingerprints of Cinnamomi Ramulus Decoction and Danggui Sini Decoction were established, and analyzed by using the similarity evaluation system software for chromatographic fingerprint of traditional Chinese medicine (2012 edition); The network pharmacology was used to screen and analyze the function target and pathway of related components of Cinnamomi Ramulus, and the "component-target-pathway" network was constructed to predict the potential Q-marker of Cinnamomi Ramulus in Danggui Sini Decoction. Results: The fingerprints of 15 batches of Cinnamomi Ramulus Decotion and 15 batches of Danggui Sini Decoction were established. The similarity of fingerprints was more than 0.96, and seven common components were identified, including protocatechuic acid, coumarin, cinnamic acid, cinnamaldehyde, cinnamyl alcohol, 2-methoxy cinnamic acid, and 2-methoxy cinnamaldehyde. A total of five active components, seven core target sites and 15 key pathways of Cinnamomi Ramulus were screened out through network pharmacology system, and based on the "Five Principles" of quality markers, 2-methoxy cinnamaldehyde, cinnamaldehyde, and cinnamic acid were predicted as potential quality markers. Conclusion: In this study, the quality markers of Cinnamomi Ramulus in Danggui Sini Decoction are analyzed by fingerprint and network pharmacology, which provides a basis for comprehensive control of the quality of Danggui Sini Decoction, reference for further study on the mechanism of Danggui Sini Decoction, and demonstration for the correlation study of quality markers of compound and single medicine in the classic prescription.
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Objective: To establish a quantitative analysis of multi-components by single marker(QAMS)method for the simultaneous determination of jaceosidin, eupatilin, limoni, evodiamine, rutaecarpine, cinnamyl alcohol, cinnamic acid and cinnamal-dehyde in Changwei San. Methods: The Waters Symmetry C18 column(250 mm×4.6 mm, 5 μm)was used for the separation, and the mobile phase was the acetonitrile(A)and 0.1% phosphoric acid(B)solution in a gradient elution at a flow rate of 1.0 ml/min. The detection wavelengths were set at 345 nm for jaceosidin and eupatilin, 215 nm for limoni, evodiamine and rutaecarpine, and 275 nm for cinnamyl alcohol, cinnamic acid and cinnamaldehyde. With evodiamine as an internal reference standard, the relative correction factors for the other 7 components were established and their contents were calculated with the relative correction factors to achieve the QAMS, and then the differences between the calculated values by QAMS and measured values by the external standard method(ESM) were compared to validate the accuracy and feasibility of the QAMS method. Results: Jaceosidin, eupatilin, limoni, evodiamine, rutaecarpine, cinnamyl alcohol, cinnamic acid and cinnamaldehyde showed good linear relationships within the ranges of 0.98-19.60, 2.67-53.40, 4.06-81.20, 1.98-39.60, 2.69-53.80, 0.56-11.20, 1.49-29.80, and 8.77-175.40 μg/ml(r≥0.9992), whose average recoveries(RSD) were 98.77%(0.96%), 99.38%(1.01%), 100.02%(0.83%), 97.80%(1.40%), 98.91%(1.18%), 96.99% (1.13%), 98.09%(1. 24%)and 99.10%(0.67%), respectively. No significant difference was observed between the calculated values by QAMS and the measured values by ESM. Conclusion: The established QAMS method is simple and accurate, which might be used to evaluate the quality of Changwei San.
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Objective::To establish a rapid evaluation method for Cinnamomi Cortex decoction pieces by near infrared spectroscopy. Method::The contents of coumarin, cinnamalol, cinnamic acid and cinnamaldehyde in 86 batches of Cinnamomi Cortex of different origins were determined by HPLC. And the NIR spectra of different batches of Cinnamomi Cortex were also collected. With NIR spectrum as independent variable and coumarin, cinnamalol, cinnamic acid and cinnamaldehyde as dependent variables, a quantitative analysis model of four components in cinnamon was established by partial least squares method. Result::The correlation coefficients (r) of coumarin, cinnamic alcohol, cinnamic acid and cinnamaldehyde near infrared quantitative analysis models were 0.952 8, 0.977 7, 0.961 9, 0.992 2, root mean square error of cross(RMSEC) were 0.012 2, 0.006 1, 0.004 3, 0.82 g·g-1, root mean square errorof cross-validation(RMSECV) were 0.015 8, 0.011 2, 0.002 0, 1.481 1 g·g-1, and root mean square error of prediction(RMSEP) were 0.017 8, 0.010 3, 0.010 3, 0.005 5, 1.63 g·g-1. Conclusion::The established NIR quantitative analysis model of four active ingredients in Cinnamomi Cortex slices has a good accuracy, and provides a basis for rapid evaluation of the quality of Cinnamomi Cortex slices.
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@#Aims: This study aimed to evaluate and compare the antibacterial activity (AA) of Origanum dubium and Cinnamomum cassia essential oils dissolved in different ratios of three different solvents against Streptococcus mutans. Methodology and results: The essential oils were obtained from O. dubium leaves and C. cassia barks using hydrodistillation method and gas chromatography/mass spectrometry (GC/MS) analyses were performed to identify the compositions. The obtained essential oils were diluted in dimethylsulphoxide (DMSO), Tween 20 and ethanol with concentrations of 10, 20 and 60% respectively. Each oil mixture was further diluted with distilled water to provide different ratios. Then, the AA of the dilutions were evaluated. Comparison of AA of essential oils showed that C. cassia had higher AA than O. dubium for each dilution ratio for Tween and ethanol. Conclusion, significance and impact of this study: The results obtained in our study lead us to affirm that the AA of both oils are dependent on dilution ratios of the solvents and the AA of C. cassia is higher than that of O. dubium except for the 1:8 and 1:16 dilution ratios of DMSO. Increasing ratios of solvents used to dilute the O. dubium and C. cassia essential oils resulted in a decrease in the antimicrobial activity against S. mutans.
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The essential oil (EO) extracted from the bark of Cinnamomum zeylanicum (Czey; also known as cinnamon), mostly derives its properties from its major compound trans-cinnamaldehyde (TCin). The present study evaluated the antimycobacterial activity of the essential oil from Czey (CzeyEO) and TCin against sensitive and resistant clinical isolates of Mycobacterium tuberculosis, as well as the combinatorial effects of CzeyEO and TCin with the anti-tuberculosis (TB) drugs rifampicin (RIF) and isoniazid (INH). The resazurin microtiter assay method was used to determine the minimum inhibitory concentration (MIC) of the components tested on the clinical isolates of M. tuberculosis. The effects of the CzeyEO/RIF, CzeyEO/INH, TCin/RIF, and TCin/INH combinations on the M. tuberculosis H37Rv reference strain were evaluated using the checkerboard method to determine the fractional inhibitory concentration index (FICI). CzeyEO and TCin inhibited all bacterial clinical isolates. In the interactive experiment, CzeyEO and TCin were found to be highly effective in reducing the resistance of resistant M. tuberculosis to RIF and INH. All four tested combinations demonstrated synergistic and additive effects, with no antagonistic effects. The synergistic combinations of CzeyEO/RIF and CzeyEO/INH exhibited FICI values of 0.375 and 0.5, respectively, while the TCin/RIF and TCin/INH combinations exhibited FICI values of 0.31 and 0.5, respectively. These results indicate that CzeyEO and TCin are potential candidates for the treatment of drug-resistant tuberculosis in combination therapy with INH and RIF.
O óleo essencial (EO) extraído da casca do Cinnamomum zeylanicum (CzeyEO), conhecido como canela, tem como seu principal composto o trans-cinamaldeído (TCin). O presente estudo avaliou a atividade antimicobacteriana de CzeyEO e do TCin contra isolados clínicos sensíveis e resistentes de Mycobacterium tuberculosis, bem como os efeitos das associações de CzeyEO e do TCin com os fármacos anti-TB, rifampicina (RIF) e isoniazida (INH). A técnica de ensaio de microtitulação da resazurina foi utilizada para determinar a concentração inibitória mínima (CIM) dos componentes testados nos isolados clínicos de M. tuberculosis. Os efeitos das associações CzeyEO/RIF, CzeyEO/INH, TCin/RIF e TCin/INH contra a cepa de referência H37Rv de M. tuberculosis foram avaliados pelo método Checkerboard, determinando o índice de concentração inibitória fracionária (ICIF). Todos os isolados clínicos bacterianos foram inibidos por CzeyEO e TCin. As interações de CzeyEO e TCin foram altamente eficazes na redução da resistência do M. tuberculosisresistente a RIF e INH. Todas as quatro combinações testadas resultaram em efeitos sinérgicos e aditivos, sem efeito antagônico. Ambas as associações de sinergismo de CzeyEO/RIF e CzeyEO/INH mostraram valores de ICIF de 0,375 e 0,5, enquanto as associações de TCin/RIF e TCin/INH apresentaram valores de ICIF de 0,31 e 0,5. CzeyEO e TCin são potenciais candidatos em terapia combinada com INH e RIF para o tratamento da tuberculose resistente.
Subject(s)
Tuberculosis , Cinnamomum zeylanicum , Anti-Bacterial Agents , Mycobacterium tuberculosisABSTRACT
Objective@#To investigate the effect of cinnamaldehyde (CIN) on the inflammation and apoptosis on human umbilical vein endothelial cells (HUVECs) induced by lipopolysaccharide (LPS), and to explore the potential mechanisms.@*Methods@#HUVECs were divided in to 8 groups: blank control group, LPS group, LPS+(low, medium, high) dose CIN groups and (low, medium, high) CIN groups. Cell cytotoxicity was determined by trypan blue staining, mRNA expression of the inflammatory factors was determined by RT-PCR,apoptosis was determined by TUNEL staining,the signal pathway was determined by Western blot.@*Results@#(1) Cell viability:compared with the control group,cell survival rate was significantly lower in the LPS group (P<0.01), while the survival rates were all significantly higher in the 3 LPS+CIN groups than in the LPS group (all P<0.01) in a concentration-dependent manner. (2) The mRNA expression of the inflammation factors: compared with the control group, mRNA expression of the inflammation factors were all increased in the LPS group (all P<0.01),while the effect of LPS could be significantly reversed by cotreatment with CIN in a concentration-dependent manner (all P<0.01). Compared with control group, the mRNA expression of the inflammation factors in the LPS group were all enhanced in a time-dependent manner (0,6,12,24 h),which could be significantly downregulated by cotreatment with LPS+CIN (high dose) in a time-dependent manner. (3) Cell apoptosis: compared with the control group, the apoptosis rate was significantly higher in the LPS group (P<0.01), while this effect could be significantly reversed by the cotreatment with CIN (high dose) (P<0.01). (4) Signaling pathway: compared with the control group, the phosphorylation of iκBα, p65 in HUVECs treated with LPS were rapidly up-regulated compared with their corresponding total proteins and the expression of TLR4 (all P<0.01), while the degree of p-iκBα/iκBα, p-p65/p65 and TLR4 could be significantly suppressed by cotreatment with CIN (high dose) (all P<0.01).@*Conclusion@#CIN can attenuate LPS induced inflammation and apoptosis in HUVECs, possibly by inhibiting the activation of NF-κB signaling pathway.
ABSTRACT
Objective: To investigate the effect and mechanism of cinnamaldehyde on the angiogenesis of diabetic retinopathy, and the effect of cinnamaldehyde on vascular endothelial growth factor (VEGF) induced proliferation, migration, tube formation and Janus kinase 2/signal transducer and activator of transcription 3 (JAK2/STAT3) pathway of EA.hy 926 cells were observed. Method:EA.hy 926 cells were divided into normal control group, model group (7 μg·L-1 VEGF), and VEGF+cinnamaldehyde group (60, 90, 120, 150 μmol·L-1). The methyl thiazolyl tetrazolium (MTT) assay and scratch test were used to observe the effect of cinnamaldehyde on the proliferation and migration of EA. hy 926 cells induced by VEGF. EA. hy 926 cells were divided into normal control group, model group (7 μg·L-1 VEGF), and VEGF+cinnamaldehyde group (90, 150 μmol·L-1). The tube formation experiment was used to observe the effect of cinnamaldehyde on the tube formation of EA. hy 926 cells induced by VEGF. EA. hy 926 cells were divided into normal control group, model group (7 μg·L-1 VEGF), VEGF+AG490 group (50 μmol·L-1), VEGF+cinnamaldehyde group (90 μmol·L-1), VEGF+cinnamaldehyde group (150 μmol·L-1), and VEGF+cinnamaldehyde group (150 μmol·L-1)+AG490 group (50 μmol·L-1). Western Blot method was used to explore the effect of cinnamaldehyde on the JAK2/STAT3 signaling pathway in EA.hy 926 cells induced by VEGF. Result:Compared with the control group, model group obviously promoted the proliferation and migration of EA.hy 926 cells(P-1) significantly suppressed VEGF-induced proliferation and migration of EA.hy 926 cells (P-1) showed an obvious inhibitory effect on the number of nodes, junctions and meshes of tubules (PPPP-1) significantly reduced the expressions of P-JAK2, P-STAT3, STAT3 proteins (P-1) obviously reduced the expressions of p-STAT3 and STAT3 proteins (PPConclusion:Cinnamaldehyde showed a significantly inhibitory effect on the proliferation, migration and tube formation of VEGF-induced EA.hy 926 cells, which was related to the inhibition of the activation of JAK2/STAT3 pathway.
ABSTRACT
Cinnamomi Ramulus and Cinnamomi Cortex are widely used to treat paralysis in traditional Chinese medicine (TCM). There are numerous and complicated relative records in ancient literatures. Doctors often use Cinnamomi Ramulus to dispel wind and cold, remove blood stasis and combine with warm-natured and heat-natured herbs to treat excess paralysis and early-stage paralysis. And Cinnamorni Cortex is used to warm and invigorate kidney Yang and combine with warm-benefiting herbs to treat deficiency paralysis and chronicle paralysis. However, modern pharmaceutical studies reported that their active substances are almost the same. The active substances in Cinnamomi Cortex are more than those in Cinnamomi Ramulus. The mechanisms of treating paralysis include:suppressing inflammation and regulating immunity by down-regulating nuclear factors(NF)-κB, mitogen activated protein kinase(MAPK), Janus kinase-signal transducers/activators of transcription(JAK/STAT) signaling pathways, regulating cell proliferation by inhibiting the proliferation of fibroblasts, osteoclasts and bone marrow mesenchymal stem cells and promoting the proliferation of osteoblast, resisting oxidation by scavenging oxygen free radicals, regulating pain by mediating TRPA1 and TRPV1,and enhancing substance metabolism and losing weight by regulating the secretion of intestinal hormones (Ghrelin, GLP-1) and improving insulin resistance. The main active ingredient Cinnamaldehyde is unstable in vivo and easily oxidized to cinnamic acid. The toxicity of the two medicines and their components are relatively low. This paper reviews and analyses relative records in ancient literatures, traditional Chinese medicine cognition of their effects in treating paralysis, the achievements and problems of chemical,pharmacological,pharmacokinetic and toxicological researches in recent years, with the aim to provide theoretical basis for further research and application.