Antibacterial and hemolytic activity of extracts and compounds obtained from epicarps and seeds of Garcinia madruno(Kunth) Hammel / Actividad antimicrobiana y hemolítica de extractos y compuestos obtenidos del epicarpio y las semillas de Garcinia madruno (Kunth) Hammel

This paper describes the evaluation of the antimicrobial and hemolytic activity of the hexane, dichloromethane, ethyl acetate and methanol extracts from seeds and epicarps of Garcinia madruno; as well garcinol, morelloflavone and volkensiflavone isolated from the same species. In the preliminary test of bacterial susceptibility, hexane extracts from seeds and epicarps and the three compounds tested only displayed inhibitory growth effect against Gram-positive bacteria. The minimum inhibitory concentrations of extract and compounds ranging from 86.6 to 1253.4 µg/mL. The hemolytic activity was assessed; however, except for the methanol extract from seeds, none of the samples studied induced hemolysis. Thus, our results suggest that extracts and compounds from G. madruno have the potential to be used in the control of pathologies associated to Gram-positive bacteria. This is the first report of the antimicrobial and hemolytic activity of extracts of different polarity obtained from seeds and epicarps of this edible species.

El presente artículo describe la evaluación de la actividad antimicrobiana y hemolítica de los extractos de hexano, diclorometano, acetato de etilo y metanol, obtenidos de la semilla y el epicarpio de Garcinia madruno; así como de garcinol, morelloflavona y volkensiflavona; aislados de la misma especie. En el ensayo de susceptibilidad bacteriana, tanto el extracto de hexano obtenido a partir de la semilla y el epicarpio, y los tres compuestos aislados, únicamente mostraron actividad inhibitoria del crecimiento contra bacterias Gram-positivas. La concentración mínima inhibitoria presentó valores entre 86.6 y 1253.4 µg/mL. También se estableció la actividad hemolítica; sin embargo, con excepción del extracto metanólico obtenido a partir de las semillas, ninguna de las muestras evaluadas indujo hemólisis. Por lo tanto, los resultados sugieren que los extractos y compuestos de G. madruno tienen el potencial de ser usados en el control de bacterias Gram-positivas asociadas a diversas patologías. Este es el primer reporte de actividad antimicrobiana y hemolítica de extractos de diferente polaridad obtenidos de las semillas y epicarpios de esta especie comestible.

Protective Effect of Procyanidin B2 on Acute Liver Injury Induced by Aflatoxin B in Rats / 生物医学与环境科学（英文）

Objective@#This study aimed to explore the protective effect of procyanidin B2 (PCB2) on acute liver injury induced by aflatoxin B (AFB ) in rats.@*Methods@#Forty Sprague Dawley rats were randomly divided into control, AFB , AFB + PCB2, and PCB2 groups. The latter two groups were administrated PCB2 intragastrically (30 mg/kg body weight) for 7 d, whereas the control and AFB groups were given the same dose of double distilled water intragastrically. On the sixth day of treatment, the AFB and AFB + PCB2 groups were intraperitoneally injected with AFB (2 mg/kg). The control and PCB2 groups were intraperitoneally administered the same dose of dimethyl sulfoxide (DMSO). On the eighth day, all rats were euthanized: serum and liver tissue were isolated for further examination. Hepatic histological features were assessed by hematoxylin and eosin-stained sections. Weight, organ coefficient (liver, spleen, and kidney), liver function (serum alanine aminotransferase, aspartate aminotransferase, alkaline phosphatase, total bilirubin, and direct bilirubin), oxidative index (catalase, glutathione, superoxide dismutase, malondialdehyde, and 8-hydroxy-2'-deoxyguanosine), inflammation factor [hepatic interleukin-6 (IL-6) mRNA expression and serum IL-6], and bcl-2/bax ratio were measured.@*Results@#AFB significantly caused hepatic histopathological damage, abnormal liver function, oxidative stress, inflammation, and bcl-2/bax ratio reduction compared with DMSO-treated controls. Our results indicate that PCB2 treatment can partially reverse the adverse liver conditions induced by AFB .@*Conclusion@#Our findings indicate that PCB2 exhibits a protective effect on acute liver injury induced by AFB .

The effect of procyanidin on periprosthetic osteolysis caused by TCP wear particles in the mouse calvaria and its mechanism / 中国应用生理学杂志

OBJECTIVE@#To investigate the protective effects of procyanidin on periprosthetic osteolysis caused by tricalcium phosphate (TCP) wear particles in the mouse calvaria and its mechanism.@*METHODS@#Forty-eight male ICR mice were randomly divided into sham group, TCP group, and procyanidin (0.2 mg/kg, 1 mg/kg, 5 mg/kg)-treated group (n=12). A periprosthetic osteolysis model in the mouse calvaria was established by implanting 30 mg of TCP wear particles onto the surface of bilateral parietal bones following removal of the periosteum. On the 2 day post-operation, procyanidin (1 mg/kg, 5 mg/kg) was locally injected to the calvaria under the periosteum every other day. After 2 weeks, all the mice were sacrificed to collect the blood samples and the calvaria. Periprosthetic osteolysis and osteoclastogenesis in the mouse calvaria were observed by tartrate resistant acid phosphatase (TRAP) staining and HE staining. mRNA levels of TRAP, capthesin K, c-Fos and NFATc1 in the periprosthestic bone tissue were examined by real-time fluorescence quantitative PCR. Serum contents of total anti-oxidation capacity (T-AOC) and MDA, and superoxide dismutase (SOD) activity were determined by chemical colorimetry. Protein expressions of autophagic biomarkers such as Beclin-1 and LC-3 in periprosthetic bone tissue of the calvaria were examined by Western blot.@*RESULTS@#Compared with sham group, periprosthetic osteolysis, osteoclastogenesis, mRNA levels of TRAP, capthesin K, c-Fos and NFATc1, and serum MDA content were increased significantly in the TCP group (P＜0.05), whereas serum T-AOC level and SOD activity were decreased. The protein expressions of Beclin-1 and LC-3, and the conversion of LC3-II from LC3-I were both up-regulated markedly in the mouse calvaria of TCP group (P＜0.05). Compared with TCP group, osteolysis, osteoclastogenesis, mRNA levels of TRAP, capthesin K, c-Fos and NFATc1 and serum MDA content were decreased obviously in the procyanidine group (P＜0.05), serum T-AOC level and SOD activity were increased, the expressions of Beclin-1 and LC-3, and the conversion of LC3-II from LC3-I were down-regulated obviously in the mouse calvaria of procyanidin group (P＜0.05).@*CONCLUSION@#Procyanidin has a protective effect of periprosthetic osteolysis caused by TCP wear particles in the mouse calvaia, its mechanism may be mediated by inhibition of oxidative stress and autophagy.

Anti-tumor activity of HIS-4,a biflavonoid from Resina draconis,on human hepatoma HepG2 and SK-HEP-1 cells / 中国中药杂志

The research of anti-hepatocellular carcinoma(HCC) drug has attracted more and more attention. Natural products are the important source of active compounds for cancer treatment. A biflavonoid HIS-4 was isolated from Resina draconis in our previous study. MTT assay, hoechst staining, and flow cytometry analysis were used to investigate the effects of HIS-4 on the proliferation and apoptosis of human hepatoma HepG2 and SK-HEP-1 cells. Moreover, the effects of HIS-4 on the migration and invasion ability of HepG2 and SK-HEP-1 cells were evaluated by wound healing assay and Transwell assay. In addition, MTT assay, flow cytometry analyses, Hoechst staining, wound healing assay, Transwell assay, and tube formation assay were used to explore the anti-angiogenic activity of HIS-4 in human umbilical vein endothelial cells(HUVECs). Mechanistically, the HIS-4 regulatory of signal pathways in H9 epG2 and SK-HEP-1 cells were analyzed by Western blot. This results showed that HIS-4 suppressed the proliferation of human hepatoma HepG2 and SK-HEP-1 cells. Moreover HIS-4 induced their apoptosis of HepG2 and SK-HEP-1 cells. HIS-4 inhibited the migration and invasion of HepG2 and SK-HEP-1 cells. Additionally, HIS-4 exhibited angiogenesis effects. Mechanistically, up-regulation of MAPK signaling pathway and down-regulation of mTOR signaling pathway may be responsible for anti-hepatoma activity of HIS-4. Therefore, HIS-4 may be a promising candidate drug for HCC treatment.

Protective effect of procyanidin B2 on intestinal barrier and against enteritis in a mouse model of trinitrobenzene sulphonic acid-induced colitis / 南方医科大学学报

OBJECTIVE@#To investigate the protective effect of procyanidin B2 (PCB2) on the intestinal barrier and against enteritis in mice with trinitrobenzene sulphonic acid (TNBS)-induced colitis and explore the possible mechanism.@*METHODS@#A mouse model of TNBS-induced colitis was established in male Balb/c mice aged 6-8 weeks. The successfully established mouse models were randomly divided into PCB2 treatment group (=10) and model group (=10) and were treated with daily intragastric administration of PCB2 (100 mg/kg, 0.2 mL) and 0.2 mL normal saline, respectively. After 4 weeks, the disease symptoms, intestinal inflammation, intestinal mucosal cell barrier function and the changes in PI3K/AKT signaling were evaluated using HE staining, immunofluorescence assay and Western blotting.@*RESULTS@#The disease activity index of the mice was significantly lower and the mean body weight was significantly greater in PCB2 group than in the model group in the 3rd and 4th weeks of intervention ( < 0.05). The levels of colonic inflammation and intestinal mucosal inflammatory mediators IL-1β and TNF-α were significantly lower while IL-10 was significantly higher in PCB2 group than in the model group ( < 0.05). Compared with those in the model group, the mice in PCB2 treatment group showed a significantly lower positive rate of bacterial translocation in the mesenteric lymph nodes and a lower thiocyanate-dextran permeability of the intestinal mucosa ( < 0.05). Western blotting showed that PCB2 treatment significantly increased the expressions of claudin-1 and ZO-1 ( < 0.05) and significantly lowered the expression levels of p-PI3K and p-AKT in the intestinal mucosa as compared with those in the model group ( < 0.05).@*CONCLUSIONS@#PCB2 suppresses intestinal inflammation and protects intestinal mucosal functions and structural integrity by inhibiting intestinal PI3K/AKT signaling pathway, suggesting the potential of PCB2 as a new drug for Crohn's disease.

Active compounds and derivatives of camellia sinensis responding to erosive attacks on dentin

Abstract This research explored the potential of Camellia sinensis-derived teas and active compounds to be used as treatments to prevent dentin wear. Human root dentin slabs were randomly assigned to 5 groups (n = 10) as follows: distilled water (DW, control), epigallocatechin-3-gallate (EGCG), theaflavin gallate derivatives (TF), commercial green tea (GT), and commercial black tea (BT). The samples were submitted to a pellicle formation and an erosive cycling model (5x/day, demineralization using 0.01 M hydrochloric acid/60 s) followed by remineralization (human stimulated saliva/60 min) for three days. The samples were treated for 5 min using the test group solutions between the erosive cycles. Dentin changes were assessed with profilometry analysis and FT-Raman spectroscopy. The data regarding wear were analyzed by ANOVA followed by Tukey's test (p < 0.05). EGCG, TF derivatives, and both regular teas significantly suppressed erosive dentin loss (38-47%, p < 0.05). No obvious changes in the Raman spectra were detected in the specimens; however, the DW group had a minor relationship of 2880/2940 cm−1. The phenolic contents in both green and black tea and the important catechins appear to have protective effects on dentin loss.

Comparison of antioxidant effects of kolaviron and vitamin C interventions on testicular structures following nevirapine administration in Sprague-Dawley rats / Comparación de los efectos antioxidantes en la intervención con kolaviron y vitamina C sobre las estructuras testiculares después de la administración de nevirapina en ratas Sprague-Dawley

Testicular toxicity has been implicated in highly active anti-retroviral therapy (HAART) treatment. Hence there is need to identify an effective antioxidant product that can alleviate testicular necrosis due to HAART administration. Forty eight adult male Sprague-Dawley rats were used in this study. The animals were divided into eight (8) groups: A-H (n= 6). Group A animals received normal saline as the control; Group B was given Nevirapine (Nv); Group C was given Kolaviron (Kv); Group D was given vitamin C; Group E was given Nv and Kv; Group F was given Nv and Vitamin C; Group G was given Nv for 56 d and Kv for 28 d serving as a withdrawal group; Group H was given corn oil. Nv, Kv and Vit. C were given at 1.54, 200 and 250 (mg·kg)/bw respectively while all administrations were through oral gavage. The body weights were taken every other day. Thereafter, they were anaesthetized with halothane. The testes were excised, weighed, fixed in Bouin's fluid and stained with H&E while the epididymes removed for semen fluid analyses. The results showed a significant (P<0.05) decrease in sperm motility in group E (Nevirapine + kolaviron) when compared with group F (Nevirapine + Vitamin C) while Sperm count was not significantly different (P>0.05) across the groups. The testicular histoarchitectural studies revealed indistinct spermatogonia, necrotic interstititial endocrine cells in the altered interstitial space, fragmented spermatids, atrophy of mature spermatocytes, degenerated germ cells, obliterated seminiferous tubules lumen, undifferentiated spermatogonia and cellular debris in the somniferous tubules lumen of nevirapine administered group but normal across the other groups. In the testis, there were no significant reduction in SOD, Catalase and GPx activities but a significant decrease in GST activity (P<0.001) when group E was compared with group F. In conclusion, vitamin C presents a better remediation in nevirapine induced spermiotoxicity compared to kolaviron in Sprague-Dawley rats.

La toxicidad testicular ha sido implicada en la terapia antirretroviral altamente activa (TARAA). Por lo tanto existe la necesidad de identificar un producto antioxidante eficaz que pueda aliviar la necrosis testicular en la administración de la TARAA. Cuarenta y ocho ratas macho Sprague-Dawley adultas fueron utilizadas. Los animales se dividieron en ocho (8) grupos: AH (n= 6). Grupo A, animales recibieron solución salina normal como el control; Grupo B, recibió Nevirapina (Nv); Grupo C, recibió Kolaviron (Kv); Grupo D, recibió vitamina C; Grupo E, recibió Nv y Kv; Grupo F, recibió Nv y vitamina C; Grupo G, recibió Nv durante 56 d y Kv por 28 d como un grupo de retirada; Grupo H, recibió aceite de maíz. Nv, Kv y Vit. C se administraron en dosis de 1, 54, 200 y 250 (mg · kg) de peso corporal respectivamente; todas las administraciones fueron por sonda oral. Los pesos corporales se tomaron cada dos días. A partir de ese momento los animales fueron anestesiados con halotano. Los testículos fueron extirpados, pesados y fijados en solución de Bouin y teñidos con H&E, mientras que el epidídimo se retiró para analizar el semen. Los resultados mostraron un descenso (p<0,05) en la motilidad de los espermatozoides en el grupo E (Nevirapina + Kolaviron) en comparación con el grupo F (Nevirapina + vitamina C), mientras que el recuento espermático no mostró diferencias significativas (P>0,05) entre los grupos. El estudio de la histoarquitectura testicular reveló espermatogonias indiferenciadas, con células intersticiales necróticas en el espacio intersticial y espermátidas fragmentadas. Además, en el grupo que recibió Nevirapina mostró espermatocitos maduros atrofiados, degeneración de células germinales, lumen de los túbulos seminíferos obliterados, espermatogonias indiferenciadas y restos celulares en el lumen de los tubulos seminíferos. En el resto de los grupos los resultados fueron normales. En el testículo hubo una reducción significativa en las actividades de la superóxido dismutasa, catalasa y glutatión peroxidasa, pero una disminución significativa en la actividad glutatión S-transferasa (P <0,001) al comparar los grupo E y F.

In vivo antileishmanial activity and chemical profile of polar extract from Selaginella sellowii

The polar hydroethanolic extract from Selaginella sellowii(SSPHE) has been previously proven active on intracellular amastigotes (in vitro test) and now was tested on hamsters infected with Leishmania (Leishmania) amazonensis (in vivo test). SSPHE suppressed a 100% of the parasite load in the infection site and draining lymph nodes at an intralesional dose of 50 mg/kg/day × 5, which was similar to the results observed in hamsters treated with N-methylglucamine antimonate (Sb) (28 mg/Kg/day × 5). When orally administered, SSPHE (50 mg/kg/day × 20) suppressed 99.2% of the parasite load in infected footpads, while Sb suppressed 98.5%. SSPHE also enhanced the release of nitric oxide through the intralesional route in comparison to Sb. The chemical fingerprint of SSPHE by high-performance liquid chromatography with diode-array detection and tandem mass spectrometry showed the presence of biflavonoids and high molecular weight phenylpropanoid glycosides. These compounds may have a synergistic action in vivo. Histopathological study revealed that the intralesional treatment with SSPHE induced an intense inflammatory infiltrate, composed mainly of mononuclear cells. The present findings reinforce the potential of this natural product as a source of future drug candidates for American cutaneous leishmaniasis.

A new biflavone glucoside from the roots of Stellera chamaejasme / 中国天然药物

The present study investigated the chemical constituents of the roots of Stellera chamaejasme (Thymelaeaceae). One new biflavone glucoside (1), along with other thirteen known compounds (2-14), was isolated by repeated column chromatographic methods and their structures were elucidated on the basis of spectral analyses. The cytotoxic activities of selected compounds were evaluated against four human cancer cell lines (A549, BEL-7402, HCT-116, and MDA-MB-231) by the SRB assay method. Compound 9 showed remarkable cytotoxicity against BEL-7402 with IC50 value being 0.65 μg·mL(-1); compounds 7, 8, and 12 exhibited significant cytotoxic activity against A549 with IC50 values being 2.38, 1.57, and 2.35 μg·mL(-1), respectively.

Isochamaejasmin induces apoptosis in leukemia cells through inhibiting Bcl-2 family proteins / 中国天然药物

The biflavonoid isochamaejasmin is mainly distributed in the root of Stellera chamaejasme L. (Thymelaeaceae) that is used in traditional Chinese medicine (TCM) to treat tumors, tuberculosis, and psoriasis. Herein, isochamaejasmin was found to show similar bioactivity against Bcl-2 family proteins to the reference Bcl-2 ligand (-)-gossypol through 3D similarity search. It selectively bound to Bcl-xl and Mcl-1 with Ki values being 1.93 ± 0.13 μmol·L(-1) and 9.98 ± 0.21 μmol·L(-1), respectively. In addition, isochamaejasmin showed slight growth inhibitory activity against HL-60 with IC50 value being 50.40 ± 1.21 μmol·L(-1) and moderate growth inhibitory activity against K562 cells with IC50 value being 24.51 ± 1.62 μmol·L(-1). Furthermore, isochamaejasmin induced apoptosis of K562 cells by increasing the intracellular expression levels of proteins of the cleavage of caspase-9, caspase-3, and PARP which involved in the Bcl-2-induced apoptosis pathway. These results indicated that isochamaejasmin induces apoptosis in leukemia cells by inhibiting the activity of Bcl-2 family proteins, providing evidence for further studying the underlying anti-cancer mechanism of S. chamaejasme L.

In vitro activity of the hydroethanolic extract and biflavonoids isolated from Selaginella sellowii on Leishmania (Leishmania) amazonensis

This study is the first phytochemical investigation of Selaginella sellowii and demonstrates the antileishmanial activity of the hydroethanolic extract from this plant (SSHE), as well as of the biflavonoids amentoflavone and robustaflavone, isolated from this species. The effects of these substances were evaluated on intracellular amastigotes of Leishmania (Leishmania) amazonensis, an aetiological agent of American cutaneous leishmaniasis. SSHE was highly active against intracellular amastigotes [the half maximum inhibitory concentration (IC50) = 20.2 µg/mL]. Fractionation of the extract led to the isolation of the two bioflavonoids with the highest activity: amentoflavone, which was about 200 times more active (IC50 = 0.1 μg/mL) and less cytotoxic than SSHE (IC50 = 2.2 and 3 μg/mL, respectively on NIH/3T3 and J774.A1 cells), with a high selectivity index (SI) (22 and 30), robustaflavone, which was also active against L. amazonensis (IC50 = 2.8 µg/mL), but more cytotoxic, with IC50 = 25.5 µg/mL (SI = 9.1) on NIH/3T3 cells and IC50 = 3.1 µg/mL (SI = 1.1) on J774.A1 cells. The production of nitric oxide (NO) was lower in cells treated with amentoflavone (suggesting that NO does not contribute to the leishmanicidal mechanism in this case), while NO release was higher after treatment with robustaflavone. S. sellowii may be a potential source of biflavonoids that could provide promising compounds for the treatment of cutaneous leishmaniasis.

Determinación de biflavonoides en diferentes partes de la especie Garcinia bakeriana (Urb) Borhidi / Determination of biflavonoids in different parts of Garcinia bakeriana (Urb) Borhidi

INTRODUCCIÓN: el género Garcinia produce una gran variedad de metabolitos secundarios representados por xantonas, acilfloroglucinoles y biflavonoides fundamentalmente. Sin embargo, existe muy poca información sobre la composición química de las especies cubanas pertenecientes a este género. OBJETIVO: determinar la presencia de 11 biflavonoides en las hojas, la corteza del tallo y el látex de Garcinia bakeriana (Urb) Borhidi. MÉTODOS : los extractos de las hojas, látex y la corteza del tallo de G. bakeriana fueron comparados empleando un método de cromatografía líquida de ultra alta eficacia (CLUAE) y 11 biflavonoides como sustancias de referencia. RESULTADOS: los biflavonoides GB-1A, GB-2A, glicósido de GB-2A, glicósido de morelloflavona, 4´´´metoxi- I3,II8-biapigenina, I3,II8-biapigenina, amentoflavona y 4´´´-metoxiamentoflavona fueron detectados como constituyentes de las hojas y la corteza del tallo de G. bakeriana. CONCLUSIONES: la especie G. bakeriana presenta biflavonoides como constituyentes de las hojas y la corteza del tallo. Además, la metodología de trabajo desarrollada contribuye al conocimiento de la composición química de la flora cubana y podría constituir una alternativa, rápida y de bajo consumo de disolventes, para el estudio comparativo de especies endémicas cubanas de escasa distribución y abundancia(AU)

INTRODUCTION: previous studies have revealed genus Garcinia to be a rich source of secondary metabolites, namely xanthones, acylphloroglucinols and bioflavonoids. However, the chemical composition of Cuban species in this genus is almost unknown. OBJECTIVE: to determine the presence of 11 biflavonoids in Garcinia bakeriana leaves, latex and stem bark. METHODS: leaves, latex and stem bark extracts of G. bakeriana were compared by using an ultra high performance liquid chromatography method (UPLC) and 11 biflavonoid standards. RESULTS: biflavonoids GB-1A, GB-2A, GB-2A glycoside, morelloflavone glycoside, 4´´´methoxy- I3,II8-biapigenin, I3,II8-biapigenin, amentoflavone y 4´´´-methoxyamentoflavone were detected as components in G. bakeriana leaves and stem bark. CONCLUSIONS: G. Bakeriana species has biflavonoids as components of its leaves and stem bark. The work methodology described in this paper helps to expand the knowledge about the chemical composition of the Cuban flora and may represent a rapid method with low dissolver consumption for the comparative study of poorly distributed and non abundant Cuban endemic species(AU)

Anti-Mycobacterium tuberculosis activity and cytotoxicity of Calophyllum brasiliense Cambess (Clusiaceae)

We evaluated the in vitro anti-Mycobacterium tuberculosis activity and the cytotoxicity of dichloromethane extract and pure compounds from the leaves of Calophyllum brasiliense. Purification of the dichloromethane extract yielded the pure compounds (-) mammea A/BB (1), (-) mammea B/BB (2) and amentoflavone (3). The compound structures were elucidated on the basis of spectroscopic and spectrometric data. The contents of bioactive compounds in the extracts were quantified using high performance liquid chromatography coupled to an ultraviolet detector. The anti-M. tuberculosis activity of the extracts and the pure compounds was evaluated using a resazurin microtitre assay plate. The cytotoxicity assay was performed in J774G.8 macrophages using the 3-(4,5-dimethyl thiazol-2-yl)-2,5-diphenyl tetrazolium bromide colourimetric method. The quantification of the dichloromethane extract showed (1) and (2) at concentrations of 31.86 ± 2.6 and 8.24 ± 1.1 µg/mg of extract, respectively. The dichloromethane and aqueous extracts showed anti-M. tuberculosis H37Rv activity of 62.5 and 125 µg/mL, respectively. Coumarins (1) and (2) showed minimal inhibitory concentration ranges of 31.2 and 62.5 µg/mL against M. tuberculosis H37Rv and clinical isolates. Compound (3) showed no activity against M. tuberculosis H37Rv. The selectivity index ranged from 0.59-1.06. We report the activity of the extracts and coumarins from the leaves of C. brasiliense against M. tuberculosis.

Amentoflavone induces apoptosis in SW480 human colorectal cancer cells via regulating β-catenin and caspase-3 expressions / 南方医科大学学报

<p><b>OBJECTIVE</b>To investigate the role of β-catenin and caspase-3 in amentoflavone-induced apoptosis of human colorectal cancer SW480 cells.</p><p><b>METHODS</b>MTT assay was used to detect the viability of SW480 cells exposed to amentoflavone, and flow cytometry was employed to assess the cell apoptosis. Western blotting was performed to determine the protein expressions of β-catenin and caspase-3 in the exposed cells.</p><p><b>RESULTS</b>Amentoflavone dose-dependently inhibited the viability of SW480 cells, and a high concentration of amentoflavone (150 µmol/L) obviously induced apoptosis of the cells. Amentoflavone exposure caused significantly increased expression of caspase-3 and suppressed β-catenin expression in the cells.</p><p><b>CONCLUSION</b>Amentoflavone-induced apoptosis in SW480 human colorectal cancer cells is associated with altered expressions of β-catenin and caspase-3.</p>

Hypolipidemic effect of a novel biflavonoid from shells of Camellia oleifera (Abel.).

Camellia oleifera Abel. [C. oleosa (Lour.) Rehd.], an evergreen plant, is used for healthful oil production, but the shells are always discarded and need to be utilized. The present study was undertaken to explore the effect of extracts from the shells of C. oleifera on adjusting cardiovascular system. A flavonoid was obtained by reflux extraction of the shells in 70% methanol, hydrolysis in 2 M hydrochloric acid, and crystallization in acetone. Its structure was identified as a novel biflavonoid. Mice model of hyperlipidemia was setup by high fat diet for 30 d to evaluate the hypolipidemic effect of the biflavonoid at dose of 50, 100 and 200 mg/kg/d (ig). Antioxidative activity was determined by levels of malondialdehyde (MDA), superoxidase dismutase (SOD) and glutathione peroxidase (GSH-Px) in mice serum. The biflavonoid significantly controlled mice weight and liver coefficient, decreased the content of total cholesterol and triglyceride, promoted the level of high density lipoprotein in a dose dependent manner. The significant decrease of MDA content and increase of SOD and GSH-Px activity indicated it enhanced antioxidative capacity in vivo and was ascribed to hypolipidemic effect. The biflavonoid is useful in the prevention of high fat diet induced hyperlipidemia.

Some bioactive potentials of two biflavanols isolated from Garcinia kola on cadmium-induced alterations of raw U937 cells and U937-derived macrophages

OBJECTIVE@#To investigate the abilities of two flavonoids - Garcinia biflavanol-1 (GB-1) and Garcinia biflavanol-2 (GB-2) from Garcinia kola (G. kola) in reducing cadmium-induced effects on raw U937 cells and U937-derived macrophages.@*METHODS@#Macrophage U937 cells were incubated with cadmium followed by treatment with the flavonoids and cell viability assessed via trypan blue staining. In the other experiment, the U937 cells were transformed to the macrophage form and treated with cadmium in order to activate them. The cells were later incubated with the flavonoids and finally the supernatant of each cell culture was analysed for the secretion of nitric oxide, catalyse activity, and the release of tumour necrosis factor-alpha, interleukin-1 and interleukin-2 as indices of macrophage activation. Quercetin (a flavonol) was used as the reference flavonoid in all experiments.@*RESULTS@#It revealed that the flavonoids significantly increased the viability of the cells and also reduced the cadmium-induced activation of the macrophage cells in a concentration-dependent manner. The flavanols GB-1 and GB-2 possessed higher activities than quercetin in all cases (P<0.05). Garcinia biflavanol-2 possessed a higher bioactivity than GB-1 significantly (P<0.05).@*CONCLUSIONS@#In addition to corroborating the several reported importance of G. kola as a potential neutraceutical and pharmacological condiment, the study also clearly indicates the role hydroxylation especially at the 3'- position of polyphenols could play in enhancing bioactivities of flavonoids.

Protection effect of amentoflavone in Selaginella tamariscina against TNF-alpha-induced vascular injury of endothelial cells / 药学学报

This study is to observe the protection effect of amentoflavone (AMT) in Selaginella tamariscina against TNF-alpha-induced vascular inflammation injury of endothelial cells. On the basis of TNF-alpha induced human umbilical vein endothelial cell, observe the influence of AMT on endothelial active factor, the contents of SOD and MDA, the protein expression of vascular endothelial adhesion molecules and inflammatory factor; study the effect of its common related signal pathways such as NF-kappaB; research the effect of AMT against TNF-a induced human umbilical vein endothelial cell injury by means of MTT, ELISA, Western blotting and the cell immunofluorescence. The results showed that AMT could increase the content of NO and decrease the levels of VCAM-1, E-selectin, IL-6, IL-8 and ET-1; enhance the activity of SOD, reduce the content of MDA; downregulate the protein expressions of VCAM-1, E-selectin, NF-kappaBp65 and up-regulate IkappaBalpha, attenuate the NF-kappaBp65 transfer to cell nucleus. AMT has the effect of protect vascular endothelial and maybe via the signal pathway of NF-kappaB to down-regulate the inflammation factor and oxidative damage factor of downstream.

Inhibitory effect and mechanism of procyanidin from vaccinium on isoprenaline-induced myocardial fibrosis in rats / 中国中药杂志

<p><b>OBJECTIVE</b>To detect the effect and mechanism of procyanidin foom vaccinium (PC) on myocardial fibrosis in rats.</p><p><b>METHOD</b>The myocardial fibrosis model in rats was built by subcutaneous injection of 5 mg x kg(-1) x d(-1) of isoprenaline (Iso) for 7 days in vivo while intragastrically administrating PC 100, 200 and 400 mg x kg(-1) x d(-1) for 14 days. Following the model was established, myocardial indexes (heart weight/body weight, HW/BW and left ventricalar weight/body weight, LVW/BW) were measured. Besides, angiotensin II and I , III collagen quantification levels in blood serum were determined respectively by ELISA. The change in the content of nitric oxide (NO) in blood serum was determined with colorimetry. The content of malondialdehyde (MDA) in left ventricle was assayed with spectrophotometry. The contents of lactate dehydrogenase (LDH) and creatine kinase (CK) in blood serum were detected with automatic biochemistry analyzer.</p><p><b>RESULT</b>Compared with the control group, the myocardial indexes, the contents of I , III collagen quantification, angiotensin II in blood serum and malondialdehyde in left ventricle were markedly increased and the content of nitric oxide in blood serum was decreased, the contents of lactate dehydrogenase and creatine kinase in blood serum were markedly increased in Iso model group (P<0.05 or P<0.01). Compared with the model group, the myocardial indexes were decreased, the contents of I , III collagen quantification, angiotensin II in blood serum were reduced in PC 200 and 400 mg x kg(-1) x d(-1) groups (P<0.05 or P<0.01). The content of nitric oxide in blood serum was increased, the content of malondialdehyde in left ventricle was markedly decreased, the contents of lactate dehydrogenase and creatine kinase in blood serum were markedly decreased in PC three groups (P<0.05 or P<0.01).</p><p><b>CONCLUSION</b>PC could inhibit collagen synthesis by decreasing angiotensin II level and increasing the content of nitric oxide and antioxidation, and thereby inhibiting myocardial fibrosis and protect myocardium in rats.</p>

A Comparative Study on Mechanical and Biochemical Properties of Bovine Pericardium After Single or Double Crosslinking Treatment

BACKGROUND AND OBJECTIVES: Glutaraldehyde (GA) has been used as a representative method of tissue preservation in cardiovascular surgery. However, GA has showed limited durability including calcification, mechanical failure and toxicity. To overcome those unsolved problems, we analyzed the crosslinking differences of primary amines, GA and genipin in their mechanical and biochemical properties with a single or double crosslinking agent for clinical application. MATERIALS AND METHODS: Samples were divided into 3 groups; control, single crosslinking fixation and double crosslinking fixation after decellurarization using bovine pericardium. For analysis of the biochemical and mechanical properties of each crosslinking method, tensile strength, percentage strain, thermal stability, resistance to pronase, nynhydrin and cytotoxicity test were studied. RESULTS: Combined hexamethylene diamine and suberic acid in the carbodiimide hydrochloride/N-hydroxysucinimide solution (EDC/NHS) after decellurarization, tensile strength and strain percentage were not statistically significant compared to the single crosslinking treated groups (p>0.05). Tissue crosslinking stability was weak in single treatment of diphenylphosphoryl azide, suberic acid, low concentration of EDC, hexamethylene diamine and procyanidin groups, but thermal stability and resistance to the pronase and ninhydrin were markedly increased in concentrated EDC/NHS or after combined double treatment with low concentration of GA or genipin (p<0.001). CONCLUSION: Single or double crosslinking with low concentration of carbodiimide, diphenylphosphonyl azide, procyanidin, suberic acid and hexane diamine were not as effective in mechanical, biochemical, cytotoxic and crosslinking properties compared to GA or genipin fixation, but their mechanical and chemical properties were much improved when combined with low concentrations of GA or genipin in the double crosslinking process.

Adsorption dynamics study on interactions of pigments and human whole saliva / 华西口腔医学杂志

<p><b>OBJECTIVE</b>In situ, real timely and dynamically monitoring the processes of theaflavin (TF), curcumin (Cur) and cyanidin (Cy) binding to human whole saliva (WS) surface has been investigated by surface plasmon resonance (SPR) technique at the molecular level.</p><p><b>METHODS</b>The affinity between pigments and WS, association rate constant (k(a)), dissociation rate constant (k(d)), association equilibrium constant (K(A)) and dissociation equilibrium constant (K(D)) of pigments binding on WS surface had been determined by SPR and the Langmuir model as well as the Freundlich model. The data were analyzed by one-way ANOVA and SNK-q test.</p><p><b>RESULTS</b>There were significant differences among TF, Cur and Cy in k(a), k(d), K(A) and K(D) (P<0.05). Our results showed that the adsorption isotherm of pigments on WS surface could be better described by the Freundlich model than the Langmuir model. The pigments adsorption on WS surface was dominant by specific interactions, such as hydrogen bonding. The affinity of pigments to WS were TF> Cur>Cy (P<0.05), as evidenced by the rate constants and equilibrium constants.</p><p><b>CONCLUSION</b>Compared with Cur and Cy, TF shows much higher adsorption capacity on WS surface, suggesting the importance of the hydroxyl group in pigment/protein interactions.</p>