Pharmaceutical Biology Journal Impact Factor & Information

Publisher: Informa Healthcare

Journal description

Current impact factor: 1.34

Impact Factor Rankings

2015 Impact Factor Available summer 2015
2013 / 2014 Impact Factor 1.337
2012 Impact Factor 1.206
2011 Impact Factor 0.878
2010 Impact Factor 0.638
2009 Impact Factor 0.672
2008 Impact Factor 0.488
2007 Impact Factor 0.364
2006 Impact Factor 0.397
2005 Impact Factor 0.394
2004 Impact Factor 0.441
2003 Impact Factor 0.413
2002 Impact Factor 0.262
2001 Impact Factor 0.312
2000 Impact Factor 0.132
1999 Impact Factor 0.164

Impact factor over time

Impact factor
Year

Additional details

5-year impact 1.06
Cited half-life 5.80
Immediacy index 0.21
Eigenfactor 0.00
Article influence 0.20
Other titles Pharmaceutical biology (Online)
ISSN 1744-5116
OCLC 42441900
Material type Document, Periodical, Internet resource
Document type Internet Resource, Computer File, Journal / Magazine / Newspaper

Publisher details

Informa Healthcare

  • Pre-print
    • Author can archive a pre-print version
  • Post-print
    • Author cannot archive a post-print version
  • Restrictions
    • 12 months embargo
  • Conditions
    • On author's personal website or institution website
    • Publisher copyright and source must be acknowledged
    • On a non-profit server
    • Must link to publisher version
    • Publisher's version/PDF cannot be used
    • NIH funded authors may post articles to PubMed Central for release 12 months after publication
    • Wellcome Trust authors may deposit in Europe PMC after 6 months
  • Classification
    ​ yellow

Publications in this journal

  • [Show abstract] [Hide abstract]
    ABSTRACT: Abstract CONTEXT: During diabetes mellitus, non-enzymatic reaction between amino groups of protein and carbonyl of reducing sugars (Millard reaction) is responsible for the major diabetic complications. Various efforts have been made to influence the process of protein glycation. OBJECTIVES: This review article provides an extensive survey of various studies published in scientific literature to understand the process of protein glycation and its measurement. Moreover, evaluation and identification of potential inhibitors (antiglycation agents) of protein glycation from natural and synthetic sources and their mechanism of action in vitro and in vivo are also addressed. METHOD: In this review article, the mechanism involved in the formation of advanced glycation end products (AGEs) is discussed, while in second and third parts, promising antiglycation agents of natural and synthetic sources have been reviewed, respectively. Finally, in vivo studies have been addressed. This review is mainly compiled from important databases such as Science, Direct, Chemical Abstracts, SciFinder, and PubMed. RESULTS: During the last two decades, various attempts have been made to inhibit the process of protein glycation. New potent inhibitors of protein glycation belonging to different classes such as flavonoids, alkaloids, terpenes, benzenediol Schiff bases, substituted indol, and thio compounds have been identified. CONCLUSION: Antiglycation therapy will be an effective strategy in future to prevent the formation of AGEs for the management of late diabetic complications Current review article highlighted various compounds of natural and synthetic origins identified previously to inhibit the protein glycation and formation of AGEs in vitro and in vivo. KEYWORDS: Advanced glycation end products; antiglycation activity; hyperglycemia; protein glycation; reducing sugars
    Pharmaceutical Biology 08/2015;
  • Mahmoud Hussein Hassan Ali, Basim Anwar Shehata Messiha, Hekma Abdel-Tawab Abdel-Latif
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    ABSTRACT: Context: Nonalcoholic fatty liver disease (NAFLD) is the most common chronic liver disease. Resveratrol (RSV) and N-acetylcysteine (NAC) are safe representatives of natural and synthetic antioxidants, respectively. Objective: The objective of this study was to evaluate protective effects of RSV and NAC, compared with ursodeoxycholic acid (UDCA), on experimental NAFLD. Materials and methods: NAFLD was induced by feeding rats a methionine choline-deficient diet (MCDD) for four cycles, each of 4 d of MCDD feeding and 3 d of fasting. Animals were divided into normal control, steatosis control, and five treatment groups, receiving UDCA (25 mg/kg/d), RSV (10 mg/kg/d), NAC (20 mg/kg/d), UDCA + RSV, and UDCA + NAC orally for 28 d. Liver integrity markers (liver index and serum transaminases), serum tumor necrosis factor-α (TNF-α), glucose, albumin, renal functions (urea, creatinine), lipid profile (total cholesterol; TC, triglycerides, high density lipoproteins, low density lipoproteins; LDL-C, very low density lipoproteins, leptin), and oxidative stress markers (hepatic malondialdehyde; MDA, glutathione; GSH, glutathione-S-transferase; GST) were measured using automatic analyzer, colorimetric kits, and ELISA kits, supported by a liver histopathological study. Results: RSV and NAC administration significantly improved liver index (RSV only), alanine transaminase (52, 52%), TNF-α (70, 70%), glucose (69, 80%), albumin (122, 114%), MDA (55, 63%), GSH (160, 152%), GST (84, 84%), TC (86, 86%), LDL-C (83, 81%), and leptin (59, 70%) levels compared with steatosis control values. A combination of RSV or NAC with UDCA seems to ameliorate their effects. Discussion and conclusion: RSV and NAC are effective on NAFLD through antioxidant, anti-inflammatory, and lipid-lowering potentials, where as RSV seems better than UDCA or NAC.
    Pharmaceutical Biology 07/2015; DOI:10.3109/13880209.2015.1060247
  • Guo-Hua Zhu, Hai-Ping Dai, Qun Shen, Ou Ji, Qi Zhang, Yun-Liang Zhai
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    ABSTRACT: Context: Curcumin is a polyphenolic compound extracted from rhizomes of the tropical plant Curcuma longa L. (Zingiberaceae) and it has antitumor, antioxidative, and anti-inflammatory effects. However, its effects on leukemia cell proliferation and invasion are not clear. Objective: This study investigates the effects of curcumin on acute monocytic leukemia SHI-1 cells at the molecular level. Materials and methods: The effects of SHI-1 cells treated with 6.25–25 μM curcumin for 12–48 h were measured by MTT assay, flow cytometry, and Matrigel transwell assay; the underlying molecular mechanisms were assessed by quantitative PCR, Western blotting, and gelatin zymography. Results: Treatment of SHI-1 cells with curcumin inhibited cell proliferation in a dose- and time-dependent manner, and the IC50 values at 12, 24, and 48 h were 32.40, 14.13, and 9.67 μM. Curcumin inhibited SHI-1 cell proliferation by arresting the cells in the S-phase, increasing the number of Annexin V-FITC+/PI− cells and promoting the loss of △Ψm. The results of PCR and Western blotting showed that curcumin increased the FasL mRNA level; inhibited Bcl-2, NF-κB, and ERK expression; and activated P38 MAPK, JNK, and caspase-3. Additionally, curcumin partially suppressed SHI-1 cell invasion and attenuated the mRNA transcription and secretion of MMP-2 and MMP-9. Discussion and conclusion: This study demonstrates that curcumin not only induces SHI-1 cell apoptosis, possibly via both intrinsic and extrinsic pathways triggered by JNK, P38 MAPK and ERK signaling, but also partially suppresses SHI-1 cell invasion, likely by reducing the levels of transcription and secretion of MMP-2 and MMP-9.
    Pharmaceutical Biology 07/2015; DOI:10.3109/13880209.2015.1060508
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    ABSTRACT: Dichapetalum filicaule Breteler (Dichapetalaceae) is a rare species occurring only in Côte d'Ivoire and Ghana. Although research on several species of the genus has produced interesting bioactive compounds, particularly the Dichapetalins, a novel class of triterpenoids with antineoplastic properties, there is virtually no information on the ethnobotanical uses and chemical constituents of D. filicaule. The phytochemical and anthelminthic activities of the constituents of D. filicaule were investigated. Chemical constituents of the petroleum ether, chloroform-acetone, and methanol root extracts of D. filicaule were isolated by column chromatography and characterized by their physico-chemical properties, 1-D and 2-D NMR spectroscopy and mass spectrometry. In vitro anthelminthic activity of the extracts and compounds against the human hookworm, Necator americanus, Stiles 1902 (Nematoda: Ancylostomatidae) was determined within a concentration range of 2500-250 μg/ml using the Egg Hatch Inhibition (EHI) Assay. The hookworm species were identified using a published polymerase chain reaction (PCR) method. A new dichapetalin, dichapetalin X (1), together with the known dichapetalin A (2), pomolic acid (3), glycerol monostearate (4), D:A-friedooleanan-3β-ol (5), and D:A-friedooleanan-3-one (6) were isolated. Compounds 1, 2, and 4 exhibited EHI with IC50 values of 523.2, 162.4, and 306.0 μg/ml, respectively, against the hookworm. The positive control albendazole gave an IC50 value of 93.27 μg/ml. This is the first report of the phytochemical investigation of D. filicaule. The study has yielded a new dichapetalin and also demonstrated the potential anthelminthic properties of the constituents.
    Pharmaceutical Biology 06/2015; DOI:10.3109/13880209.2015.1059861
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    ABSTRACT: Natural products are good sources of natural dietary antioxidants that are believed to protect the body against hepatotoxic effect induced by oxidative stress. Hedyotis diffusa Willd (Rubiaceae) (HDW) is a traditional Chinese medicinal herb that has been shown to possess a variety of antioxidant properties. The present study examines and explains the cell protective property of HDW water extract (WEHDW). 2,2-Diphenyl-1-(2,4,6-trinitrophenyl) hydrazyl (DPPH) assay was used to measure the free radical scavenging property of WEHDW (0.001-10 mg/mL). The protective effect of WEHDW (0.3-10 mg/mL 2 h pretreatment) against hydrogen peroxide (H2O2, 200 μM for 6 h) induced cytotoxicity in human hepatic cells, LO2, was evaluated using cell viability assay and nuclear staining. The molecular pathway of WEHDW's effect was investigated by using Western blot assay. WEHDW had a 50% scavenging concentration (SC50) at 0.153 mg/mL in the DPPH assay. Exposure of LO2 cells to H2O2 resulted in apoptosis which could be markedly attenuated by pre-treating WEHDW in a concentration-dependent manner (0.5, 1, 3, 5, or 10 mg/mL) (all with p < 0.001, versus control). Moreover, Hoechst (nuclear) staining showed that 1 mg/mL WEHDW could protect LO2 cells by attenuating apoptotic cell death mediated by H2O2. It was found that WEHDW reversed H2O2-induced activation of MEK/ERK pathway and H2O2-induced inhibition of P13-K/AKT/GSK3β pathway in LO2 cells. WEHDW may help to improve the antioxidant defense system, resulting in prevention of oxidative stress-related fatty liver diseases.
    Pharmaceutical Biology 06/2015; DOI:10.3109/13880209.2015.1056310
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    ABSTRACT: Despite phytochemical studies of Agrimonia pilosa Ledeb. (Rosaceae), the antidiabetic effects of this plant are unknown. This study characterizes the isolated compounds from the aerial parts of A. pilosa and evaluates their PTP1B and α-glucosidase inhibitory properties. Ethanol extract of A. pilosa was found to inhibit 64% PTP1B activity at 30 μg/mL. The ethanol extract was partitioned with methylene chloride, ethyl acetate, n-butanol, and water fractions. Among these, the ethyl acetate fraction displayed the most potent PTP1B activity. The ethyl acetate extract was separated by chromatographic methods to obtain flavonoids and triterpenoids (1-11); which were evaluated for their inhibitory effects on PTP1B activity with p-nitrophenyl phosphate (p-NPP) as a substrate, and also α-glucosidase enzyme. Compounds 1-11 were identified as apigenin-7-O-β-d-glucuronide-6″-methyl ester, triliroside, quercetin-7-O-β-d-glycoside, quercetin-3-O-β-d-glycoside, kaempferol, kaempferol-3-O-α-l-rhamnoside, β-sitosterol, ursolic acid, tormentic acid, methyl 2-hydroxyl tricosanoate, and palmitic acid. Compounds 8, 9, and 11 displayed inhibitory effects on PTP1B activity with IC50 values of 3.47 ± 0.02, 0.50 ± 0.06, and 0.10 ± 0.03 μM, respectively. Compounds 3, 4, 6, and 9 exhibited inhibition of the α-glucosidase activity with IC50 values of 11.2 ± 0.2, 29.6 ± 0.9, 28.5 ± 0.1, and 23.8 ± 0.4 μM, respectively. As major ingredients of A. pilosa, compounds 1, 6, 8, and 9 showed the greatest inhibitory potency on PTP1B activity. Compounds 3, 6, 8, and 9 also showed potent inhibitory effects on α-glucosidase enzyme. This result suggested the potential of these compounds for developing antidiabetic agents.
    Pharmaceutical Biology 06/2015; DOI:10.3109/13880209.2015.1048372
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    ABSTRACT: Pereskia aculeata Miller (Cactaceae) is a cactus distributed from south to northeast of Brazil, where its leaves are commonly used as a vegetable, in skin wound healing, and to treat inflammation. The objective of this study was to perform the chemical characterization and to evaluate the antinociceptive activity of the hydromethanolic fraction obtained from the methanol extract of P. aculeata leaves. Chemical characterization was performed by UPLC-MS analysis. The antinociceptive activity was evaluated by the acetic acid-induced writhing, formalin, and tail-flick tests in mice, administering the single oral doses of 100, 200, and 300 mg/kg 1 h before each test. Tryptamine, abrine, mescaline, hordenine, petunidin, di-tert-butylphenol isomers, and quercetin were identified. The antinociceptive activity was inversely proportional to the administered doses in the acetic acid test, as the dose of 100 mg/kg reduced by 78% the number of writhings, while the doses of 200 and 300 mg/kg reduced by 64% and 41%, respectively. In the formalin test, the dose of 300 mg/kg inhibited by 50% and 86% the licking paw time in the first and second phases, respectively, while the doses of 200 mg/kg (45% and 62%, respectively) and 100 mg/kg (15% and 48%, respectively) were less effective. The sample did not respond to the tail-flick test. Those results suggested a peripheral and central antinociception devoid of an opioid effect. Pereskia aculeata not only is a plant food with high nutritional value but also presents analgesic potential. It is the first time that this bioactivity is reported for this species.
    Pharmaceutical Biology 06/2015; DOI:10.3109/13880209.2015.1008144
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    ABSTRACT: Viola tianshanica Maxim. (Violaceae) is a perennial herb distributed in Central Asia, especially in the Xinjiang Uygur Autonomous Region (XUAR) of China. Preliminary study showed that the ethanol extract of the herb exhibited the anti-complement activity against the classical pathway, but the active components responsible for this capacity remain unknown and are yet to be studied. The objective of this study was the isolation and identification of the anti-complement constituents of V. tianshanica. The ethyl acetate and n-butanol fractions from the ethanol extract of V. tianshanica were purified. The structures of the isolates were identified by spectroscopic methods, and comparing their spectral data with those reported in the literature. All the isolates (0.02-2.50 mg/mL) were evaluated for their anti-complement activity against the classical and alternative pathways. Twenty-one phenolic compounds including 15 flavonol O-glycosides (1-15), one flavone 6,8-di-C-glycoside (16), one flavone aglycone (17), and four phenolic acid derivatives (18-21) were isolated and identified. Bioassay showed that 11 compounds inhibited the classical pathway and the alternative pathway with CH50 and AP50 values of 0.113-1.210 mM and 0.120-1.579 mM, respectively. Preliminary mechanistic study using complement-depleted sera demonstrated that 1 acted on C1q, C2, C4, and C9 components, 16 on C1q, C4, and C5, and 21 on C1q, C3, C4, and C9. All isolated compounds except 1 and 10 were reported for the first time from V. tianshanica. Compound 16 is the first flavone C-glycoside isolated from the herb. Flavonol O-glycosides and phenolic acids contributed the anti-complement activity of the herb.
    Pharmaceutical Biology 06/2015; DOI:10.3109/13880209.2015.1055635
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    ABSTRACT: Tarragon (Artemisia dracunculus L., Asteraceae) is an ancient herb, which is widely used as a medicine, flavoring, or fragrance. To determine the antinociceptive and anti-inflammatory effects of aerial parts of tarragon, we investigated the effects of ethanolic extract of the plant in adult male Balb/c mice. Antinociceptive activity was determined using formalin, hot-plate, and writhing tests. The effect of the ethanolic extract on acute inflammation was evaluated by xylene-induced ear edema in mice. The ethanolic extract was administered at doses of 5, 10, 50, and 100 mg/kg, i.p. The control group received saline as vehicle of ethanolic extract. Our results showed that the ethanolic extract (50 and 100 mg/kg) decreased both phases of pain in the formalin test (ED50 = 109.66 and 87.13 mg/kg, respectively). In the hot-plate test, the extract (50 and 100 mg/kg) increased pain threshold during 60 min (ED50 = 81.03 mg/kg). The extract (50 and 100 mg/kg) exhibited antinociceptive activity against acetic acid-induced writhing (ED50 = 66.99 mg/kg). The extract (50 and 100 mg/kg) showed significant activity in the xylene ear edema test (ED50 = 78.20 mg/kg). Pretreatment of the animals with naloxone decreased the analgesia induced by the extract in hot-plate and formalin tests; therefore, opioid receptors may be involved, at least partly, in the analgesic effect of tarragon extract. The results suggested that tarragon have significant analgesic and anti-inflammatory effects in mice, and, therefore, further studies are required to evaluate these effects and additional potential of the plant.
    Pharmaceutical Biology 06/2015; DOI:10.3109/13880209.2015.1056312
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    ABSTRACT: Sweetgum oil (SO) obtained from the Liquidambar orientalis Mill (Hamamelidaceae) tree has been used in Turkish folk medicine for centuries as an antiulcerigenic. Some studies have reported the antibacterial and antioxidant activities of SO; however, its effect on hepatic and oxidative stress complications is still unexplored. This study investigates the hepatoprotective effect and the antioxidant role of SO against carbon tetrachloride (CCl4) toxicity. The experiment included control, CCl4, SO, and CCl4 + SO treatment groups. Control and SO group rats were fed a diet without CCl4. CCl4 and CCl4 + SO treatment groups received 0.5 mL/kg CCl4 diluted in olive oil (1:1 dilution) intraperitonally injection twice per week. The CCl4 + SO group also received 1000 mg/kg SO-supplemented feed for 50 d. Blood and tissue samples were used for the determination of hepatic damage serum biomarkers (HDSBs) levels, antioxidant defense system constituents (ADSCs), and malondialdehyde (MDA) contents. In addition, the liver was evaluated for histopathological changes. According to the results, the HDSBs levels of the CCl4 group were significantly (p < 0.05) increased compared with the control, whereas the HDSB levels of the CCl4 + SO group resulted in marked decreases (p < 0.05) compared with the CCl4 group. In addition, the results showed that SO-supplemented diet restored the CCl4-induced MDA and ADS towards to control. Hepatoprotection of SO is further substantiated by the almost normal histologic findings in the CCl4 + SO group against degenerative changes in the CCl4 group. It was concluded that SO has a hepatoprotective effect and antioxidant capacity against CCl4 toxicity.
    Pharmaceutical Biology 06/2015; DOI:10.3109/13880209.2015.1045086
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    ABSTRACT: Thyme has been used in traditional medicine for medicinal purposes since ancient times. The objective of this study was to investigate the effects of thymol and carvacrol as two major constituents of thyme on dendritic cells (DCs) maturation and T cell activation. Splenic DCs were treated with non-cytotoxic concentrations of the components and then analyzed for MHC II, CD86, and CD40 expression by flow cytometry. The effects of compounds on mitogenic, as well as allogenic T cell responses in mixed lymphocyte culture (MLR) and the release of cytokines were investigated. At 0.1 µg/ml, reduced mean fluorescent intensity (MFI) of CD86 for thymol (80.3 ± 0.2% of untreated control) and CD40 for carvacrol (79.5 ± 0.14%) was observed (p < 0.001). Decreased mitogenic T cell proliferation by thymol [proliferation index (PI) from 0.93 ± 0.11 at 1 µg/ml to 0.42 ± 0.16 at 100 µg/ml (p < 0.01)] and carvacrol [PI from 1.08 ± 0.3 at 1 µg/ml to 0.28 ± 0.1 at 100 µg/ml (p < 0.001)] was seen. Ten micrograms/ml thymol (PI, 0.85 ± 0.04) and carvacrol (PI, 0.89 ± 0.03) inhibited allogenic T cell response (p < 0.05). Decreased IFN-γ level in MLR supernatant from 1441 ± 27.7 pg/ml in untreated cells to 944 ± 32.1 at 10 µg/ml of thymol and of carvacrol (886 ± 31.7 pg/ml) (p < 0.01) was found. IL-4 levels were decreased in the presence of both compounds (p < 0.01). These data showed the suppressive effects of thymol and carvacrol on DCs maturation and function, as well as T cell responses.
    Pharmaceutical Biology 06/2015; DOI:10.3109/13880209.2015.1055579
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    ABSTRACT: Shorea robusta Gaertn.f. (Dipterocarpaceae) resin is used for treating infected wounds and burns by tribals in India. The objective of this study was to investigate wound-healing activity of S. robusta resin extracts and essential oil in rats. Methanol extract (SRME), petroleum ether, benzene insoluble fraction of methanol extract (SRPEBIME), and essential oil (SREO) of S. robusta resin were incorporated in soft yellow paraffin (10% w/w) and applied once daily on incision and excision wounds of Wistar rats. Framycetin ointment (1.0% w/w) was applied to the standard group. Tensile strength (on the 10th day), wound contraction, and scar area (on the 14th day) were recorded. On the 15th day, granulation tissues of excision wounds were analyzed for total protein, hydroxyproline, and hexosamine contents and activities of lipid peroxidation and super oxide dismutase (SOD). Histopathology of the wounds was also studied. SRPEBIME and SREO healed incision and excision wounds faster than plain ointment base and framycetin. Tensile strength of SRPEBIME-treated incision wounds was 53% higher than that of control animals. In excision wounds, wound contraction and scar areas were found to be 99% and 7.7 mm(2) (SRPEBIME) and 71.7% and 21 mm(2) (control). Protein and hydroxyproline contents were higher in SRPEBIME (20.8 and 3.5% w/w) and SREO (17.4 and 2.8% w/w) groups as against 9.95 and 1.48% w/w in control groups. Histopathology revealed complete epithelization and new blood vessel formation in SRPEBIME groups. SRPEBIME and SREO have significant wound-healing activities on incision and excision wounds.
    Pharmaceutical Biology 06/2015; DOI:10.3109/13880209.2015.1052886
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    ABSTRACT: Carum copticum seeds have been prescribed in the traditional system of medicine for the treatment of immune disorders, such as asthma and rheumatism. The objective of this study was to determine immunomodulatory effects of the alcoholic extract and isolated compounds in Swiss albino mice. Seeds of C. copticum were extracted with 95% v/v alcohol. The immunomodulatory activity of the crude extract was evaluated at the doses of 100, 300, and 500 mg/kg body weight of mice, administered in mice once daily (orally) for 25 days. Volatile oil of C. copticum was isolated by steam distillation and was characterized by GLC and HPLC. Bio-assay-guided fractionation and isolation were carried out and the isolated compounds were characterized and subjected to immunomodulatory activity studies. The n-hexane fraction yielded p-cymene, carvacrol, and α-pinene. The LD50 value of the crude extract was found to be 4500 mg/kg and the values reported for p-cymene, carvacrol, and α-pinene in the literature were 4750, 810, and 3700 mg/kg, respectively. The oral administration of crude extract, n-hexane fraction (HEF), and isolated oils at the dose of 500, 150, and 50 mg/kg body weight, respectively, showed a significant increase in the HA titers, DTH-response, and phagocytosis. The stimulatory effect observed, on humoral and cellular immunity, was compared with the standard (levamisole treated) and control groups. The results obtained in the study endorse the traditional use of the seeds of C. copticum and the isolated constituents act as immunostimulants.
    Pharmaceutical Biology 06/2015; DOI:10.3109/13880209.2015.1050116
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    ABSTRACT: Despite the beneficial effects of barberry (Berberis integerrima Berberidaceae) on decreasing systemic hypertension, its influence has not been investigated on pulmonary hypertension. The objective of this study is to examine the effect of barberry fruit, on monocrotaline-induced pulmonary hypertension. Nine groups were arranged as follows: the control group, the monocrotaline (M) group, the barberry groups with doses of 50, 100, and 200 (mg/kg), the M plus barberry groups, and the M plus sildenafil group. Two weeks after a single injection of monocrotaline (60 mg/kg, s.c.), barberry water extracts or sildenafil (30 mg/kg/d) were gavaged daily for 2 weeks. At the end of the 4th week, hemodynamic, biochemical, and histopathological parameters were assessed. In comparison with the M group, barberry (200 mg/kg) or sildenafil significantly reduced the right ventricular systolic pressure (RVSP) (22.95 ± 1.78 mm Hg and 30.71 ± 1.64 mm Hg, versus 41.28 ± 1.5 mm Hg), right ventricular hypertrophy (RVH) (0.39 ± 0.03 and 0.42 ± 0.02, versus 0.57 ± 0.02), and the medial wall thickness (MWT) (4.56 ± 0.15 µm and 5.97 ± 0.19 µm, versus 7.02 ± 0.43 µm). Barberry or sildenafil had no significant effect on the plasma level of endothelin-1, glutathione peroxidase, and the malondialdehide of lung. 200 mg/kg of barberry has an improving effect on the monocrotaline-induced pulmonary hypertension. This effect was stronger than that of the sildenafil's and may have been mediated through mechanisms other than the modulation of the endothelin-1 or redox system.
    Pharmaceutical Biology 05/2015; DOI:10.3109/13880209.2015.1050676
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    ABSTRACT: Bisbibenzyl compounds have gained our interests for their potential antitumor activity in malignant cell-types. The objective of this study is to investigate the effect of bisbibenzyl compounds riccardin C (RC), marchantin M (MM), and riccardin D (RD) on androgen receptor (AR) in prostate cancer (PCa) cells. After exposure to 10 μM of the compounds for 24 h, cell cycle and cell survival analyses were performed using FACS and MTT assay to confirm the effect of these bisbibenzyls on PCa LNCaP cells. Changes in the AR expression and function, as the result of exposure to the compounds, were investigated using real-time PCR, ELISA, transient transfection, western blotting (WB), immunoprecipitation, and immunofluorescence staining (IF). Chemical-induced autophagy was examined by WB, IF, and RNAi. RC, MM, and RD reduced the viability of LNCaP cells accompanied with arrested cell cycle in the G0/G1 phase and induction of apoptosis. Further investigation revealed that these compounds significantly inhibited AR expression at mRNA and protein levels, leading to the suppression of AR transcriptional activity. Moreover, inhibition of proteasome activity by bisbibenzyls, which in turn caused the induction of autophagy, as noted by induction of LC3B expression, conversion, and accumulation of punctate dots in treated cells. Co-localization of AR/LC3B and AR/Ub suggested that autophagy contributed to the degradation of polyubiquitinated-AR when proteasome activity was suppressed by the bisbibenzyls. Suppression of proteasome activity and induction of autophagy were involved in bisbibenzyl-mediated modulation of AR activities and apoptosis, suggesting their potential in treating PCa.
    Pharmaceutical Biology 05/2015; DOI:10.3109/13880209.2015.1049278