Effect of crocin on the morphine‐induced antinociception in the formalin test in rats

In this study, the effects of intraperitoneal (i.p.) injection of crocin in the absence and presence of subcutaneous (s.c.) injections of morphine and naloxone were investigated on the formalin test in rats. The formalin test was induced by intra‐plantar (i.pl.) injection of formalin (50 μL, 1%), and the time spent licking and biting of the injected paw was measured for 1 h. Formalin induced a marked biphasic (first phase: 0–5 min and second phase: 15–45 min) pain response. Morphine (1 mg/kg, s.c.) significantly (p < 0.05) suppressed both phases of pain. Naloxone (2 mg/kg, s.c.) alone did not change the intensity of pain, but pretreatment with naloxone (2 mg/kg) significantly (p < 0.05) prevented morphine (1 mg/kg)‐induced antinociception. Crocin at doses of 50, 100 and 200 mg/kg significantly (p < 0.05) attenuated pain. Crocin (100 mg/kg, i.p.) significantly (p < 0.05) increased the morphine (1 mg/kg, s.c.)‐induced antinociception. Naloxone (2 mg/kg) did not reverse the suppressive effect of crocin (100 mg/kg) on pain. Crocin at a dose of 400 mg/kg significantly (p < 0.05) suppressed locomotor activities. These findings indicate that morphine through a naloxone‐sensitive mechanism produced analgesia. Crocin produced a dose‐dependent antinociceptive effect. In addition, crocin increased morphine‐induced antinociception, but naloxone did not change the antinociceptive effect of crocin. Copyright © 2009 John Wiley & Sons, Ltd.     

Antidiarrhoeal activity of Hypoxis hemerocallidea Fisch. & C. A. Mey. (Hypoxidaceae) Corm (‘African potato’) aqueous extract in rodents

This study investigated the antidiarrhoeal activity of Hypoxis hemerocallidea corm aqueous extract (APE) on experimentally‐induced diarrhoea, gastrointestinal motility, intestinal transit and enteropooling in rodents. H. hemerocallidea corm aqueous extract (APE, 50–400 mg/kg, p.o.) produced dose‐dependent and significant (p < 0.05–0.01) protection of rats and mice against castor oil‐induced diarrhoea, inhibited intestinal transit and delayed gastric emptying. Like atropine (1 mg/kg, p.o.), APE (50–400 mg/kg, p.o.) produced dose‐dependent and significant (p < 0.05–0.01) antimotility effect, and caused dose‐related inhibition of castor oil‐induced enteropooling in the animals. Like loperamide (10 mg/kg, p.o.), APE (50–400 mg/kg, p.o.) dose‐dependently and significantly (p < 0.05–0.01) delayed the onset of castor oil‐induced diarrhoea, decreased the frequency of defaecation and reduced the severity of diarrhoea in the rodents. Compared with control animals, APE (50–400 mg/kg, p.o.) dose‐dependently and significantly (p < 0.05–0.01) decreased the volume of castor oil‐induced intestinal fluid secretion, and reduced the number, weight and wetness of faecal droppings. APE (50–400 mg/mL) also produced concentration‐related and significant (p < 0.05–0.01) inhibitions of the spontaneous, pendular contractions of the rabbit isolated duodenum, and attenuated acetylcholine (ACh, 0.1–5.0 µg/mL)‐induced contractions of the guinea‐pig isolated ileum. Although the precise mechanism of the antidiarrhoeal activity of APE could not be established, the results of this study indicate that APE possesses antidiarrhoeal activity. This finding supports the use of ‘African potato’ as a natural supplementary remedy for the treatment, management and/or control of diarrhoea in some rural communities of southern Africa. Copyright © 2009 John Wiley & Sons, Ltd.     

Protective effect of Morinda citrifolia fruits on β‐amyloid (25–35) induced cognitive dysfunction in mice: An experimental and biochemical study

The neuroprotective effect of an ethyl acetate extract of Morinda citrifolia (Rubiaceae) Linn. fruits (EMC, ethyl acetate extract of Morinda citrifolia) at doses of 200 and 400 mg/kg, p.o. was studied on β‐amyloid (25–35) peptide induced cognitive dysfunction in mice. In the step‐down inhibitory avoidance, EMC exhibited a significant increase in short‐term memory and long‐term memory (p < 0.05). A significant decrease (p < 0.01) in escape latency was noticed in the animals in the water maze. A significant increase (p < 0.01) in alteration of behavior was exhibited upon administration of EMC 200 and 400 mg/kg on the Y maze. Exploratory parameters such as line crossings, head dipping and rearing were increased significantly in EMC treated groups in a dose‐dependent manner (p < 0.05 and p < 0.01). A significant reduction (p < 0.05) in acetyl cholinesterase activity was noticed in the EMC 200 and 400 mg/kg treated groups. The level of monoamine oxidase‐A was decreased by the administration of EMC 200 and 400 mg/kg (p < 0.05 and p < 0.01, respectively). EMC at a dose of 400 mg/kg exhibited a significant increase (p < 0.01) in the levels of serotonin and dopamine. Antioxidant enzymes such as superoxide dismutase, glutathione reductase, glutathione peroxidase and ascorbic acid were decreased significantly in the b‐amyloid peptide injected group, whose levels were restored significantly (p < 0.01) by the administration of EMC (400 mg/kg). Copyright © 2009 John Wiley & Sons, Ltd.     

Paullinia cupana Mart. var. sorbilis,guarana, increases survival of Ehrlich ascites carcinoma (EAC) bearing mice by decreasing cyclin‐D1 expression and inducing a G0/G1 cell cycle arrest in EAC cells

The objective of this work is to report the antiproliferative effect of P. cupana treatment in Ehrlich Ascites Carcinoma (EAC)‐bearing animals. Female mice were treated with three doses of powdered P. cupana (100, 1000 and 2000 mg/kg) for 7 days, injected with 10⁵ EAC cells and treated up to day 21. In addition, a survival experiment was carried out with the same protocol. P. cupana decreased the ascites volume (p = 0.0120), cell number (p = 0.0004) and hemorrhage (p = 0.0054). This occurred through a G1‐phase arrest (p < 0.01) induced by a decreased gene expression of Cyclin D1 in EAC cells. Furthermore, P. cupana significantly increased the survival of EAC‐bearing animals (p = 0.0012). In conclusion, the P. cupana growth control effect in this model was correlated with a decreased expression of cyclin D1 and a G1 phase arrest. These results reinforce the cancer therapeutic potential of this Brazilian plant. Copyright © 2010 John Wiley & Sons, Ltd.     

Preliminary observations on the antifatigue effects of longan (Dimocarpus longan Lour.) seed polysaccharides

The antifatigue effects of the hot‐water extract of longan (Dimocarpus longan Lour.) seeds were studied in mice. Longan seed polysaccharides were administered at doses of 50, 100, 200 and 400 mg/kg and antifatigue activity was evaluated using a swimming test, along with the determination of serum urea nitrogen, hepatic glycogen and blood lactic acid content. The results show that longan seed polysaccharides, in doses ranging from 50 to 100 mg/kg, extended swimming time, increased hepatic glycogen (p < 0.01, n = 10), reduced blood urea nitrogen (p < 0.01, n = 10) and decreased blood lactic acid (p < 0.01, n = 10) in the mice. Therefore longan seed polysaccharides may have potential as an antifatigue agent. Copyright © 2010 John Wiley & Sons, Ltd.     

Effects of Piperine,Cinnamic Acid and Gallic Acid on Rosuvastatin Pharmacokinetics in Rats

The purpose of this study was to investigate the potential pharmacokinetic interactions with natural products (such as piperine (PIP), gallic acid (GA) and cinnamic acid (CA)) and rosuvastatin (RSV) (a specific breast cancer resistance protein, BCRP substrate) in rats. In Caco₂ cells, the polarized transport of RSV was effectively inhibited by PIP, CA and GA at concentration of 50 μM. After per oral (p.o.) coadministration of PIP, CA and GA (10 mg/kg) significantly increased intravenous exposure (AUC_last) of RSV (1 mg/kg) by 73.5%, 62.9% and 53.3% (p < 0.05), respectively than alone group (control). Compared with the control (alone) group, p.o. coadministration of PIP, CA and GA (10 mg/kg) significantly increased the oral exposure (AUC_last) of RSV (5 mg/kg) by 2.0‐fold, 1.83‐fold (p < 0.05) and 2.34 ‐fold (p < 0.05), respectively. Moreover, the cumulative biliary excretion of RSV (5 mg/kg, p.o.) was significantly decreased by 53.3, 33.4 and 39.2% at the end of 8 h after p.o. co‐administration of PIP, CA and GA (10 mg/kg), respectively. Taken together, these results indicate that the natural products such as PIP, CA and GA significantly inhibit RSV transport in to bile and increased the plasma exposure (AUC_last) of RSV. Copyright © 2012 John Wiley & Sons, Ltd.     

Hypoglycemic effect of a leaf extract of Pseuderanthemum palatiferum (Nees) Radlk. in normal and streptozotocin-induced diabetic rats

Ethnopharmacological relevance

Pseuderanthemum palatiferum (Nees) Radlk (Acanthaceae) was first found in Northern Vietnam and expanded throughout the country including the Mekong Delta region. The leaves of this plant are recommended in folk medicine of Vietnam and Thailand for promoting and treating various diseases including hypertension, diarrhea, arthritis, hemorrhoids, stomachache, tumors, colitis, bleeding, wounds, constipation, flu, colon cancer, nephritis, and diabetes.

Aim of the study

The hypoglycemic effect of an 80% ethanolic leaf extract from the leaves of Pseuderanthemum palatiferum (PPE) was investigated in normal and streptozotocin (STZ)-induced diabetic rats.

Materials and methods

The PPE was administered daily and orally to the rats at the doses of 250, 500, and 1000 mg/kg body weight (b.w.) for 14 days. The levels of fasting plasma glucose (FPG), serum insulin, and biochemical data such as blood urea nitrogen (BUN), triglycerides (TG), total cholesterol (TC), high-density lipoprotein (HDL), low-density lipoprotein (LDL), and alkaline phosphatase (ALP) were evaluated. The hypoglycemic effect of PPE was compared to that of the known anti-diabetic drug glibenclamide (0.25 mg/kg b.w.).

Results

FPG and serum insulin in normal rats were not significantly different from the control and test groups in all dosages. The treated diabetic rats which had received PPE and glibenclamide showed significantly (p < 0.05) decreased FPG and increased serum insulin levels at the end of the experiment. The hypoglycemic effect of PPE at the dose of 250 mg/kg b.w. was significantly (p < 0.05) more effective than that of glibenclamide. The serum insulin in PPE fed diabetic rats at the dose of 250 mg/kg b.w. was not different from those which had received glibenclamide, and this dose was significantly (p < 0.05) more effective than PPE at the doses of 500 and 1000 mg/kg b.w. while PPE increased HDL and decreased TC, TG, LDL, BUN and ALP in the diabetic rats.

Conclusions

PPE has a beneficial effect in hyperglycemic rats and may prevent the complication of diabetes.     

Effect of boldo (Peumus boldus Molina) infusion on lipoperoxidation induced by cisplatin in mice liver

Peumus boldus Molina (Monimiaceae), commonly referred to as ‘boldo’, is used in traditional Chilean medicine to treat hepatic and gastrointestinal diseases. Its leaves are rich in antioxidant compounds, principally alkaloids and flavonoids. This study evaluates the protective effect of a complete boldo leaf infusion on lipoperoxidation (MDA determination at 532 nm) induced by cisplatin in mice liver. To determine if the observed effect can be explained by the action of boldine or catechin, each compound was studied separately. The mice were divided into 8 groups (n = 6): (I) not treated; (II) treated with cisplatin 6 mg/Kg b.w.; (III) treated with boldo leaf infusion 5%; (IV) pretreated with boldo leaf infusion 5% and treated with cisplatin 6 mg/Kg b.w.; (V) treated with boldine 50 mg/Kg b.w.; (VI) pretreated with boldine 50 mg/Kg b.w. and treated with cisplatin 6 mg/kg.b.w.; (VII) treated with catechin; and (VIII) pretreated with catechin 50 mg/Kg b.w. and treated with cisplatin 6 mg/Kg b.w. As expected, the treatment with cisplatin significantly increased (p < 0.01) lipoperoxidation in comparison with the non‐treated group. Pretreatment with boldo leaf infusion significantly diminished (p < 0.05) the lipoperoxidation induced by cisplatin with respect to the animals not pretreated with the infusion. The pretreatments with boldine and catechin significantly diminished (p < 0.05) the lipoperoxidation induced by cisplatin with respect to the group treated only with cisplatin. The results suggest that the boldo infusion is acting as a protector with respect to the oxidative hepatic damage caused by cisplatin, and that this protective ability would be due to the presence in the infusion of the natural antioxidants boldine and principally catechin. These findings suggest the potential use of the infusion as a chemoprotector. Copyright © 2009 John Wiley & Sons, Ltd.     

Hyptis pectinata: Redox Protection and Orofacial Antinociception

Hyptis pectinata L. Poit, known as ‘sambacaitá’, is used in Brazil to treat inflammatory and painful disorders. In this study, the antioxidant and orofacial antinociceptive properties of the aqueous extract of H. pectinata leaves (AEPH) were assessed using in vitro and in vivo models. Thus, AEPH reduced the 2,2‐diphenyl‐1‐picrylhydrazyl radical up to 72.10% with an EC₅₀ of 14.56 µg/ml. It also inhibited 40.80% of the lipoperoxidation induced by 2′‐azobis (2‐amidinopropane) dihydrochloride in the thiobarbituric acid‐reactive substances assay. The orofacial antinociceptive activity was evaluated in mice pre‐treated with AEPH (100, 200 and 400 mg/kg, p.o.) and morphine (5 mg/kg, i.p.), which received afterwards formalin‐ (20 µl, 2% solution, s.c.), glutamate‐ (40 µl, 25 mM, s.c.) and capsaicin‐ (20 µl, 2.5 µg, s.c.) to induce orofacial nociception. AEPH at all doses reduced (p < 0.001) the nociceptive response in the first (43–62%) and second (47–80%) phases of the formalin test. Besides, the effect of AEPH (400 mg/kg) was not changed in the presence of naloxone (1.5 mg/kg, i.p.), an opioid antagonist. AEPH significantly inhibited mice face rubbing for capsaicin (23–69%, p < 0.05) and glutamate (48–77%, p < 0.001) at all doses. The findings suggested the AEPH has peripheral and central antinociceptive activities, which are not related to opioid receptors. Copyright © 2012 John Wiley & Sons, Ltd.     

The Effect of Butin on the Vitiligo Mouse Model Induced by Hydroquinone

Vernonia anthelmintica (L.) Willd has been traditionally used in the treatment of vitiligo in Uyghur medicine. This study used butin, the main component of V. anthelmintica, to study the influence on hydroquinone‐induced vitiligo in mice. The animals were randomly divided into six groups: control, model, 8‐methoxypsoralen (8‐MOP, 4.25 mg/kg), and butin (0.425, 4.25, and 42.5 mg/kg) groups. The number of melanin‐containing hair follicles, basal layer melanocytes, melanin‐containing epidermal cells, the expression of tyrosinase (TYR) and tyrosinase‐related protein‐1 (TRP‐1), the malondialdehyde (MDA), and cholinesterase (CHE) activity in serum were measured. Our results indicated that compared with the model group, the melanin‐containing hair follicles, the expression of TYR and TRP‐1 increased, the activity of CHE decreased after treatment with 8‐MOP and all doses of butin (p < 0.05, p < 0.01), the basal layer melanocytes and melanin‐containing epidermal cells increased significantly after treatment with butin 4.25 and 42.5 mg/kg (p < 0.05, p < 0.01), and the MDA activity decreased after using butin 4.25 and 42.5 mg/kg and 8‐MOP (p < 0.05, p < 0.01). Our results support the use of butin on vitiligo, and its possible mechanisms may be related to increase the TYR and TRP‐1 protein expression and decrease the activity of MDA and CHE in hydroquinone‐induced vitiligo model in mice. Copyright © 2017 John Wiley & Sons, Ltd.     

Neuropharmacological Studies on Ethanol Extracts of Valeriana officinalis L.: Behavioural and Anticonvulsant Properties

An ethanol total extract of the roots of Valeriana officinalis L. in doses equivalent to 0.5–800 mg valerian root/kg b.w.i.p. was tested in male mice for possible neuropharmacological efficacy and in this respect compared with diazepam and haloperidol. The extract did not modify spontaneous motility, nociception or body temperature, and did not produce palpebral ptosis. However, it was anticonvulsant against picrotoxin (but not pentetrazol and harman) with an ED₅₀ between 4.5 and 6 mg/kg and it prolonged thiopental anaesthesia. After fractionation of the crude extract, the antipicrotoxin activity was present mainly in the methylene chloride fraction (ED₅₀=0.25 mg/kg). Pure valerenic acid (12.5 mg/kg b.w.i.p.) also exerted an antipicrotoxin effect.     

Terminalia arjuna: an Ayurvedic Cardiotonic,Regulates Lipid Metabolism in Hyperlipaemic Rats

The lipid lowering action of the bark powder of Terminalia arjuna (T. arjuna ) has been studied in triton and cholesterol fed rats. Serum lipids were found to be lowered by T. arjuna (100 mg/kg, b.w.) in triton induced hyperlipaemia. Chronic feeding of this powder (100 mg/kg, b.w., p.o.) in animals simultaneously fed with cholesterol (25 mg/kg, b.w.) for 30 days, caused lowering in lipids and protein levels of β-lipoproteins followed by an increase in high density lipoprotein-cholesterol compared with the cholesterol fed groups. T. arjuna alters lipolytic activities in plasma, liver, heart and adipose tissues of hyperlipaemic rats. The lipid lowering action of this natural product is mediated through inhibition of hepatic cholesterol biosynthesis, increased faecal bile acid excretion and enhanced plasma lecithin:cholesterol acyltransferase activity and stimulation of receptor mediated catabolism of low density lipoprotein.     

Effect of berberine on the pharmacokinetics of substrates of CYP3A and P‐gp

The in vivo effects of berberine (BBR), the widely used bioactive herbal ingredient from many traditional Chinese medicinal herbs, on the pharmacokinetics of carbamazepine (CBZ, a substrate of CYP3A) and its metabolite carbamazepine 10,11‐epoxide (ECBZ), digoxin (DIG, a substrate of P‐gp) and cyclosporine A (CsA, a dual substrate of CYP3A and P‐gp) were evaluated in rats. After a 2‐week pretreatment with BBR, the pharmacokinetic parameters of i.g. administered CBZ and ECBZ were not significantly altered. The pharmacokinetics of i.v. administered DIG was not modified by single and 2‐week pretreatments with BBR, but a dose‐dependent increase in AUC and C_max was observed in the i.g. administered DIG parameters in rats. The AUCs of DIG with BBR (30 mg/kg, 100 mg/kg) were 133%, 170% (single) and 123%, 169% (2‐week) of control, respectively. The AUC and C_max of i.g. administered CsA with a 2‐week pretreatment with BBR increased by 62% and 43% (BBR 30 mg/kg, p < 0.05), 96% and 60% (BBR 100 mg/kg, p < 0.01), compared with the control. In conclusion, berberine produced a dose‐dependent increased bioavailability of digoxin and cyclosporine A by inhibition of intestinal P‐gp. No significant changes in CYP3A activity by berberine were observed. Copyright © 2009 John Wiley & Sons, Ltd.     

Adjuvant Therapy with Bioavailability‐Boosted Curcuminoids Suppresses Systemic Inflammation and Improves Quality of Life in Patients with Solid Tumors: A Randomized Double‐Blind Placebo‐Controlled Trial

Curcuminoids are bioactive polyphenolics with potent antiinflammatory properties. Although several lines of in vitro and preclinical evidence suggest potent anticancer effects of curcuminoids, clinical findings have not been conclusive. The present randomized double‐blind placebo‐controlled trial aimed to evaluate the efficacy of curcuminoids as adjuvant therapy in cancer patients. Eighty subjects with solid tumors who were under standard chemotherapy regimens were randomly assigned to a bioavailability‐boosted curcuminoids preparation (180 mg/day; n = 40) or matched placebo (n = 40) for a period of 8 weeks. Efficacy measures were changes in the health‐related quality of life (QoL) score (evaluated using the University of Washington index) and serum levels of a panel of mediators implicated in systemic inflammation including interleukins 6 (IL‐6) and 8 (IL‐8), TNF‐α, transforming growth factor‐β (TGFβ), high‐sensitivity C‐reactive protein (hs‐CRP), calcitonin gene‐related peptide (CGRP), substance P and monocyte chemotactic protein‐1 (MCP‐1). Curcuminoid supplementation was associated with a significantly greater improvement in QoL compared with placebo (p < 0.001). Consistently, the magnitude of reductions in TNF‐α (p < 0.001), TGFβ (p < 0.001), IL‐6 (p = 0.061), substance P (p = 0.005), hs‐CRP (p < 0.001), CGRP (p < 0.001) and MCP‐1 (p < 0.001) were all significantly greater in the curcuminoids versus placebo group. In contrast, the extent of reduction in serum IL‐8 was significantly greater with placebo versus curcuminoids (p = 0.012). Quality of life variations were associated with changes in serum TGFβ levels in both correlation and regression analyses. Adjuvant therapy with a bioavailable curcuminoid preparation can significantly improve QoL and suppress systemic inflammation in patients with solid tumors who are under treatment with standard chemotherapy protocols. Copyright © 2014 John Wiley & Sons, Ltd.     

Antinociceptive Effects of Eugenol Evaluated in a Monoiodoacetate‐induced Osteoarthritis Rat Model

The aim of the present study was to evaluate whether eugenol, the main constituent of clove oil, has the capacity to provide analgesia in the monoiodoacetate‐induced rat model of osteoarthritis. Animals (n = 6/group) received either eugenol (20 or 40 mg/kg) or a vehicle by gavage. Daily administrations were initiated 2 days post osteoarthritis induction and continued for the duration of the study (4 weeks). Gait analysis was performed using the CatWalk method and secondary mechanical allodynia was assessed with von Frey filaments. Selected spinal cord peptides (substance P, calcitonin gene‐related peptide and dynorphin) were quantified by mass spectrometry. Significant changes were identified in dynamic gait parameters (swing speed, swing phase duration and duty cycle) of the affected limb following 40 mg/kg eugenol treatment compared with the vehicle (p < 0.05). Von Frey results revealed significant differences between the 40 mg/kg treatment and the vehicle group during the first and the third week of the study (p < 0.02). Spinal pain‐related peptide analysis revealed a decreased content of substance P and CGRP accompanied by an increase of dynorphin in animals treated with 40 mg/kg eugenol. These results suggest a therapeutic potential of eugenol to alleviate osteoarthritis‐related pain. Copyright © 2012 John Wiley & Sons, Ltd.     

Antiobesity Effects of Chinese Black Tea (Pu‐erh Tea) Extract and Gallic Acid

The antiobesity effects of Chinese black tea (Pu‐erh tea) and of gallic acid (GA) were investigated using in vitro and in vivo assays. Chinese black tea extract (BTE) and GA inhibited pancreatic lipase activity in a dose‐dependent manner in vitro; the IC(inhibitory concentration)₅₀ values were 101.6 and 9.2 µg/mL, respectively. Black tea extract (50, 100 mg/kg body weight (b.w.)) and GA (15, 45 mg/kg b.w.) significantly suppressed the elevation of blood triglyceride after oral administration of a corn oil emulsion (8 mL oil/kg b.w.) to male ddY mice. Moreover, the antiobesity effects of BTE and GA were also evaluated in a mouse model of diet‐induced obesity. Female ddY mice were divided into seven groups; normal diet (ND) group, high fat diet (HFD) group, BTE (0.2% and 0.6% of diets) groups, and GA (0.007%, 0.02% and 0.1% of diets) groups; the experimental groups were fed the test diets for 12 weeks. The BTE 0.6% and GA 0.1% groups showed significant suppression of weight gain. The weight of parametrial adipose tissue was strongly correlated with the body weight. These results suggest that GA contributes to the antiobesity effect of BTE as an active constituent by inhibiting pancreatic lipase activity. Copyright © 2011 John Wiley & Sons, Ltd.     

Pycnogenol® efficiency on glycaemia,motor nerve conduction velocity and markers of oxidative stress in mild type diabetes in rats

The aim of this study was to describe the effects of Pycnogenol^® at various doses on preprandial and postprandial glucose levels, the levels of thiobarbituric acid reactive substances (TBARs) and N‐acetyl‐β‐d ‐glucosaminidase (NAGA) and on motor nerve conduction velocity (MNCV) in streptozotocin (STZ)‐induced diabetic rats. Pycnogenol^® treatment (10, 20, 50 mg/kg body weight (b.w.)/day) lasted for 8 weeks after induction of diabetes. Pycnogenol^® significantly decreased elevated levels of preprandial glycaemia in treated animals at all doses. At doses of 10 mg/kg b.w./day and 20 mg/kg b.w./day it significantly decreased elevated levels of postprandial glycaemia compared with diabetic non‐treated animals. Pycnogenol^® failed to induce a significant decrease of postprandial glycaemia at a dose of 50 mg/kg b.w./day. Pycnogenol^® improved significantly the impaired MNCV at doses of 10 and 20 mg/kg b.w./day compared with non‐treated animals. The levels of TBARs were elevated in diabetic rats. The levels of NAGA increased gradually despite the treatment. Pycnogenol^® failed to affect the increased levels of TBARs and NAGA. Pycnogenol^® lowered the elevated levels of glycaemia and reduced the decline in motor nerve conduction velocity in STZ‐induced diabetic rats. The effect of Pycnogenol^® on postprandial glycaemic levels and MNCV was not dose‐dependent. Copyright © 2009 John Wiley & Sons, Ltd.     

白边岛衣多糖抗肿瘤作用的研究

白边岛衣多糖腹腔注射200mg/kg(1/5LD₅₀)能显著抑制小鼠肉瘤180、艾氏腹水癌和宫颈癌-u14等肿瘤的生长,但不能延长白血病L7217小鼠的存活时间,50mg/kg和100mg/kg(1/10和1/20 LD₅₀)能增加小鼠网状内皮系统的吞噬功能。     

马钱苷联合miR-3619-5p靶向迁移侵袭增强因子1对宫颈癌SiHa细胞迁移和凋亡的影响

目的 研究马钱苷联合miR-3619-5p靶向迁移侵袭增强因子1(migration and invasion enhancer 1,MIEN1)对宫颈癌SiHa细胞迁移和凋亡的影响。方法 采用qRT-PCR法检测宫颈癌SiHa、Hela、CasKi细胞和正常宫颈上皮Ect1/E6E7细胞中miR-3619-5p m RNA表达。在宫颈癌SiHa细胞中转染miR-3619-5p mimics上调miR-3619-5p的表达,给予马钱苷处理,采用CCK-8法分析细胞增殖;流式细胞术分析细胞凋亡;Transwell小室分析细胞迁移和侵袭能力的变化;Western blotting法分析剪切型半胱氨酸天冬氨酸蛋白酶-3(cleaved cystein-asparate protease-3,cleaved Caspase-3)和基质金属蛋白酶-2(matrix metalloprotease-2,MMP-2)蛋白表达。生物信息学软件预测miR-3619-5p的靶基因,利用荧光素酶报告系统鉴定二者的靶向关系。在宫颈癌SiHa细胞中共转染miR-3619-5p mimics和MIEN1过表达载体...     

Role for monoaminergic systems in the antidepressant-like effect of ethanol extracts from Hemerocallis citrina

Ethnopharmacological relevance

Hemerocallis citrina, a traditional herbal medicine, has been used for the improvement of emotions in Eastern-Asia countries.

Aim of the study

Herein, we explored the antidepressant-like effect and its monoaminergic mechanism of the ethanol extracts from Hemerocallis citrina (HCE).

Materials and methods

Effect of HCE (90, 180 and 360 mg/kg, p.o.) on the immobility time was assessed in the mouse forced swim test (FST) and tail suspension test (TST), and locomotor activity was evaluated in the open-field test (OFT). Additionally, the monoamine neurotransmitters serotonin (5-HT), noradrenaline (NA) and dopamine (DA) levels involved in the antidepressant-like effect of HCE were also measured in the mice brain regions of frontal cortex and hippocampus.

Results

HCE (90, 180 and 360 mg/kg, p.o.) administration significantly reduced the immobility time in both the FST and TST without accompanying changes in locomotor activity in the OFT. The pretreatment of mice with WAY 100635 (0.1 mg/kg, s.c., a 5-HT_1A receptor antagonist), cyproheptadine (3 mg/kg, i.p., a 5-HT₂ receptor antagonist), prazosin (62.5 μg/kg, i.p., an α₁-adrenoceptor antagonist), yohimbine (1 mg/kg, i.p., an α₂-adrenoceptor antagonist), propranolol (5 mg/kg, i.p., a β-adrenoceptor antagonist) or sulpiride (50 mg/kg, i.p., a dopamine D₂ receptor antagonist), but not SCH23390 (0.05 mg/kg, s.c., a dopamine D₁ receptor antagonist) prevented the antidepressant-like effect of HCE (360 mg/kg, p.o.) in the TST. In addition, HCE enhanced 5-HT and NA levels in the frontal cortex and hippocampus as well as elevated DA levels in the frontal cortex.

Conclusion

The results indicate that the antidepressant-like effect of HCE is dependent on the serotonergic (5-HT_1A and 5-HT₂ receptors), noradrenergic (α₁-, α₂- and β-adrenoceptors) and dopaminergic (D₂ receptor) systems as well as the elevation of 5-HT, NA and DA levels in the mouse brain.