OBJECTIVETo study the factors that affect mucosal absorption of gardenia extract.

METHODTake vitro frog skin as a model to study the vitro mucosal permeation. The impacts of the osmotic pressure and the pH value of permeation medium on the Papp of the Jasminoidin were studied, and the effect of frog skin on the stability of Jasminoidin was investigated also.

RESULTThe Papp of Jasminoidin were (0.53 +/- 0.01), (0.21 +/- 0.05), (0.44 +/- 0.12), (0.42 +/- 0.13), (0.26 +/- 0.03) cm x min(-1) by using the normal saline (pH 6.88), pure water, 1.8 % NaCl solution, normal saline (pH 4.05) and normal saline (pH 10.05) as permeation medium for each. The accumulated permeation rate was (55.69 +/- 9.81)% by 12 h, using normal saline as permeation medium respectively, and there was no obvious time lag. Jasminoidin began to degrade around 8 h by affectedof frog skin, the constant of degradation rate (K) was 1.999, and the t1/2 was 0.347 h.

CONCLUSIONThe mucosal permeability of gardenia extract by using the vitro model of frog skin is good, and consistent with zero level absorption process. The osmotic pressure and pH value significantly affected the permeation and the isotonic and partial neutral permeation medium are more conducive to the permeation and absorption of Jasminoidin. The degradation effect of frog skin to the Jasminoidin will not affect mucosal permeation research. In vitro model of frog skin is a suitable way to simulate mucosal permeation process of the gardenia extract.

Gardenia ; chemistry ; Hydrogen-Ion Concentration ; Mucous Membrane ; drug effects ; physiology ; Permeability ; drug effects ; Plant Extracts ; chemistry ; pharmacology ; Skin ; drug effects ; Skin Absorption ; drug effects ; physiology ; Solubility

To investigate the effects of butyl alcohol extract of Baitouweng Decoction(BAEB) on neutrophil chemotaxis in vaginal mucosa of mice with vulvovaginal candidiasis(VVC). Seventy-two SPF female Kunming mice were randomly divided into normal control group, model group, fluconazole group, BAEB low-dose group, middle-dose group and high-dose group. Subcutaneous injection of estradiol benzoate was conducted to induce pseudo-estrus, and then 2×10~6 CFU·mL~(-1)of Candida albicans was inoculated into vaginal lumen, followed by drug treatment for 7 days. Gram staining was used to observe the morphological changes of C. albicans in vagina; vaginal fungal load was detected on agar plate. Histological changes of vaginal tissues in mice were observed by HE staining. Lactate dehydrogenase(LDH), interleukin-6(IL-6) and tumor necrosis factor(TNF-α) levels in mouse lavage fluid were detected by enzyme-linked immunosorbent assay(ELISA). Neutrophils in vaginal lavage fluid was observed and counted by using Pap smear. The levels of IL-8 and MIP-2 in vaginal mucosa were detected by ELISA. IL-8 and MIP-2 mRNA levels in vaginal mucosa of mice were detected by qRT-PCR. The results showed that as compared with the normal group, VVC model group had a large number of hyphae and a high level of fungal loadinvagina. The vaginal mucosa was completely destroyed, the number of neutrophils increased, and the protein and mRNA levels of IL-8 and MIP-2 were up-regulated. After BAEB treatment, the hyphae of the treatment group was decreased, the fungal load was decreased, the impaired mucosa showed different degrees of improvement, the inflammatory factors were decreased to varying degrees, and the protein and mRNA levels of chemokine IL-8 and MIP-2 were down-regulated. In conclusion, BAEB may be used to treat VVC by inhibiting vulvovaginal candidiasis via blocking neutrophils recruitment into vagina.
1-Butanol ; Animals ; Candida albicans ; Candidiasis, Vulvovaginal/drug therapy* ; Chemotaxis/drug effects* ; Drugs, Chinese Herbal/pharmacology* ; Female ; Mice ; Mucous Membrane/drug effects* ; Neutrophils/drug effects* ; Vagina/diagnostic imaging*

Animals ; Anti-HIV Agents ; pharmacology ; HIV ; drug effects ; genetics ; physiology ; HIV Infections ; drug therapy ; immunology ; virology ; Humans ; Mucous Membrane ; immunology ; virology ; Virus Replication ; drug effects

OBJECTIVE: To test the acute and chronic toxicity of topical application of 0.5% podophyllotoxin-loaded nanostructured lipid carriers (POD-NLC) to the vaginal mucosa. METHODS: Twelve New Zealand rabbits were randomized into 3 groups and subjected to daily topical applications of normal saline (control group), 0.5% podophyllotoxin tincture (POD-T) or 0.5% POD-NLC on the vaginal mucosa for 10 consecutive days, and the pathological changes in the mucosa were graded using the Eckstein scoring system.The acute toxicity of POD-NLC was tested in 20 SD female rats, which received intravaginal administration of POD-NLC or vehicle for 3 times within 24 h; After 14 days of continuous observation, the rats were dissected for calculating the viscera coefficient.For testing the chronic toxicity of POD-NLC, 80 SD female rats were randomized into 4 groups and subjected to daily intravaginal administration of the vehicle or POD-NLC at low, moderate or high doses for 13 consecutive weeks.The rats were weighed once a week and at the end of the experiment, 2/3 of the rats from each group were sacrificed to collect blood samples, calculate the viscera coefficient, and examine the pathological changes in the liver.The remaining 1/3 rats were observed for another 2 weeks without further drug treatment and the same examinations were performed. RESULTS: In the rabbits, 0.5% POD-NLC elicited only mild irritation while POD-T caused moderate irritation of the vaginal mucosa.In the acute toxicity test, the organ coefficients were comparable between the rats treated with the vehicle and POD-NLC (>0.05).Long-term intravaginal administration of POD-NLC did not produce significant changes in the behavior, activity, body weight, blood biochemical profiles or organ coefficient as compared with the vehicle control group (>0.05). CONCLUSIONS Intravaginal administration of 0.5% POD-NLC causes very mild irritation without obvious acute or chronic toxicity to the vaginal mucosa in rabbits and rats.
Administration, Intravaginal ; Animals ; Female ; Liposomes ; Mucous Membrane ; drug effects ; Nanostructures ; toxicity ; Podophyllotoxin ; administration & dosage ; toxicity ; Rabbits ; Random Allocation ; Rats ; Vagina ; drug effects

Corticotrophin-releasing factor (CRF) plays a major role in coordinating stress responses. We aimed to test whether blocking endogenous CRF activity can prevent the stress-induced dilation of intercellular spaces in esophageal mucosa. Eighteen adult male rats were divided into 3 groups: 1) a non-stressed group (the non-stressed group), 2) a saline-pretreated stressed group (the stressed group), 3) and an astressin-pretreated stressed group (the astressin group). Immediately after completing the experiments according to the protocol, distal esophageal segments were obtained. Intercellular space diameters of esophageal mucosa were measured by transmission electron microscopy. Blood was sampled for the measurement of plasma cortisol levels. Mucosal intercellular spaces were significantly greater in the stressed group than in the non-stressed group. Mucosal intercellular spaces of the astressin group were significantly smaller than those of the stressed group. Plasma cortisol levels in the stressed group were significantly higher than in the non-stressed group. Pretreatment with astressin tended to decrease plasma cortisol levels. Acute stress in rats enlarges esophageal intercellular spaces, and this stress-induced alteration appears to be mediated by CRF. Our results suggest that CRF may play a role in the pathophysiology of reflux-induced symptoms or mucosal damage.
Animals ; Corticotropin-Releasing Hormone/*antagonists & inhibitors/metabolism/pharmacology ; Esophagus/anatomy & histology/*drug effects ; Extracellular Space/*drug effects ; Hydrocortisone/blood ; Male ; Mucous Membrane/anatomy & histology/*drug effects ; Neuroprotective Agents/pharmacology ; Peptide Fragments/*pharmacology ; Rats ; Rats, Wistar ; *Stress, Psychological/blood/physiopathology

OBJECTIVETo investigate the effects of transforming growth factor-β1 (TGF-β1) on growth controlling and the expression of connective tissue growth factor mRNA(CTGF mRNA) in urethra epithelium cells and fibroblasts cultured in vitro.

METHODSUrethra epithelial cells and fibroblasts were cultured in vitro and identified. The fourth generation cells were divided into control group (cultured by cell medium without TGF-β1) and experimental groups(cultured by cell medium containing TGF-β1 1, 2, 4 and 8 µg/L), the vital force of cells were examined by MTT and cell counting, the expression of CTGF mRNA were examined by RT-PCR after 24 hours.

RESULTSThe optical density and cell count decreased in experimental groups of urethra epithelium cells and increased in experimental groups of fibroblasts with the concentration of TGF-β1 being heightened compared with the control group (P < 0.05). The expression of CTGF mRNA increased with the heightening concentration of TGF-β1 in all experimental groups of urethra epithelium cells and fibroblasts by RT-PCR (P < 0.05).

CONCLUSIONSTGF-β1 can inhibit the growth of urethra epithelium cells and promote the growth of fibroblasts in vitro, it can induce the expression of CTGF mRNA in two cells above-mentioned.

Animals ; Cell Survival ; drug effects ; Cells, Cultured ; Connective Tissue Growth Factor ; genetics ; metabolism ; Epithelial Cells ; cytology ; drug effects ; metabolism ; Fibroblasts ; cytology ; drug effects ; metabolism ; Male ; Mucous Membrane ; cytology ; RNA, Messenger ; genetics ; Rabbits ; Transforming Growth Factor beta1 ; pharmacology ; Urethra ; cytology

Plants in Acaceae family are often considered as ornamental and medicines. However many of them have irritation properties. As medicinal plants some of them are recorded in Chinese Pharmacopoeia and they are figured as poisonous. Through investigating the domestic and overseas studied paper, the needle-like calcium oxalate crystal exits in the plants of Acaceae family could be thought as irritation components of them. This conclusion is same with the studied conclusion of our study group in the medicines plant of Pinellia ternate belonging to the Acaceae family and our studies showed that the needle-like calcium oxalate crystal was the main irritation component of raw P. ternate. The irritated mechanism of raphides is relevant to its special shape, the protein enzyme adhering to it and idioblasts in plants.
Araceae ; chemistry ; Calcium Oxalate ; analysis ; poisoning ; Conjunctival Diseases ; chemically induced ; Crystallization ; Dermatitis, Contact ; etiology ; Humans ; Mucous Membrane ; drug effects ; Pinellia ; chemistry ; Plants, Medicinal ; chemistry

AIMTo assess the efficacy and safety of anal submucosal injection (ASI) of amikacin in chronic bacterial prostatitis (CBP).

METHODSFifty male outpatients with CBP were randomly divided into two groups. Thirty cases of ASI group were given amikacin 400 mg daily by ASI for ten times and the other twenty cases of intramuscular injection (IM) group were given the same drug daily by IM. All patients were evaluated with NIH-Chronic prostatitis symptom index (NIH-CPSI), the bacteria culture of the expressed prostate secretion (EPS), proctoscopic examination, rectal biopsy and the clinical manifestation were checked at pretreatment and on day 7 and 90 after cessation of therapy.

RESULTSThe cure rate, apparent effective rate and effective rate of ASI group and IM group were 33.3% vs 5% (P<0.05), 43.3% vs 10% (P<0.05) and 16.7% vs 20% (P>0.05), respectively. The score of NIH-CPSI in both of ASI group and IM group decreased significantly 7 days after cessation of therapy, both ASI and IM of amikacin could relieve symptoms within a short time. However, 3 months after cessation of therapy the score of NIH-CPSI in ASI group continued down in spite of no significant differences compared with 7 days after cessation of therapy, but the score of IM group was rebound nearly closed to level of pretreatment at 23.8 8.5 and significantly higher than that of ASI group. The amount of white blood cell (WBC) of EPS in ASI group increased slightly at 7 days after cessation of therapy without significant difference with pretreatment (P>0.05), but it significantly decreased at 3 months after cessation of therapy, the amount of WBC of EPS in ASI group was lower than that of IM group at 3 months after cessation of therapy (P<0.05). Proctoscopic examination of anal canal were normal after ASI therapy and the rectum biopsy showed no obvious histopathologic abnormality at the site of injection except mild focal submucosal infiltration of lymphocytes and plasma cells at 7 days after cessation of therapy which disappeared on 3 months after cessation of therapy. All patients had no evident complications.

CONCLUSIONASI could be recommended as a new safe, effective, painless method of antibiotics administration in the treatment of CBP.

Adult ; Amikacin ; administration & dosage ; adverse effects ; Anal Canal ; cytology ; Anti-Bacterial Agents ; administration & dosage ; adverse effects ; Biopsy ; Gram-Negative Bacterial Infections ; drug therapy ; Humans ; Injections ; methods ; Male ; Middle Aged ; Mucous Membrane ; Prostatitis ; drug therapy ; microbiology ; Treatment Outcome

OBJECTIVETo observe the effect of formula of removing both phlegm and blood stasis (TYTZ) in inhibiting the inflammatory reaction in Chinese mini-swine with coronary atherosclerosis.

METHODTotally 36 Chinese mini-swine were randomly divided to six groups: the normal control group, the model group, the Shujiangzhi group and TYTZ groups with does of 2.0, 1.0 and 0.5 g x kg(-1), and six each in every group. Except for the normal control group, all of other groups were fed with high-fat diet for 2 weeks. Interventional balloons are adopted to injure their left anterior descending artery endothelium. After the operation, they were fed with high-fat diet for 8 weeks to prepare the coronary atherosclerosis model. In the 8th week after the operation and administration, the intravascular ultrasound was adopted to observe the coronary artery plaque burden of each group and the pathological morphology of coronary artery. Such inflammatory factors as high-sensitivity C-reactive protein (hs-CRP), tumor necrosis factor (TNF)-alpha and interleukin (IL)-6 were detected by ELISA. The expression of NF-kappaB p65 nuclear translocation was observed by the immunohistochemical method.

RESULTCompared with the normal control group, the model group showed significant increase in the coronary artery plaque burden at the end of the experiment (P < 0.01), notably abnormal structural changes in atherosclerotic vascular tissues, luminal stenosis, a large number of foam cells and inflammatory cell infiltration, remarkable growth of hs-CRP, TNF-alpha and IL-6 levels (P < 0.01). The immunohistochemical staining also showed the significant increase in the NF-kappaB p65 nuclear translocation of coronary artery of Chinese mini-swine in the model group. Compared with the model group, TYTZ could significantly attenuate atherosclerotic plaque burden (P < 0.01), inhibit the coronary luminal stenosis, reduce inflammatory cell infiltration, decrease such inflammatory cell factors as hs-CRP, TNF-alpha and IL-6 in serum, and inhibit the NF-kappaB p65 nuclear translocation of coronary artery (P < 0.05 or P < 0.01).

CONCLUSIONTYTZ can reduce the downstream inflammatory reaction by controlling NF-kappaB p65 nuclear translocation, so as to inhibit the occurrence and development of coronary atherosclerotic plaque in Chinese mini-swine.

Animals ; C-Reactive Protein ; metabolism ; Coronary Artery Disease ; blood ; complications ; drug therapy ; pathology ; Female ; Inflammation ; complications ; Interleukin-6 ; blood ; Male ; Medicine, Chinese Traditional ; methods ; Mucous Membrane ; drug effects ; secretion ; Swine ; Swine, Miniature ; Tumor Necrosis Factor-alpha ; blood

OBJECTIVETo compare the effect of An's Shaobei Injection ([symbols; see text]) with Xiaozhiling Injection ([symbols; see text]) in patients with internal hemorrhoids of grade I-III.

METHODSThis cohort study included 1,520 internal hemorrhoids patients with grade I-III who were scheduled for liquid injection treatment from July 2003 to July 2009. The cohort included patients who underwent either An's Shaobei Injection treatment (the treatment group, 760 cases) or Xiaozhiling Injection treatment (the control group, 760 cases). All patients were followed up regularly for 3 years; the observing indices included anal function recovery and clinical response after operation.

RESULTSAmong the 1,520 patients, 1,508 (99.2%) completed the 3-year follow-up. The efficacy rate was 97.5% in the treatment group, significantly higher than the control group (91.8%, P<0.01). The recurrence rate in the treatment group was 0.5%, significantly lower than that of the control group (1.3%, P<0.01). In addition, perianal callosity occurred in 8 cases (1.1%) and anorectal stricture in 26 cases (3.5%) after operation in the control group. There was no perianal callosity and anorectal stricture in the treatment group.

CONCLUSIONThe treatment with An's Shaobei Injection demonstrated superior clinical effect to Xiaozhiling Injection with fewer adverse effects.

Adult ; Anal Canal ; drug effects ; pathology ; Drugs, Chinese Herbal ; administration & dosage ; adverse effects ; Female ; Follow-Up Studies ; Hemorrhoids ; drug therapy ; pathology ; Humans ; Injections, Intralesional ; Male ; Middle Aged ; Mucous Membrane ; drug effects ; pathology ; Prospective Studies ; Recurrence ; Sclerosing Solutions ; administration & dosage ; adverse effects ; Severity of Illness Index ; Treatment Outcome