OBJECTIVE: To investigate the effect of pirfenidone for reducing urethral stricture following urethral injury in rats and explore the possible mechanism. METHODS: Thirty male SD rats were randomly assigned into negative control group, positive control group and pirfenidone group (n=10). In pirfenidone and positive control groups, the rats were subjected to incision of the posterior urethral cavernous body followed by daily intraperitoneal injection of pirfenidone (100 mg/kg) and an equivalent volume of solvent, respectively. The rats in the negative control group were given intraperitoneal injections of solvent without urethral injury. At two weeks after modeling, retrograde urethrography was performed for observing urethral stricture, and the injured urethral tissues were harvested for HE staining, Masson staining, immunohistochemical staining and Western blotting for detecting the protein expressions of α-SMA and TGF-β1. The mRNA expressions of the inflammatory factors TNF-α, IL-6, and IL-1β were detected using qRT-PCR. RESULTS: The body weight of the rats in pirfenidone group was significantly decreased compared with that in the other two groups (P < 0.05). Retrograde urethrography showed significant narrowing of the urethra in the positive control group but not in the pirfenidone group. HE staining of the injured urethral tissues showed obvious proliferation of urethral epithelial cells with narrow urethral cavity and increased inflammatory cells in positive control group. The pathological findings of the urethra were similar between pirfenidone group and the negative control group. Masson staining revealed obviously reduced collagen fibers and regular arrangement of the fibers in pirfenidone group as compared to the positive control group. Compared with those in the negative control group, the expressions of α-SMA and TGF-β1 were significantly increased in the positive control group, and pirfenidone treatment significantly inhibited their expressions (P < 0.05 or 0.01). Pirfenidone also significantly inhibited the mRNA expressions of TNF-α, IL-6, and IL-1β in the injured urethral tissue (P < 0.05 or 0.01). CONCLUSION Pirfenidone can prevent urethral fibrosis and stricture after urethral injury possibly by inhibiting the TGF-β1 pathway and inflammatory response.
Animals ; Female ; Humans ; Interleukin-6/metabolism* ; Male ; Pyridones/pharmacology* ; RNA, Messenger/metabolism* ; Rats ; Rats, Sprague-Dawley ; Solvents ; Transforming Growth Factor beta1/metabolism* ; Tumor Necrosis Factor-alpha/metabolism* ; Urethral Stricture/pathology*

Twelve flavonoids were isolated and purified from the ethyl acetate fraction of 95% ethanol extract of Dalbergia odorifera by heat reflux extraction, solvent extraction, recrystallization, normal phase silica gel, Sephadex LH-20, MCI gel and HPLC methods. The structures were identified with multiple spectroscopic methods, including 1 D-NMR, 2 D-NMR and MS. The compounds were identified as 6,7,8-trimethoxy-5,4'-dihydroxy isoflavone(1), medicarpin(2), 7,2'-dihydroxy-4'-methoxy-isoflavanol(3), biochanin A(4), prunetin(5), genistein(6), pratensein(7), 3-(4-hydroxyphenyl)-6-isopentenyl-7-methoxy-4H-chromen-4-one(8), tectorigenin(9), irisolidone(10), vestitol(11), and formononetin(12). Compound 1 was a new isoflavone, and compound 8 was isolated from D. odorifera for the first time. The results showed that compounds 1-3 had inhibitory effects on tyrosinase, with inhibition rates of 35.58%, 38.63% and 51.34% at the concentration of 1.0 mmol·L~(-1), respectively.
Dalbergia/chemistry* ; Ethanol ; Flavonoids/chemistry* ; Genistein ; Isoflavones/pharmacology* ; Monophenol Monooxygenase ; Plant Extracts/pharmacology* ; Silica Gel ; Solvents

Enzymes have a wide range of applications and great industrial potential. However, large-scale applications of enzymes are restricted by the harsh industrial environment, such as high temperature, strong acid/alkali, high salt, organic solvents, and high substrate concentration. Adaptive modification (such as rational or semi-rational design, directed evolution and immobilization) is the most common strategy to improve the catalysis of enzymes under industrial conditions. Here, we review the catalysis of enzymes in the industrial environment and various methods adopted for the adaptive modifications in recent years, to provide reference for the adaptive modifications of enzymes.
Biocatalysis ; drug effects ; Biotechnology ; Enzymes ; chemistry ; metabolism ; Hot Temperature ; Hydrogen-Ion Concentration ; Protein Engineering ; Solvents ; chemistry ; pharmacology

To search for the active diuretic fractions of Clematidis Armandii Caulis( CAC) and determine its main active chemical components by using liquid chromatography-mass spectrometry( LC-MS) and diuretic activity evaluation. CAC 75% ethanol extracts and extracts from different polar solvents were orally administered to saline-loaded rats at different doses. 6 h urinary volume,p H and contents of electrolyte Na+,K+and Cl-were measured. The chemical components of the active fractions were separated and identified by ultra performance liquid chromatography-electrospray ionization-quadrupole time of flight-mass spectrometry( UPLC-ESI-Q-TOF-MS/MS) method. As compared with the control group,the urine volume was increased by 44%( P< 0. 01) and 34%( P < 0. 05) in CAC75% ethanol extract 57. 74 and 28. 8 mg·kg-1 groups respectively; the Na+excretion was increased by 52%( P< 0. 01) and 45%( P<0. 05),respectively; while the Cl-excretion was increased by 101%( P<0. 01) and 85%( P<0. 05),respectively. The urine volume,Na+excretion and Cl-excretion were increased by 50%( P< 0. 01),58%( P< 0. 05),and 65%( P< 0. 05) respectively in petroleum ether extract 70. 98 mg·kg-1 group as compared with the control group. While for the n-butanol extract 194. 18 mg·kg-1 group,the urine volume,Na+and Cl-excretion were increased by 42%( P<0. 01),41%( P<0. 05) and 97%( P<0. 01),respectively. The diuretic activity of other fractions was not obvious. There was no statistical difference in K+excretion in all groups. The results of LC-MS analysis showed that six compounds,including two sterols,one chromogen and three fatty acids,were identified from petroleum ether extract.Fourteen compounds,including six triterpenoid saponins,six lignin glycosides,one sterol glycoside and one phenolic glycoside,were identified from the n-butanol extract. All the results suggested that the ethanol extract of CAC had remarkable diuretic activity and its main effective components included sterol,triterpenoid saponin and lignin glycosides.
Animals ; Ascomycota ; chemistry ; Diuretics ; pharmacology ; Materia Medica ; pharmacology ; Rats ; Solvents ; Spectrometry, Mass, Electrospray Ionization ; Tandem Mass Spectrometry

OBJECTIVETo study and compare the conventional extraction procedure with microwave assisted extraction (MAE) for some Ayurvedic Rasayana drugs and to evaluate their antioxidant potential and carry out the characterization of extracts by thin layer chromatography.

METHODSThree Ayurvedic rasayana plants Allium sativum Linn., Bombax ceiba Linn. and Inula racemosa Hook. were evaluated for an improved MAE methodology by determining the effects of grinding degree, extraction solvent, effect of dielectric constant and duration of time on the extractive value. Antioxidant potential of all three drugs was evaluated with 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity and reducing power was determined by using Gallic acid as standard. Further thin layer chromatographic (TLC) analysis was performed on pre-activated Silica Gel G plates and Rf value were compared with those reported for the important biomarkers.

RESULTSThe total extractive value for Allium sativum Linn. was 36.95% (w/w) and 49.95% (w/w) for ethanol extraction respectively. In case of Bombax ceiba Linn. the yield of aqueous extract by MAE was 50% (w/w) compared to 42% (w/w) in ethanol (50% v/v). Percent yield of Inula racemosa Hook. in aqueous extract was found to be 27.55% (w/w) which was better than ethanol extract (50%) where the yield was 25.95% (w/w). Upon antioxidant activity evaluation. sativum extract showed an absorbance of 0.980±0.92 at concentration of 500 μg with maximum reducing capacity. This was followed by. ceiba Linn. 0.825±0.98 and. racemosa Hook. with 0.799±2.01 at a concentration of 500 μg. TLC based standardization of. sativum Linn. extract shows single spot with Rf value of 0.38, B. ceiba Linn. extract shows Rf values were 0.23, 0.58, 0.77, 0.92 and I. racemosa Hook. extract spot had a Rf value of 0.72.

CONCLUSIONSA significant improvement in extractive values was observed as a factor of time and other advantages by using MAE technology. All three drugs have high antioxidant potential and a TLC profiling similar to reported ones. The presence of fructan type polysaccharide can be further utilized for bioactivity directed fractionation and evaluation of immunomodulatory activity.

Antioxidants ; pharmacology ; Biphenyl Compounds ; chemistry ; Chromatography, Thin Layer ; methods ; Ethanol ; chemistry ; Free Radical Scavengers ; pharmacology ; Inhibitory Concentration 50 ; Medicine, Ayurvedic ; Microwaves ; Oxidation-Reduction ; drug effects ; Pharmaceutical Preparations ; isolation & purification ; Picrates ; chemistry ; Plants, Medicinal ; chemistry ; Solvents ; Time Factors

OBJECTIVETo investigate the antioxidant activity of methanolic extracts of Lantana camara (L. camara) various parts and the determination of their total phenolics content.

METHODSThe extract was screened for possible antioxidant activities by free radical scavenging activity(DPPH), xanthine oxidase inhibition activity and Griess-Ilosvay method.

RESULTSThe results showed that all the plant parts possessed antioxidant properties including radical scavenging, xanthine oxidase inhibition and nitrites scavenging activities. The antioxidative activities were correlated with the total phenol. The leaves extract of L. camara was more effective than that of other parts.

CONCLUSIONSThis study suggests that L. camara extracts exhibit great potential for antioxidant activity and may be useful for their nutritional and medicinal functions.

Allopurinol ; pharmacology ; Antioxidants ; pharmacology ; Chronic Disease ; drug therapy ; Free Radical Scavengers ; pharmacology ; Humans ; Lantana ; chemistry ; Methanol ; Oxidation-Reduction ; Oxidative Stress ; drug effects ; Phenols ; pharmacology ; Phytotherapy ; methods ; Plant Extracts ; pharmacology ; Plant Leaves ; chemistry ; Plant Roots ; chemistry ; Plant Stems ; chemistry ; Plants, Medicinal ; chemistry ; Reactive Oxygen Species ; Solvents

OBJECTIVETo examine the oral toxicity of repeated dosing of Strobilanthes crispus (S. crispus) ethanol leaves extract on the liver and kidney functions in Sprague Dawley rats.

METHODSYoung female rats aged between 8 and 12 week-old were randomly assigned into four groups with five animals each group (n=5). The first group served as control, while the second, third and fourth groups were orally treated with a single dose daily with 150 mg/kg, 300 mg/kg, and 600 mg/kg of S. crispus ethanol leaves extract for 14 d consecutively. Cage-side observation was conducted for first 4 h after each dosing. The body weight changes, food consumptions and water intake were also recorded. Serum biochemical parameters, i.e., aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase, creatinine and urea were determined at Day 15. All results were expressed as mean±SD and analysed using Dunnett's test.

RESULTSIt was obtained that 14-day oral administration of S. crispus ethanol leaves extract did not cause any adverse effects or lethality to the female Sprague Dawley rats. No significant changes in serum biochemical parameters, relative organs weights, body weights, food intake and water consumptions were observed between the treatment groups and control.

CONCLUSIONSIn conclusion, 14-day oral administration of S. crispus ethanol leaves extract was safe to be consumed in female rats without affecting the liver and kidney functions.

Acanthaceae ; chemistry ; toxicity ; Administration, Oral ; Animals ; Dose-Response Relationship, Drug ; Ethanol ; pharmacology ; Female ; Kidney ; drug effects ; pathology ; Liver ; drug effects ; pathology ; Oxidative Stress ; drug effects ; Phytotherapy ; adverse effects ; Plant Extracts ; pharmacology ; Plant Leaves ; chemistry ; toxicity ; Rats ; Rats, Sprague-Dawley ; Solvents ; pharmacology

OBJECTIVETo investigate the in vitro antimicrobial activities of the leaf extract in different solvents viz., methanol, ethanol and water extracts of the selected plant Ricinus communis.

METHODSAgar well diffusion method and agar tube dilution method were carried out to perform the antibacterial and antifungal activity of methanol, ethanol and aqueous extracts.

RESULTSMethanol leaf extracts were found to be more active against Gram positive bacteria (Bacillus subtilis: ATCC 6059 and Staphylococcus aureus: ATCC 6538) as well as Gram negative bacteria (Pseudomonas aeruginosa: ATCC 7221 and Klebsiella pneumoniae) than ethanol and aqueous leaf extracts. Antifungal activity of methanol and aqueous leaf extracts were also carried out against selected fungal strains as Aspergillus fumigatus and Aspergillus flavus. Methanolic as well as aqueous leaf extracts of Ricinus communis were effective in inhibiting the fungal growth.

CONCLUSIONSThe efficient antibacterial and antifungal activity of Ricinus communis from the present investigation revealed that the methanol leaf extracts of the selected plant have significant potential to inhibit the growth of pathogenic bacterial and fungal strains than ethanol and aqueous leaf extracts.

Anti-Bacterial Agents ; pharmacology ; Antifungal Agents ; pharmacology ; Aspergillus ; drug effects ; Gram-Negative Bacteria ; drug effects ; Gram-Positive Bacteria ; drug effects ; Humans ; Methanol ; chemistry ; Microbial Sensitivity Tests ; Plant Extracts ; pharmacology ; Plant Leaves ; chemistry ; Ricinus ; chemistry ; Solvents ; chemistry ; Water ; chemistry

OBJECTIVETo reveal the antibacterial activity of sequentially extracted different cold organic solvent extracts of fruits, flowers and leaves of Lawsonia inermis (L. against) some pathogenic bacteria.

METHODSPowders of fruits, flowers and leaves of L. inermis were continuously extracted with dichloromethane (DCM), ethyl acetate and ethanol at ambient temperature. The dried extracts were prepared into different concentrations and tested for antibacterial activity by agar well diffusion method, and also the extracts were tested to determine the available phytochemicals.

RESULTSExcept DCM extract of flower all other test extracts revealed inhibitory effect on all tested bacteria and their inhibitory effect differed significantly (P<0.05). The highest inhibitory effect was showed by ethyl acetate extract of flower against Staphylococcus aureus (S. aureus) and Pseudomonas aeruginosa (P. aeruginosa), and ethyl acetate extract of fruit on Escherichia coli (E. coli) and Bacillus subtilis (B. subtilis). The ethyl acetate and ethanol extracts of flower, fruit and leaf expressed inhibition even at 1 mg/100 µl against all test bacteria. Among the tested phytochemicals flavonoids were detected in all test extracts except DCM extract of flower.

CONCLUSIONSThe study demonstrated that the ethyl acetate and ethanol extracts of fruit and flower of L. inermis are potentially better source of antibacterial agents compared to leaf extracts of respective solvents.

Anti-Bacterial Agents ; chemistry ; pharmacology ; Bacteria ; drug effects ; Disk Diffusion Antimicrobial Tests ; Flowers ; chemistry ; Fruit ; chemistry ; Lawsonia Plant ; chemistry ; Phytochemicals ; chemistry ; Plant Components, Aerial ; chemistry ; Plant Extracts ; chemistry ; pharmacology ; Plant Leaves ; chemistry ; Solvents ; Sri Lanka

OBJECTIVETo research the mechanism of dormancy and find out the breaking method for the seeds of Epimedium wushanense.

METHODThe water permeability of seed coat was tested by weighing seeds. The germination inhibitor of the seeds were determined with biotic measurement. The development of embryos, germination rate and germination potential were determined after stratification.

RESULTThe water permeability of seed coat was 41.86% after 5 h. The extracts of seeds had strong inhibition effects to the length growth of cabbage seedlings. The growth and development of embryos under the cold stratification (5 degrees C) were better than that under the other conditions. The embryo rate extended from 15.39% to 86.21% after 90 d. Germination rate and germination potential after stratification under 5 degrees C were significantly higher than that under other temperatures.

CONCLUSIONThe results showed that there was no obstacle of water permeability on the test of E. wushanense, after-ripening of embryogenesis and the germination inhibitor of the seed were the main reason for the seed dormancy. The cold stratification would be an effective way for breaking of the dormancy, which could significantly promote the seed embryogenesis and increase germination rate comparing to other methods.

Epimedium ; drug effects ; growth & development ; physiology ; Plant Dormancy ; drug effects ; physiology ; Seeds ; drug effects ; growth & development ; physiology ; Solvents ; pharmacology ; Temperature ; Time Factors ; Water ; pharmacology