THE ESTIMATION OF ANTHRACENE DERIVATIVES IN SENNA AND RHUBARB.
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BACKGROUND: Many methods have been employed, with variable success, in the treatment of cutaneous myiasis caused by Chrysomya species. AIMS: Experiment 1: to assess the larvicidal effect of mineral turpentine (MT) and the main ingredient of MT, low aromatic white spirits (LAWS), on Chrysomya megacephala larvae in vitro. Experiment 2: to assess the larvicidal effects of aqueous extracts of winged senna (Cassia alata), and aqueous extracts, ethanolic extracts and essential oil of betel leaf (Piper betle). METHODS: In experiment 1, two samples of LAWS were obtained from two industrialists (samples 1 and 2). Adult flies of C. megacephala were bred in the insectory of the Department of Parasitology, Faculty of Medicine, University of Colombo. Petri dishes were prepared with pads of cotton wool. These cotton pads were soaked separately in MT, LAWS samples 1 and 2, and normal saline as a control. Ten larvae were placed in each Petri dish. The activity of the larvae was observed and recorded half-hourly. MT and the two samples of LAWS were analyzed by chromatography. In experiment 2, volatile essential oil of betel was prepared using a standard steam distillation process. An ethanolic extract of betel was obtained after boiling the crushed leaf with water, and mixing the stock with ethanol. Betel oil dilutions of 1-4% were prepared using 1% Tween 80 (v/v aq) as a solvent, with 0.05 g/100 mL sodium lauryl sulphate (as stabilizer) and 0.01 g/100 mL methyl paraben (as a preservative). Cotton wool swabs soaked in 1, 2, 3 and 4% essential oil of betel in 1% Tween 80 (v/v aq) prepared as above, 1, 2, 3 and 4% ethanolic extract of betel, 50 and 25% aqueous extract of C. alata, and 50 and 25% aqueous extract of betel were placed in separate Petri dishes. Ten larvae were placed in each Petri dish. 1% Tween 80 solvent with the stabilizer and the preservative, but without betel essential oil, was used as a negative control and MT was used as a positive control. Larval motility was assessed as before. RESULTS: MT and the two LAWS samples killed the larvae in vitro within 4 h. Chromatography showed more unidentified constituents in MT than in pure LAWS, indicating additional substances in MT. The 4 and 3% preparations of the essential oil of betel were effective in killing 100% of the larvae of Chrysomya within 3 h 30 min. The 2% extract of betel essential oil killed 96.7% of larvae in 4 h. Ethanolic and aqueous extracts of betel, the aqueous extract of C. alata, normal saline and the Tween 80 solvent were not larvicidal. CONCLUSIONS: MT and LAWS, the main ingredient of MT, were effective in killing Chrysomya larvae. Essential oil obtained from betel leaves also showed a dose-dependent larvicidal effect on Chrysomya larvae. This natural product may be effective in the treatment of wound myiasis.
From the hexane extract of the bark of the stems of Senna racemosa (syn. Cassia racemosa) a new dihydroanthracenone derivative, named racemochrysone, was isolated. Its structure was established as 8,9-dihydroxy-3-methoxy-2,2,6-trimethyl-(2H)-anthracen-1-one based on spectroscopical data, mainly 1D and 2D NMR experiments. In addition beta-sitosterol, stigmasterol, chrysophanol and physcion were obtained. From the leaves extracts the piperidine alkaloid cassine and the hexitol pinitol were obtained.
For immunization, sennoside B was conjugated with bovine serum albumin. The hapten density in the antigen conjugate was determined to be 3 mol mol(-1) protein by matrix-assisted laser desorption-ionization TOF mass spectrometry. A hybridoma secreting monoclonal antibody against sennoside B was produced by fusing splenocytes from mouse immunized with the sennoside B conjugate and mouse myeloma cells. Weak cross-reactivities occurred with sennoside A which is a stereochemical isomer, and a monomer of sennoside B, rhein, but no cross-reactivity was observed with other related anthraquinones and phenolics. The range of the assay extended from 0.5 ng ml(-1) to 15 ng ml(-1) of sennoside B, and good correlation between ELISA and HPLC methods was obtained when crude extracts of rhubarb were analyzed.
A simple and precise ion-pair high-performance liquid chromatographic method was developed for the determination of sennoside A and B in Rhei Rhizoma. A reversed-phase chromatographic system consisting of a chemically bonded ODS silica gel column with an acetate buffer (pH 5.0)-acetonitrile (68:32), containing 5 mM tetra-n-heptylammonium bromide, as the mobile phase was used. Sennoside A and B in this crude drug were separated and determined within 20 min after direct injection of the solution extracted with 70% methanol. The results for various samples are presented.
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OBJECTIVE: To determine sennoside A in rhubarb extracts by solvent extraction and SFE-CO2. METHODS: Sennoside A was extracted by ultrasonic vibration. The analytical column was Allitima RP C18 (250 x 4.6 mm, 5 microm). The mobile phase consisted of 0.1% TFA-HCN (44:56). The flow rate was 1.0 ml/min. The UV detector wavelength was 280 nm and the reference wavelength was 600 nm. The column temperature was 25 degrees C. RESULT: Considering the extracting rate of sennoside A, solvent extraction was better than SFE-CO2.
Abuse of laxatives, most of them belonging to the group of colonic stimulants or cathartics, can cause various disorders. Extensive diagnostic work can be avoided by early toxicological screening of the suspected patients with respect to laxatives. Because no screening method of this kind was available, we developed a procedure with which all phenolic and anthraquinone laxatives--except sodium picosulfate--can be detected in urine. This method is based on high-performance thin-layer chromatography in two systems after pretreatment of a 20-mL urine sample with beta-glucuronidase and subsequent column extraction. The procedure is very sensitive: at least 32 h after a single dose of bisacodyl, danthron, phenolphthalein, or sennoside, the drug can be detected in the urine. Bisoxatin and oxyphenisatin are still detectable in the urine 18 h after intake. The method is also highly specific; none of 73 other drugs interfered in either of the two chromatographic systems. This procedure can be helpful for the early diagnosis of laxative abuse.
The effects of sennosides (Sen, an extract of Chinese rhubarb) on cellular spontaneous electric activities of guinea pig taenia coli were studied by intracellular microelectrode technique. Sen 0.1-20 mmol.L-1 improved the depolarization of cell membrane, quickened the burst of slow wave potential, and increased notably the frequency of spike potentials. Sen (20 mmol.L-1) induced spontaneous spike potentials. These results provide direct evidence for the enhancing effect of Sen on intestinal peristalsis at cellular level.
A reversed-phase column liquid chromatographic method for the analysis of sennosides A and B present in leaf and pod extracts of Cassia angustifolia has been developed using a Symmetry C18 column and a linear binary gradient profile. The method can be utilised for the quantitative determination of other sennosides as a baseline resolution for most of the constituents was achieved. The method is economical in terms of the time taken and the amount of solvent used (25 mL) for each analysis. The validity of the method with respect to analysis was confirmed by comparing the UV spectra of each peak with those of reference compounds using a photodiode array detector.
OBJECTIVE: To examine the effects of chronic treatment and a single high-dose application of anthranoids and sodium picosulphate on the neuropeptide content of the rat colon. DESIGN AND METHODS: Over a 6-month period, eight groups of rats were each given one of the following: sennosides or sodium picosulphate in low daily doses (10 and 2.5 mg/kg/day, respectively), in high daily doses (40 and 10 mg/kg/day, respectively), and in high twice-weekly doses (30 and 7.5 mg/kg/day, respectively); high daily doses of danthron (500 mg/kg/day); and vehicle (tragacanth 0.5%) only. Four further groups of rats each received a single dose of vehicle or a high dose of one of the three laxatives. All rats were killed 48 h after the last dose. The ascending and descending colon were removed and separated into mucosa, submucosa, and muscularis externa. Vasoactive intestinal polypeptide (VIP), somatostatin, and substance P were extracted by boiling and homogenizing the tissue in acetic acid, and their levels were determined using validated radioimmunoassays. RESULTS: After long-term treatment with high doses of sennosides and danthron, but not after a single high-dose administration, there was a significant reduction in mucosal levels of VIP and somatostatin and in submucosal levels of somatostatin of both colonic segments, as well as in the level of VIP in the muscularis externa of the descending colon. Substance P levels remained unaffected. Sodium picosulphate had no effect. CONCLUSIONS: Chronic treatment with anthranoids in high doses, but not with sodium picosulphate, reduces VIP and somatostatin levels in the rat colon. This may represent damage to the enteric nervous tissue or a pharmacological effect of the anthranoids, causing decreased synthesis or increased breakdown of these peptides.
HYPOTHESIS: Senna is more efficient than polyethylene glycol as mechanical preparation before elective colorectal surgery. DESIGN: Prospective, randomized, single-blind study. SETTING: Multicenter study (18 centers). PATIENTS: Five hundred twenty-three consecutive patients with colonic or rectal carcinoma or sigmoid diverticular disease, undergoing elective colonic or rectal resection followed by immediate anastomosis. INTERVENTION: Two hundred sixty-two patients were randomly allotted to receive senna (1 package diluted in a glass of water) and 261 to receive polyethylene glycol (2 packages diluted in 2-3 L of water), administered the evening before surgery. All patients received 5% povidone iodine antiseptic enemas (2 L) the evening and the morning before surgery. Ceftriaxone sodium and metronidazole were given intravenously at anesthetic induction. MAIN OUTCOME MEASURES: Degree of colonic and rectal cleanliness. RESULTS: Colonic cleanliness was better (P=.006), fecal matter in the colonic lumen was less fluid (P=.001), and the risk for moderate or large intraoperative fecal soiling was lower (P=.11) with senna. Overall, clinical tolerance did not differ significantly between groups, but 20 patients receiving polyethylene glycol (vs 16 with senna) had to interrupt their preparation, and 15 patients (vs 8 with senna) complained of abdominal distension. Senna, however, was better tolerated (P = .03) in the presence of stenosis. There was no statistically significant difference found in the number of patients with postoperative infective complications (14.7% vs 17.7%) or anastomotic leakage (5.3% vs 5.7%) with senna and polyethylene glycol, respectively. CONCLUSION: Mechanical preparation before colonic or rectal resection with senna is better and easier than with polyethylene glycol and should be proposed in patients undergoing colonic or rectal resection, especially patients with stenosis.
Patients undergoing elective left colectomy for colonic carcinoma or diverticulosis (n = 341) were randomly assigned to three groups. Patients in groups 1 (102 patients) and 2 (122 patients) had two 5% povidone-iodine enemas whereas those in group 3 (117 patients) had saline enemas. Groups 1 and 3 received 24-hour intravenous cefotaxime sodium and metronidazole hydrochloride. Group 2 received single injections of ceftriaxone sodium (1 g) and ornidazole (1 g). Senna concentrate was administered the evening before surgery. There was no statistically significant difference found between groups 1 and 2 concerning the number of infected patients (eight vs 11), anastomotic leakages (four vs four), extra-abdominal complications (32 vs 29), or infection-related deaths (one vs zero). Despite poorer tolerance, povidone-iodine enema was more effective than saline enemas, as there were less infected patients in group 1 (8%) or groups 1 + 2 (8.5%) than in group 3 (13%). Single-dose ceftriaxone-ornidazole combined with povidone-iodine enemas is effective against infective complications in elective left colonic surgery for carcinoma or diverticular disease. Single-dose antibiotic prophylaxis reduces costs and work for the nursing staff.
Laxative senna products and several of their specific components have been submitted to a large number of genetic tests. While most studies gave negative responses, results from some of the studies suggest that components of senna products, particularly emodin and aloe-emodin, have genotoxic activity. Assessment of the genotoxicity profile of these substances, in light of other data from animal and human metabolism or kinetic studies, human clinical trials and rodent carcinogenicity studies do not support concerns that senna laxatives pose a genotoxic risk to humans when consumed under prescribed use conditions.
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