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Evidence-based Complementary and... 2021Linn. (CQ) is a medicinal plant with good evidence for the treatment of hemorrhoids, listed in the Thai National List of Herbal Products in the oral dosage form. (Wall...
BACKGROUND
Linn. (CQ) is a medicinal plant with good evidence for the treatment of hemorrhoids, listed in the Thai National List of Herbal Products in the oral dosage form. (Wall ex. DC.) R. K. Jansen. (AP) is a medicinal plant with a local anesthetic effect.
OBJECTIVE
To investigate the potential of rectal suppositories containing CQ and AP extracts to alleviate symptoms of hemorrhoids compared with the commercialized rectal suppository containing hydrocortisone and cinchocaine.
MATERIALS AND METHODS
Hemorrhoid outpatients ( = 105) with different severity grades (I, II, or III) from eight hospitals in northern Thailand were included in this study. Hemorrhoid severity was graded by proctoscopy associated with either anal pain or bleeding related to hemorrhoids or both. The patients were randomly allocated to two groups: CQ-AP group ( = 52) or the commercialized rectal suppository group ( = 53). One suppository was rectally administered twice daily in the morning and at bedtime for seven days. Evaluations were performed by physicians on days 1, 4, and 8 of the study. The primary endpoints were bleeding and prolapse size, while the secondary endpoint was anal pain.
RESULTS
Baseline demographics, lifestyle, constipation, number of prolapses, grade of hemorrhoid severity, and duration of experiencing hemorrhoids were comparable in both groups of patients. The effects of CQ-AP and the commercialized rectal suppository on bleeding, prolapse size, and anal pain were comparable. The patients in both groups were satisfied with both products at comparable levels and stated a preference for further use in the case of hemorrhoids recurrence. In terms of safety, the patients in the commercialized rectal suppository group experienced a higher incidence of adverse events, including anal pain and bleeding.
CONCLUSION
Rectal suppositories containing a combined extract of CQ and AP show potential in alleviating hemorrhoidal symptoms with a good safety profile.
PubMed: 34765003
DOI: 10.1155/2021/5605323 -
PloS One 2015Butyrylcholinesterase (BChE) activity assay and inhibitor phenotyping can help to identify patients at risk of prolonged paralysis following the administration of...
Butyrylcholinesterase (BChE) activity assay and inhibitor phenotyping can help to identify patients at risk of prolonged paralysis following the administration of neuromuscular blocking agents. The assay plays an important role in clinical chemistry as a good diagnostic marker for intoxication with pesticides and nerve agents. Furthermore, the assay is also commonly used for in vitro characterization of cholinesterases, their toxins and drugs. There is still lack of standardized procedure for measurement of BChE activity and many laboratories use different substrates at various concentrations. The purpose of this study was to validate the BChE activity assay to determine the best dilution of human serum and the most optimal concentration of substrates and inhibitors. Serum BChE activity was measured using modified Ellman's method applicable for a microplate reader. We present our experience and new insights into the protocol for high-throughput routine assays of human plasma cholinesterase activities adapted to a microplate reader. During our routine assays used for the determination of BChE activity, we have observed that serum dilution factor influences the results obtained. We show that a 400-fold dilution of serum and 5mM S-butyrylthiocholine iodide can be successfully used for the accurate measurement of BChE activity in human serum. We also discuss usage of various concentrations of dibucaine and fluoride in BChE phenotyping. This study indicates that some factors of such a multicomponent clinical material like serum can influence kinetic parameters of the BChE. The observed inhibitory effect is dependent on serum dilution factor used in the assay.
Topics: Biological Assay; Butyrylcholinesterase; Butyrylthiocholine; Cholinesterase Inhibitors; Humans; Indicator Dilution Techniques; Pesticides
PubMed: 26444431
DOI: 10.1371/journal.pone.0139480 -
Immunology Mar 1982The functional similarities between C-reactive protein (CRP) and immunoglobulin raised the possibility that modified CRP might resemble immunoglobulin in its activating...
The functional similarities between C-reactive protein (CRP) and immunoglobulin raised the possibility that modified CRP might resemble immunoglobulin in its activating effects upon the human platelet. Thermally-aggregated CRP (H-CRP), but not unmodified CRP, induced reactions of aggregation and secretion from isolated platelets; maximum responses occurred with less than 50 microgram/ml H-CRP and were similar to responses mediated by thermally-aggregated human IgG (AHGG). Platelet activation induced by H-CRP was sensitive to the presence of EDTA and dibucaine, required metabolic energy and was inhibited by increased levels of cAMP. Like AHGG, H-CRP acted synergistically with other platelet stimulators, although on a weight basis H-CRP appeared approximately ten- to twenty-fold more effective than AHGG. Complexes formed between CRP and certain of its polycationic ligands (PLL and protamine) shared platelet activating properties with H-CRP, whereas complexes of CRP and CPS did not. These data point to the ability of appropriately modified CRP to stimulate or enhance platelet responsiveness, and taken together with those reactivities described previously between modified CRP and certain lymphocytes, phagocytes, and the complement system, support the concept that CRP can initiate biological activities similar to those mediated by immunoglobulin.
Topics: C-Reactive Protein; Hot Temperature; Humans; Immunoglobulins; In Vitro Techniques; Ligands; Platelet Aggregation; Polylysine; Polysaccharides, Bacterial; Streptococcus pneumoniae
PubMed: 7061105
DOI: No ID Found -
The Biochemical Journal Jan 1987The influence of Ca2+ on myofibrillar proteolysis was evaluated in the isolated extensor digitorum longus muscle incubated in vitro with agents previously shown to...
Differential effects of acute changes in cell Ca2+ concentration on myofibrillar and non-myofibrillar protein breakdown in the rat extensor digitorum longus muscle in vitro. Assessment by production of tyrosine and N tau-methylhistidine.
The influence of Ca2+ on myofibrillar proteolysis was evaluated in the isolated extensor digitorum longus muscle incubated in vitro with agents previously shown to increase the intracellular concentration of Ca2+. Myofibrillar proteolysis was evaluated by measuring the release of N tau-methylhistidine, and total proteolysis was evaluated by measuring tyrosine release by incubated muscles after the inhibition of protein synthesis with cycloheximide. Incubated muscles released measurable quantities of N tau-methylhistidine, and muscle contents of the amino acids remained stable over 2 h of incubation. The release of N tau-methylhistidine by incubated muscles was similar to its release by perfused rat muscle in response to brief starvation, indicating the integrity of the incubated muscles. Ca2+ ionophore A23187, dibucaine, procaine, caffeine and elevated K+ concentration increased lactate release by incubated muscles and decreased tissue contents of ATP and phosphocreatine to varying degrees, indicating the metabolic effectiveness of the agents tested. Only A23187 and dibucaine increased total cell Ca2+, and they increased tyrosine release. Caffeine and elevated [K+] increased neither cell Ca2+ nor tyrosine release; however, only A23187 and dibucaine increased tyrosine release significantly. On the other hand, these agents were without effect on myofibrillar proteolysis as assessed by N tau-methylhistidine release by incubated muscles and changes in tissue contents of the amino acid. In fact, some of the agents tested tended to decrease myofibrillar proteolysis slightly. These results indicate that acute elevation of intracellular Ca2+ is associated with increased breakdown of non-myofibrillar but not myofibrillar proteins. Because of this, the role of elevated Ca2+ in muscle atrophy in certain pathological states is questioned. The data also indicate that the breakdown of myofibrillar and non-myofibrillar proteins in muscle is regulated independently and by different pathways, a conclusion reached in previous studies with perfused rat muscle.
Topics: 2,4-Dinitrophenol; Adenosine Triphosphate; Animals; Calcium; Dinitrophenols; Lactates; Lactic Acid; Male; Methylhistidines; Muscle Proteins; Phosphocreatine; Rats; Rats, Inbred Strains; Starvation; Tyrosine
PubMed: 3566705
DOI: 10.1042/bj2410121 -
European Journal of Hospital Pharmacy :... Jul 2016This work aimed to evaluate the quality of non-sterile formulations compounded at Centro Hospitalar Cova da Beira (Covilhã, Portugal) immediately after preparation and...
OBJECTIVES
This work aimed to evaluate the quality of non-sterile formulations compounded at Centro Hospitalar Cova da Beira (Covilhã, Portugal) immediately after preparation and up to the defined 'beyond-use date'.
METHODS
Microbiological quality control tests were performed in accordance with monograph 5.1.4 of the European Pharmacopoeia 8.0. Samples of compounded products were collected from January to December 2014 after preparation and were analysed immediately and reanalysed after storage under the established conditions, for each preparation.
RESULTS
In the test period, 392 preparations were analysed, corresponding to 24 different formulations (8 intermediate preparations, 11 oral solutions/suspensions and 5 topical preparations). All preparations were in accordance with the pharmacopoeia specifications immediately after preparation. However, for the formulations 'prednisolone oral solution (5 mg/mL)' and 'nitroglycerine and cinchocaine ointment (0.25%/0.5%)', the microbial counts of some batches exceeded the defined limits after storage up to the beyond-use date.
CONCLUSIONS
These results show that the compounding practices implemented at this pharmacy department are able to ensure the microbiological quality of compounded products. This microbiological quality control methodology also allowed identification of the need to replace formulations shown not to be stable throughout the storage period. On the basis of these results, a monthly routine of microbiological control of a random sample of compounded medicines was established in order to ensure their quality and safety for use.
PubMed: 31156854
DOI: 10.1136/ejhpharm-2015-000769 -
Biochimica Et Biophysica Acta Dec 1997Mitochondrial permeability transition (MPT) induced by the thiol cross-linker phenylarsine oxide (PhAsO) in Ca(2+)-depleted mitochondria incubated in the presence of...
Mitochondrial permeability transition (MPT) induced by the thiol cross-linker phenylarsine oxide (PhAsO) in Ca(2+)-depleted mitochondria incubated in the presence of ruthenium red, an inhibitor of the Ca2+ uniporter, is stimulated by the addition of extramitochondrial Ca2+. The presence of extramitochondrial Ca2+ stimulates the reaction of mitochondrial membrane protein thiol groups with PhAsO. Both Ca(2+)-induced increase in mitochondrial membrane permeabilization and protein thiol group reaction with PhAsO are dependent on time (5-10 min to be complete) and the concentration of Ca2+ (1-25 microM). Mitochondrial permeabilization induced by PhAsO (15 microM) and extramitochondrial Ca2+ is inhibited by ADP, cyclosporin A, dibucaine and Mg2+, while mitochondrial permeabilization induced by high concentrations of PhAsO (60 microM) in the absence of Ca2+ is inhibited only by ADP and cyclosporin A. These results suggest that dibucaine and Mg2+ can inhibit mitochondrial permeabilization by antagonizing the effect of Ca2+ on the mitochondrial membrane. Once mitochondrial permeabilization induced by 15 microM PhAsO and extramitochondrial Ca2+ has already occurred, the addition of the Ca2+ chelator EGTA restores mitochondrial membrane potential (MPT pore closure), suggesting that the presence of Ca2+ is essential for the maintenance of the permeability of the mitochondrial membrane to protons (MPT pore opening). In conclusion, the results presented indicate that low Ca2+ concentrations acting at the external side of the inner mitochondrial membrane can stimulate mitochondrial permeability transition induced by PhAsO, due to increased accessibility of protein thiol groups to the reaction with PhAsO and increased probability of MPT pore opening.
Topics: Animals; Arsenicals; Calcium; Calcium Channels; Calcium-Binding Proteins; Chelating Agents; Cross-Linking Reagents; Egtazic Acid; Intracellular Membranes; Membrane Potentials; Membrane Proteins; Mitochondria, Liver; Osmolar Concentration; Permeability; Rats; Rats, Wistar; Ruthenium Red; Sulfhydryl Compounds
PubMed: 9452768
DOI: 10.1016/s0005-2728(97)00078-9 -
The Journal of Cell Biology Feb 1976Tertiary amine local anesthetics (dibucaine, tetracaine, procaine) reversibly affect the morphology of untransformed BALB/3T3 cells and the organization of...
Tertiary amine local anesthetics (dibucaine, tetracaine, procaine) reversibly affect the morphology of untransformed BALB/3T3 cells and the organization of membrane-associated cytoskeletal elements. In the presence of these drugs cells contract and become rounded in shape with the appearance of numerous surface "blebs." Electron microscope examination of anesthetic-treated cells revealed significant reductions in plasma membrane-associated microtubules and microfilaments and/or their plasma membrane attachment. The relationship of the findings on local anesthetic-induced changes in cellular cytoskeletal systems is discussed in relation to previous proposals on plasma membrane organization and control of cell surface receptor topography and mobility.
Topics: Cell Line; Cell Membrane; Cells, Cultured; Dibucaine; Dose-Response Relationship, Drug; Microtubules; Procaine; Tetracaine
PubMed: 1245553
DOI: 10.1083/jcb.68.2.395 -
Revista Do Colegio Brasileiro de... 2014To evaluate the effects of topical policresulen and cinchocaine in the postoperative pain behavior of open hemorrhoidectomy. (Randomized Controlled Trial)
Randomized Controlled Trial
OBJECTIVE
To evaluate the effects of topical policresulen and cinchocaine in the postoperative pain behavior of open hemorrhoidectomy.
METHODS
We conducted a prospective, double-blinded, controlled study. The control group received the usual guidelines with oral medications. The topical treatment group received, in addition, the application of the ointment and was comprised of two subgroups (policresulen + cinchocaine, and placebo). Pain intensity was recorded with the visual analogue scale.
RESULTS
43 patients were operated on: control group - n = 13, one excluded; placebo - n = 15; and policresulen + cinchocaine - n = 15. The mean age was 45.98 years and 37.2% were men. The average pain intensity was 4.09 (immediate postoperative), 3.22 (hospital discharge), 5.73 (day 1) , 5.77 (day 2), 5.74 (day 3), 5.65 (day 7), 5.11 (day 10), 2.75 (day 15) and 7.70 (first bowel movement), with no difference between groups in all periods.
CONCLUSION
This study showed no reduction in pain after hemorrhoidectomy with the use of topical policresulen and cinchocaine.
Topics: Administration, Topical; Analgesia; Anesthetics, Local; Anti-Infective Agents; Cresols; Dibucaine; Double-Blind Method; Drug Combinations; Drug Therapy, Combination; Female; Formaldehyde; Hemorrhoidectomy; Humans; Longitudinal Studies; Male; Middle Aged; Pain Measurement; Pain, Postoperative; Prospective Studies
PubMed: 24918721
DOI: 10.1590/s0100-69912014000200004 -
Anesthesiology Mar 2005Succinylcholine remains the standard neuromuscular blocking drug for tracheal intubation in emergency situations. The short duration of action is due to its rapid...
BACKGROUND
Succinylcholine remains the standard neuromuscular blocking drug for tracheal intubation in emergency situations. The short duration of action is due to its rapid hydrolytic degradation by butyrylcholinesterase (plasmacholinesterase). Multiple variants of this enzyme are known (A, F, S, H, J, K variants) with different effects on enzyme activity. This study was undertaken to evaluate the use of molecular genetic methods in patients with clinically prolonged neuromuscular block.
METHODS
Nine patients with a neuromuscular block of 14 min to 5 h were selected. All four exons of the butyrylcholinesterase were amplified by polymerase chain reaction and analyzed by automated sequencing. Molecular genetic results were compared with clinical relaxation time and with biochemical test results (total butyrylcholinesterase activity, dibucaine and fluoride inhibition).
RESULTS
Seven of nine patients were mutation carriers. Five of these had more than one mutation. The A and K variants were the most frequent variations. Three of four patients who were homozygous for the A variant were also carriers of the K allele. The authors identified one novel mutation (G1294T) introducing a stop codon at amino acid position 432. The duration of neuromuscular block was substantially different between patients with identical butyrylcholinesterase genotypes.
CONCLUSIONS
Variations in the genetic sequence of butyrylcholinesterase are frequent in patients with prolonged duration of action of succinylcholine. Direct sequencing of the whole butyrylcholinesterase gene is an appropriate method for genotyping and, accordingly, should be used in future clinical studies with drugs metabolized by this enzyme (e.g., succinylcholine, mivacurium).
Topics: Adult; Aged; Aged, 80 and over; Butyrylcholinesterase; Child; Female; Genotype; Humans; Male; Mutation; Neuromuscular Blockade; Neuromuscular Depolarizing Agents; Succinylcholine; Time Factors
PubMed: 15731589
DOI: 10.1097/00000542-200503000-00009 -
The Journal of Cell Biology Nov 1976This study makes use of a procedure designed to illustrate, without serial section analysis, the three-dimensional changes in the ciliary axoneme produced by microtubule...
This study makes use of a procedure designed to illustrate, without serial section analysis, the three-dimensional changes in the ciliary axoneme produced by microtubule sliding, and to confirm essential features of the sliding microtubule hypothesis of ciliary movement. Cilia, isolated from Tetrahymena pyriformis by the dibucaine procedure, are attached to polylysine substratum, and treated with Triton X-100. Critical point drying maintains three-dimensional structure without embedding. The detergent removes the membrane and many axonemes unroll, always in an organized fashion so that doublets follow one another in sequence, according to the enantiomorphic form of the cilium. The central pair of microtubules fall to the side as a unit. The parallel doublet microtubules retain relative longitudinal positions in part by interdoublet or nexin links. Spoke organization and tip patterns are preserved in the opened axonemes. We generalize the work of Warner and Satir (Warner, F. D., and P. Satir, 1976. J. Cell Biol. 63:35-63) to show that spoke group arrangements are maintained for all doublets in straight regions, while systematic displacements occur in bent regions. The conclusion that local contraction of microtubles is absent in the axoneme is strengthened, and direct graphic demonstrations of sliding at the ciliary tip are shown. A morphogenetic numbering scheme is presented which results in a quantitative fit of the tip images to the images predicated by the equation for doublet sliding, and which makes possible new comparisons of structural parameters between axonemes and with cilia of other organisms.
Topics: Animals; Cilia; Microtubules; Polyethylene Glycols; Tetrahymena pyriformis
PubMed: 825521
DOI: 10.1083/jcb.71.2.589