1.Synthesis, structure characterization and anti-tumor activity of lanthanide complex Ln (Phen)2 (5-Fu)3 (NO3) (NO3 )2.
Wen-yuan ZHONG ; Zhi-xing HU ; Shun-fang CHEN ; Shu-yu JI ; Yi-ping ZHOU ; Ma-lin LI
Acta Pharmaceutica Sinica 2005;40(11):997-1000
AIMTo study the biochemistry of lanthanides, the cooperative action of inorganic and organic anti-tumor drugs.
METHODSA series of rare earth complexes were synthesized with Ln(NO3) 6H2O, Phen and 5-Fu. Their anti-tumor activity was measured by the improved MTT, SRB methods.
RESULTSThe formula of complex Ln[(Phen)2(5-Fu)3(NO3)](NO3)2(Ln = Y, La, Ce, Sm, Gd, Dy, Er; Phen = 1, 10-phenanthroline; 5-Fu = fluorouracil) was characterized by elemental analyses, molar conductivity, IR, TGA, and 13C NMR spectra. The preliminary biological activity studies indicated that Lanthanide complex has strong anti-tumor activity in vitro.
CONCLUSIONThe complex might have anti-tumor cooperation action.
Antineoplastic Agents ; chemical synthesis ; chemistry ; pharmacology ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Cerium ; chemistry ; Drug Synergism ; Dysprosium ; chemistry ; Erbium ; chemistry ; Fluorouracil ; chemistry ; Gadolinium ; chemistry ; Humans ; Lanthanoid Series Elements ; chemistry ; Lanthanum ; chemistry ; Phenanthrolines ; chemistry ; Samarium ; chemistry ; Structure-Activity Relationship ; Yttrium ; chemistry
2.Transient Receptor Potential C4/5 Like Channel Is Involved in Stretch-Induced Spontaneous Uterine Contraction of Pregnant Rat.
Seungsoo CHUNG ; Young Hwan KIM ; Ji Hyun JOENG ; Duck Sun AHN
The Korean Journal of Physiology and Pharmacology 2014;18(6):503-508
Spontaneous myometrial contraction (SMC) in pregnant uterus is greatly related with gestational age and growing in frequency and amplitude toward the end of gestation to initiate labor. But, an accurate mechanism has not been elucidated. In human and rat uterus, all TRPCs except TRPC2 are expressed in pregnant myometrium and among them, TRPC4 are predominant throughout gestation, suggesting a possible role in regulation of SMC. Therefore, we investigated whether the TRP channel may be involved SMC evoked by mechanical stretch in pregnant myometrial strips of rat using isometric tension measurement and patch-clamp technique. In the present results, hypoosmotic cell swelling activated a potent outward rectifying current in G protein-dependent manner in rat pregnant myocyte. The current was significantly potentiated by 1microM lanthanides (a potent TRPC4/5 stimulator) and suppressed by 10microM 2-APB (TRPC4-7 inhibitor). In addition, in isometric tension experiment, SMC which was evoked by passive stretch was greatly potentiated by lanthanide (1microM) and suppressed by 2-APB (10microM), suggesting a possible involvement of TRPC4/5 channel in regulation of SMC in pregnant myometrium. These results provide a possible cellular mechanism for regulation of SMC during pregnancy and provide basic information for developing a new agent for treatment of premature labor.
Animals
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Female
;
Gestational Age
;
Humans
;
Lanthanoid Series Elements
;
Mice
;
Muscle Cells
;
Myometrium
;
Obstetric Labor, Premature
;
Osmotic Pressure
;
Patch-Clamp Techniques
;
Pregnancy
;
Rats*
;
Uterine Contraction*
;
Uterus
3.A study of in vitro antibacterial activity of lanthanides complexes with a tetradentate Schiff base ligand.
Waleed Mahmoud Al MOMANI ; Ziyad Ahmed TAHA ; Abdulaziz Mahmoud AJLOUNI ; Qasem Mohammad Abu SHAQRA ; Muaz Al ZOUBY
Asian Pacific Journal of Tropical Biomedicine 2013;3(5):367-370
OBJECTIVETo establish the antibacterial activity of lanthanides complexes with a tetradentate Schiff base ligand L.
METHODS(N, N'-bis (1-naphthaldimine)-o-phenylenediamine) was prepared from the condensation of 2-hydroxy-1-naphthaldehyde with o-phenylenediamine in a molar ratio of 2:1. The antimicrobial activity of the resultant Ln (III) complexes was investigated using agar well diffusion and micro-broth dilution techniques; the latter was used to establish the minimum inhibitory concentrations for each compound investigated.
RESULTSMost of Ln (III) complexes were found to exhibit antibacterial activities against a number of pathogenic bacteria with MICs ranging between 1.95-250.00 µg/mL. Staphylococcus aureus was the most susceptible bacterial species to [LaL(NO3)2(H2O)](NO3) complex while Shigella dysenteriae and Escherichia coli required a relatively higher MIC (250 µg/mL). The complexes La (III) and Pr (III) were effective inhibitors against Staphylococcus aureus, whereas Sm (III) complex was effective against Serratia marcescens. On the other hand, Gd (III), La (III) and Nd (III) were found to be more potent inhibitors against Pseudomonas aeruginosa than two of commonly used antibiotics. The remaining Ln (III) complexes showed no remarkable activity as compared to the two standard drugs used.
CONCLUSIONSTetradentate Schiff base ligand L and its complexes could be a potential antibacterial compounds after further investigation.
Anti-Bacterial Agents ; chemistry ; pharmacology ; Bacteria ; drug effects ; Disk Diffusion Antimicrobial Tests ; Lanthanoid Series Elements ; chemistry ; pharmacology ; Ligands ; Microbial Sensitivity Tests ; Schiff Bases ; chemistry
4.A STUDY ON THE PHYSICAL PROPERTIES AND BIOLOGICAL CHARACTERISTICS OF DENTAL MAGNETIC ATTACHMENTS.
Yong Sik LIM ; Yung Soo KIM ; Chang Whe KIM ; Yong Ho KIM
The Journal of Korean Academy of Prosthodontics 1999;37(1):1-22
In order to investigate various physical and biological properties of dental magnetic attachments studies on retentive characteristics, corrosion properties, cytotoxicity of different magnetic systems for dental applications were done. For the study of retentive characteristics changes of retentive force by increasing air gap, wear properties of various attachment systems and loss of magnetic force by heat treatment were measured. For the study of corrosion property of magnet covering metal electrochemical corrosion was done in artificial saliva and 0.9% NaCl solution between -1,000 mVSCE and +1,000 mVSCE. Anodic polarization curves are obtained about 6 types of samples and 2 types of solution. Corroded surfaces were examined with metallurgical microscope, scanning electron microscope and surface profilometer. For the study of cytotoxicity of magnetic attachment and its field cell growth and agar overlay test were done. The results of this study were as follows. 1.In Magnetic attachments using closed circuit retentive force at zero air gap was greater than magnets using open circuit, but decrease of retentive force by increasing air gap was also greater than open systems. 2.After 40,000 cycles of wear test all mechanical attachment resulted in varing degree of retention loss but in magnetic attachments no loss of retentive force was observed. 3.The magnetic attachment using Neodymium magnet showed early loss of retentive force about 200degrees C but attachment using Samarium magnet showed some resistance to heat treatment and complete retention loss was observed about 500degrees C. The keeper was not influenced by heat treatment in retention. 4.In electrochemical corrosion test Dyna magnetic attachment covering metal showed the highiest corrosion resistance and Shiner magnet covering metal showed the least corrosion resistance and examination of corroded surface with metallurgical microscope, scanning electron microscope and surface profilometer also showed same results with anodic polarization curves. 5.The result of cell culture tests on the magnet covered with metal showed least recognizable cytotoxicity.
Agar
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Cell Culture Techniques
;
Corrosion
;
Cyprinidae
;
Hot Temperature
;
Neodymium
;
Population Characteristics*
;
Saliva, Artificial
;
Samarium
5.Advances in collateral damage of laser ablation of dental hard tissues.
Jing LIU ; Pei-jun LÜ ; Yu-chun SUN ; Yong WANG
Chinese Journal of Stomatology 2013;48(9):573-575
Carbon Dioxide
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Dental Enamel
;
injuries
;
Dental Pulp
;
injuries
;
Dentin
;
injuries
;
Erbium
;
Hot Temperature
;
Humans
;
Laser Therapy
;
adverse effects
;
Lasers
;
Lasers, Solid-State
;
Neodymium
;
Tooth
;
radiation effects
6.Mechanism of Acetylcholine-induced Endothelium-dependent Relaxation in the Rabbit Carotid Artery by M3-receptor Activation.
Yong Jin SONG ; Seong Chun KWON
The Korean Journal of Physiology and Pharmacology 2004;8(6):313-317
The present study were designed to characterize the action mechanisms of acetylcholine (ACh) -induced endothelium-dependent relaxation in arteries precontracted with high K (70 mM). For this, we simultaneously measured both muscle tension and cytosolic free Ca2 concentration ([Ca2 ]i), using fura-2, in endothelium-intact, rabbit carotid arterial strips. In the artery with endothelium, high K increased both [Ca2 ]i and muscle tension whereas ACh (10microM) significantly relaxed the muscle and increased [Ca2 ]i. In the presence of NG-nitro-L-arginine (L-NAME, 0.1 mM), ACh increased [Ca2 ]i without relaxing the muscle. In the artery without endothelium, high K increased both [Ca2 ]i and muscle tension although ACh was ineffective. 4-DAMP (10 nM) or atropine (0.1microM) abolished ACh-induced increase in [Ca2 ]i and relaxation. The increase of [Ca2 ]i and vasorelaxation by ACh was siginificantly reduced by either 3microM gadolinium, 10microM lanthanum, or by 10microM SKF 96365. These results suggest that in rabbit carotid artery, ACh-evoked relaxation of 70 mM K -induced contractions appears to be mediated by the release of NO. ACh-evoked vasorelaxation is mediated via the M3 subtype, and activation of the M3 subtype is suggested to stimulate nonselective cation channels, leading to increase of [Ca2 ]i in endothelial cells.
Acetylcholine
;
Arteries
;
Atropine
;
Carotid Arteries*
;
Cytosol
;
Endothelial Cells
;
Endothelium
;
Fura-2
;
Gadolinium
;
Lanthanum
;
Muscle Tonus
;
Nitric Oxide
;
Nitroarginine
;
Relaxation*
;
Vasodilation
7.Ca2+ is a Regulator of the WNK/OSR1/NKCC Pathway in a Human Salivary Gland Cell Line.
Soonhong PARK ; Sang Kyun KU ; Hye Won JI ; Jong Hoon CHOI ; Dong Min SHIN
The Korean Journal of Physiology and Pharmacology 2015;19(3):249-255
Wnk kinase maintains cell volume, regulating various transporters such as sodium-chloride cotransporter, potassium-chloride cotransporter, and sodium-potassium-chloride cotransporter 1 (NKCC1) through the phosphorylation of oxidative stress responsive kinase 1 (OSR1) and STE20/SPS1-related proline/alanine-rich kinase (SPAK). However, the activating mechanism of Wnk kinase in specific tissues and specific conditions is broadly unclear. In the present study, we used a human salivary gland (HSG) cell line as a model and showed that Ca2+ may have a role in regulating Wnk kinase in the HSG cell line. Through this study, we found that the HSG cell line expressed molecules participating in the WNK-OSR1-NKCC pathway, such as Wnk1, Wnk4, OSR1, SPAK, and NKCC1. The HSG cell line showed an intracellular Ca2+ concentration ([Ca2+]i) increase in response to hypotonic stimulation, and the response was synchronized with the phosphorylation of OSR1. Interestingly, when we inhibited the hypotonically induced [Ca2+]i increase with nonspecific Ca2+ channel blockers such as 2-aminoethoxydiphenyl borate, gadolinium, and lanthanum, the phosphorylated OSR1 level was also diminished. Moreover, a cyclopiazonic acid-induced passive [Ca2+]i elevation was evoked by the phosphorylation of OSR1, and the amount of phosphorylated OSR1 decreased when the cells were treated with BAPTA, a Ca2+ chelator. Finally, through that process, NKCC1 activity also decreased to maintain the cell volume in the HSG cell line. These results indicate that Ca2+ may regulate the WNK-OSR1 pathway and NKCC1 activity in the HSG cell line. This is the first demonstration that indicates upstream Ca2+ regulation of the WNK-OSR1 pathway in intact cells.
Cell Line*
;
Cell Size
;
Gadolinium
;
Humans
;
Lanthanum
;
Oxidative Stress
;
Phosphorylation
;
Phosphotransferases
;
Salivary Glands*
;
Sodium Chloride Symporters
;
Sodium-Potassium-Chloride Symporters
8.Recent advances in laser treatment for benign prostatic hyperplasia.
Journal of the Korean Medical Association 2017;60(5):401-408
Benign prostatic hyperplasia (BPH) is one of the most common urological diseases in men after middle age. The most common surgical treatment of BPH is transurethral prostatectomy. Recently, because of the rapid development of lasers, they have been used for the treatment of BPH. The treatment of BPH using lasers has been shown to lead to significant improvements in symptoms and to have excellent therapeutic effects. It is widely used as a minimally invasive treatment of BPH because of the risk and complications associated with transurethral prostate resection. Currently, 3 kinds of lasers are generally used in the treatment of BPH in Korea: potassium-titanyl-phosphate, holmium, and thulium lasers. With developments in laser technology, surgical procedures have improved continuously. The most common surgical procedures are holmium laser enucleation of the prostate (HoLEP), photoselective vaporization of the prostate (PVP), and thulium laser enucleation of the prostate. HoLEP is an effective surgical procedure for large prostates. PVP is safe for patients who are elderly, are in poor general health, or are taking anticoagulants. Thulium laser enucleation of prostate has advantages over PVP and HoLEP surgery due to specific characteristics of the laser and the surgical method. Compared with transurethral prostate resection, laser-based surgical procedures require shorter hospitalization and Foley catheter insertion periods. HoLEP and PVP are safe and effective methods for the surgical treatment of BPH. Therefore, if more data are accumulated from research into these methods, they will become the standard surgical treatments for prostate hyperplasia.
Aged
;
Anticoagulants
;
Catheters
;
Holmium
;
Hospitalization
;
Humans
;
Hyperplasia
;
Korea
;
Lasers, Solid-State
;
Male
;
Methods
;
Middle Aged
;
Prostate
;
Prostatic Hyperplasia*
;
Therapeutic Uses
;
Thulium
;
Transurethral Resection of Prostate
;
Urologic Diseases
;
Volatilization
9.Effect and impact of holmium laser versus thulium laser enucleation of the prostate on erectile function.
Kai HONG ; Yu-qing LIU ; Jian LU ; Chun-lei XIAO ; Yi HUANG ; Lu-lin MA
National Journal of Andrology 2015;21(3):245-250
OBJECTIVETo compare the effect and impact of holmium laser enucleation of the prostate (HoLEP) and 120-W thulium: YAG vapoenucleation of the prostate (ThuVEP) on erectile function in the treatment of benign prostatic hyperplasia (BPH).
METHODSWe retrospectively analyzed 93 cases of symptomatic BPH treated by HoLEP or 120 W ThuVEP. We made comparisons between the two groups of patients in the baseline and postoperative clinical and surgical indexes as well as their IPSS, quality of life (QOL), maximum flow rate (Qmax), postvoid residual urine volume (PVR), and IIEF-EF scores before surgery and during the 12-month follow-up.
RESULTSThuVEP, in comparison with HoLEP, achieved a significantly shorter operation time ([57.6 +/- 12. 8] vs. [70.4 +/- 21.8] min, P = 0.001) and a higher laser efficiency ([0.71 +/- 0.18] vs. [0.62 +/- 0.19] g/min, P = 0. 021). At 1, 6, or 12 months of follow-up, no significant differences were observed in IPSS, OOL, Omax, and PVR between the two groups (P > 0.05). Both the HoLEP and ThuVEP groups showed low incidences of complications and remarkably improved IIEF-EF scores at 12 months postoperatively, but with no significant differences (both P > 0.05). However, in those with relatively normal erectile functions before operation, the mean IIEF-EF score was reduced from 22.8 +/- 2.2 preoperatively to 21.0 +/- 2.7 after HoLEP, (P = 0.036).
CONCLUSIONBoth HoLEP and 120W ThuVEP are effective and safe in the treatment of BPH. Compared with HoLEP, 120 W ThuVEP has even a higher laser efficiency. However, neither can significantly improve erectile function, and HoLEP may have a short-term negative impact on the relatively normal erectile function of the patient.
Aged ; Holmium ; Humans ; Laser Therapy ; adverse effects ; methods ; Lasers, Solid-State ; therapeutic use ; Male ; Middle Aged ; Penile Erection ; Prostatectomy ; adverse effects ; methods ; Prostatic Hyperplasia ; surgery ; Quality of Life ; Retrospective Studies ; Thulium ; Transurethral Resection of Prostate ; Treatment Outcome ; Urine
10.Erbium: YAG Laser Sclerostomy in Rabbits.
Journal of the Korean Ophthalmological Society 1997;38(3):437-442
The present study investigates the effects of the new Erbium:YAG(yttrium aluminum garnet) laser sclerostomy in eight rabbits eyes. The energy was set at 10mJ per pulse with the frequeny of 10Hz, and the total energy for the full thickness sclerostomy procedure was rated at 90 to 150ml. Following the procedure, the mean intraocualar pressure was significantly reduced for up to 7 days, and the histopathological observation at day 7 revealed clearly demarcated wound margins at the resected sites. The sesults suggest that te Erbium:YAG laser sclerostomy may be a good supportive procedures to conventional treatment of glaucoma.
Aluminum
;
Erbium*
;
Glaucoma
;
Lasers, Solid-State*
;
Rabbits*
;
Sclerostomy*
;
Wounds and Injuries