• Environmental Analysis Health and Toxicology
• /
• v.15 no.1_2
• /
• pp.13-18
• /
• 2000

A few in vitro methods were developed to compare the result on the phototoxicity of phenothiazines. By the MTT assay, the Candida test, and the RBC photohemolysis, the phototoxicities of UVA and UVB irradiation were measured. This paper presents the comparisons of methods which are effective to measure the phototoxicities of the chemicals causing phototoxicity and photoallergy. The tested chemicals of phenothiazines include Chlorpromazine, Promethazine, Perphenazine, Chlorprothixene, Trifluoperazine and Thioridazine. Each chemical represented variable results according to the test methods. MTT assay shows the most sensitive method.

• Journal of Photoscience
• /
• v.12 no.1
• /
• pp.25-32
• /
• 2005

Binding of N-Alkyl phenothiazines (NAP) to bovine serum albumin (BSA) was studied by spectroscopic methods.It was found that the phenothiazine ring common to all drugs makes major contribution to interaction. However, the nature of alkylamino group at position 10 influences the protein binding significantly. Stern-Volmer plots indicated the presence of static component in the quenching mechanism. The high magnitude of rate constant of quenching indicated that the process of energy transfer occurs by intermolecular interaction and thus the drug-binding site is in close proximity to tryptophan residues of BSA. Binding studies in presence of hydrophobic probe, 8-anilino-1-naphthalein-sulphonic acid showed that there is hydrophobic interaction between drug and the probe and they do not share common sites in BSA. Thermodynamic parameters obtained from data at different temperatures showed that the binding of NAP to BSA predominantly involve hydrophobic forces. The effects of some cations and anions common ions were investigated on NAP-BSA interactions. The CD spectrum of BSA in presence of drug showedthat binding of drug leads to change in the helicity of the protein.

• Bulletin of the Korean Chemical Society
• /
• v.34 no.3
• /
• pp.899-906
• /
• 2013

Using generated conformations from docking analysis by Gold algorithm, some 3D-QSAR models; CoMFA and CoMSIA have been created on 39 N-benzoylated phenoxazines and phenothiazines, including their S-oxidized analogues. These molecules inhibit the polymerization of tubulin into microtubules and thus they have been studied for the development of antitumor drugs. Training set for the CoMFA and CoMSIA models using 30 docked conformations gives $q^2$ Leave one out (LOO) values of 0.756 and 0.617, and $r^2$ ncv values of 0.988 and 0.956, respectively. The ability of prediction and robustness of the models were evaluated by test set, cross validation (leave-one-out and leave-ten-out), bootstrapping, and progressive scrambling approaches. The all-orientation search (AOS) was used to achieve the best orientation to minimize the effect of initial orientation of the structures. The docking results confirmed CoMFA and CoMSIA contour maps. The docking and 3D-QSAR studies were thoroughly interpreted and discussed and confirmed the experimental $pIC_{50}$ values.

• Journal of Food Hygiene and Safety
• /
• v.13 no.3
• /
• pp.232-237
• /
• 1998

The purpose of this study is to examine the phototoxicity of four phenothiazine derivatives such as chlorpromazine, perphenazine, trifluoroperazine and promethazine, and to investigate the effects of ascorbic acid on their phototoxicity by UVB irradiation. Effects of the test compounds on RBCs were monitored with a spectrophotometer by the method of Kahn et al. The extent of photohemolysis by tested phenothiazine derivatives were increased with their concentration and toxic photoproducts were formed by chlorpromazine and promethazine with preirradiated UVB. Photohemolysis postirradiated chlorpromazine and perphenazine and preirradiated promethazine were decreased with the use of ascorbic acid significantly.

• Environmental Analysis Health and Toxicology
• /
• v.5 no.1_2
• /
• pp.45-50
• /
• 1990

In order to investigate the phototoxicity of five phenothiazine derivatives and one thioxanthen derivative were examined by using in vitro method based on growth inhibition of Candida albicans and red blood cell hemolysis. Effects of the test compounds on RBCs were monitored with a spectrophotometer and a drug PI in the Candida albicans was calculated on the basis of the lowest concentration giving a yeast-free zone. All phenothiazines phototoxic in the red blood cell hemolysis method were positive in the yeast test except promethazine. It was also observed that toxic photo-products were formed by perphenazine and chlorpromazine in the red blood cell hemolysis.

• Journal of Food Hygiene and Safety
• /
• v.9 no.1
• /
• pp.15-21
• /
• 1994

The mutagenic activity of four phenothiazine derivatives such as chlorpromazine, perphenazine, trifluoperazine and thioridazine in conjunction with UV-A irradiation or not based on the Ames plate incorporation test in the presence and absence of liver microsomal enzyme(S9 fraction). None of these compounds and their photo-excited were detected as mutagen in the Salmonella microsome assay with TA 98 and TA 100.

• Proceedings of the Korean Society of Applied Pharmacology
• /
• 1994.04a
• /
• pp.328-328
• /
• 1994

광독성 및 광알러지를 일으키는 제반 약물이나 화학물질의 안정성과생체 이용율을 높이고 현재까지 확실하게 규명되어있지 않은 약물 및 화학물질에의한 광독성 광알러지성의 기전을 이해하고 설명할수있는 학문적 기초를 확립 하고저 phenothiazines 중 몇가지 약물를 택하여 적혈구를 이용한 광용혈 여부와 이에 미치는 ascorbic acid, butyl hydroxy anisole, dibutyl hydroxy toluene의 영향을 조사하였다. 각 약물 농도를 50$\mu\textrm{g}$/m1로 하고 UVA(350nm.2.5 ㎽/cm)조사시간은 30분으로 하여 적혈구의 광용혈현상을 Kahn등의 방법에의해 spectrophotometer로 측정한결과 chlorpromazine, perphenazine, thioridazine매 의한 광용혈정도는 ascorbic acid에의해 유의성 있게 감소되었다. 또한 적혈구를 가하기 전 각 약물을 미리조사시켜 생성된 물질에의한 광용혈현상의 광독성생성물질은 chlor- promazine과 thioridazine에서 보여졌으며, chlorpromazine의 광독성생성물질에 의한 적혈구 용혈현상만 ascorbic acid에의해 감소되었다.

• Archives of Pharmacal Research
• /
• v.10 no.3
• /
• pp.153-157
• /
• 1987

Reaction of oxazolin-5-ones 1 with p-amino-diphenylamine was resulted in the formation of the corresponding imidazoline-5-ones 2 which on treatment with sulphur afforded phenothizaines 3. Acridine derivatives 5 were obtained from acetylaminodiphenyl amines derivatives 6 on heating with AnCl$_2$ at $200^{\circ}C.$3 reacted with chloroacetyl chloride to give 7 which reacted in turn with different amines to give 8. Antibacterial activity of the obtained products was studied.

• The Journal of Korean Medicine
• /
• v.23 no.1
• /
• pp.170-176
• /
• 2002

Diabetic Peripheral Polyneuropathy is one of the most distressing complications of diabetes, Drugs such as narcotic analgesics, tricyclic antidepressants, anticonvulsants and phenothiazines have been used to treat diabetic peripheral polyneuropathy, but these drugs are not very effective for the many patients and the side effects may become intolerable. In oriental medicine, usually the main etiology of diabetic Peripheral Polyneuropathy is insufficiency of Blood due to the state of dry-heat in the human body. Therefore, we use Bogan-tang to treat numbness of Diabetic Peripheral Polyneuropathy. Bogan-tang was administrated twice a day for 15 days, and VAS Scale was performed every day to evaluate numbness and insufficiency of blood. In both cases, numbness and insufficiency of blood were improved without any side effects. This study suggests that Bogan-tang is an effective drug in the treatment of Diabetic Peripheral Polyneuropathy.

• Journal of Food Hygiene and Safety
• /
• v.7 no.4
• /
• pp.143-147
• /
• 1992

This study was conducted to investigate the effects of ascorbic add on their phototoxicity of four phenothiazine derivatives such as chloropromazine, perphenazine, trifluoperazine and thioridazine. Effects of the test compounds on RBes were monitored with a spectrophotometer by the method of Kahan et al. The extent of photohemolysis by chlorpromazine, perphenazine and thioridazine were decreased with the use of ascorbic acid. It was observed that toxic photoproducts were formed by chlorpromazine and thioridazine with preirtadiated. Although red blood cell hemolysis by preirradiated chlorpromazine was decreased with the use of ascorbic acid but thioridazine was not changed.