Adduct formation with the DNA bases adenosine, cytidine and guanosine has been shown in vitro. The products were identified as 3-(2'-deoxyribofuranosyl)-7-formylimidazo(2,1-i)purine, chloropropenal derivatives of adenosine and cytidine, etheno derivatives of adenosine, cytidine and guanosine, ethanocarbaldehyde derivatives of adenosine and cytidine and adenosinylethenoadenosine derivatives of adenosine. The later products were postulated to be formed by oxidative properties of mucochloric acid (MCA). The formation of the chloroprenal derivatives, ethanocarbaldehyde derivatives and etheno derivatives from MCA is explained by an initial formation of mucoxychloric acid, which may be further broken down to chloroacetaldehyde, which could proceed via the chloromalonaldehyde that reacts with the nucleosides and forms subsequently the derivatives.
Human Health. There are no reliable experimental data on the toxicokinetic behavior of mucochloric acid (MCA) in vivo available. From the results of acute toxicity studies, it is very likely that MCA itself or its metabolites are systemically available after oral exposure. In vitro, MCA reacted with N-acetylcysteine, cysteine and glutathione (GSH). The acute toxicity (LD50) of MCA was between 300 and 400 mg/kg bw in rats after oral exposure and >200 mg/kg bw (highest tested dose) in rabbits after dermal exposure. The LC50 after 4-hour inhalation exposure of rats was >5.1 mg/L (highest tested concentration). Clinical signs included atonia and ataxia after oral exposure, preening, dyspnea and salivation during inhalation, and skin irritation after dermal exposure. MCA is corrosive to the rabbit skin and eye. A guinea pig sensitization test was negative, but limited experience from occupational exposure in humans indicates a skin sensitizing potential of MCA. There is limited data on repeated dose toxicity available, indicating that irritant/corrosive effects at the site of first contact are the main effects to be expected after repeated exposure. In pregnant rats, no systemic target organ has been identified after oral exposure from day 6 to 19 p.c. (LOAEL: 30 mg/kg bw/day, based on reduced food consumption and body weight gain together with minor clinical symptoms (ptyalism) and whitish foci in the stomach interpreted as local effects due to the corrosive properties of MCA; NOAEL: 5 mg/kg bw/day). No target organ was identified in mice after dietary exposure to 7 mg/kg bw/day for 18 months (only one dose tested). ... In vitro, MCA is a direct acting mutagen and clastogen in mammalian and bacterial cells, and forms exocyclic DNA adducts. In vivo, mucochloric acid caused a slight, but statistically significant increase in the incidence of total nuclear anomalies (including micronuclei, pyknotic nuclei and karyorrhectic nuclei) in the duodenum of mice after a single oral exposure to 60.8 and 79.4 mg/kg bw. MCA induced micronuclei in one animal out of ten per dose group in the duodenum of mice after single oral doses (38.9, 60.8, and 79.4 mg/kg bw). Based on the available in vitro and in vivo data, it can be concluded that MCA has a genotoxic potential. Because of its corrosive properties, and the very limited exposure potential, animal tests with MCA for its effects on fertility were not performed. In an oral developmental study performed in accordance with OECD TG 414 in rats, the NOAEL for maternal toxicity was 5 mg/kg bw/day. The NOAEL for developmental toxicity was 60 mg/kg bw/day, which was the highest dose level applied. There were no signs of developmental toxicity or teratogenicity. MCA did not induce aberrant crypt foci or intestinal tumors when given in drinking water at dose levels of 0.45 and 0.9 mg/mL over 6 weeks to rats or at dose levels of 0.18 and 0.35 mg/mL over 4 weeks with subsequent 12-weeks recovery to mice, respectively. The available data for MCA are not sufficient to judge its carcinogenicity. Given the available data for genotoxicity there are, however, concerns with regard to this endpoint.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
副作用
Dermatotoxin - 皮肤烧伤。
Dermatotoxin - Skin burns.
来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases
毒理性
毒性数据
LC50 (大鼠) = 5,100 毫克/立方米/4小时
LC50 (rat) = 5,100 mg/m3/4h
来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases
毒理性
人类毒性摘录
体征和症状：皮肤：可能会引起过敏性皮肤反应。
/SIGNS AND SYMPTOMS/ Skin: May cause allergic skin reaction.
/SIGNS AND SYMPTOMS/ ... Symptoms of exposure may include burning sensation, coughing, wheezing, laryngitis, shortness of breath, headache, nausea, and vomiting. Inhalation may result in spasm, inflammation and edema of the larynx and bronchi, chemical pneumonitis, and pulmonary edema. Material is extremely destructive to tissue of the mucous membranes and upper respiratory tract, eyes, and skin.
Preparation of substituted butenolides via palladium-free etherification and amination of masked mucohalic acids
申请人：Blazecka Garth Peter
公开号：US20050059831A1
公开（公告）日：2005-03-17
Methods and materials for preparing 4-substituted-2-buten-4-olides are disclosed. The methods include reacting a masked mucohalic acid with a primary or secondary amine or with an arylol in the presence of a base. Unlike existing processes, the disclosed methods do not require the use of palladium, which make them well suited for preparing intermediates in drug syntheses.
COMPOUND SUITABLE FOR DETECTION OF MITOCHONDRIAL COMPLEX-1
申请人：HAMAMATSU PHOTONICS K.K.
公开号：US20150225368A1
公开（公告）日：2015-08-13
Provided is a compound represented by formula (1-0):
wherein in formula (1-0), R represents —O(CH
2
)
n
—, —O(CH
2
)
n
OC
2
H
4
—, —CH
2
O(CH
2
)
n
— or —CH
2
O(CH
2
)
n
OC
2
H
4
—; n represents an integer from 1 to 5; and Q
1
represents F or —OCH
3
.
Oxidative cleavage of DNA by pentamethine carbocyanine dyes irradiated with long-wavelength visible light
作者：Carla T. Mapp、Eric A. Owens、Maged Henary、Kathryn B. Grant
DOI：10.1016/j.bmcl.2013.11.035
日期：2014.1
containing micro molar concentrations of halogenated dye, irradiation at 575, 588, 623, or 700nm produces good photocleavage of plasmid DNA. UV–visible spectra show that the carbocyanines are in their H-aggregated and monomeric forms. Scavenger experiments point to the involvement of singlet oxygen and hydroxyl radicals in DNAphotocleavage.
这里，我们报告七种对称羰花青染料，其中两个氮取代的苯并〔合成ë ]吲哚鎓环通过五甲桥，其接合内消旋与氯或溴与氢取代。苯并[ e ]吲哚的杂原子被苯丙基，甲基或阳离子季铵基团改性。在含有微摩尔浓度的卤化染料的反应中，在575、588、623或700 nm处进行辐照可对质粒DNA进行良好的光裂解。紫外可见光谱表明，花青素呈H聚集和单体形式。清道夫实验指出单重态氧和羟基自由基参与DNA光裂解。
Endocrine-specific NIR fluorophores for adrenal gland targeting
作者：Yoshitomo Ashitate、Andrew Levitz、Min Ho Park、Hoon Hyun、Vivek Venugopal、GwangLi Park、Georges El Fakhri、Maged Henary、Sylvain Gioux、John V. Frangioni、Hak Soo Choi
DOI：10.1039/c6cc03845j
日期：——
The adrenal glands (AGs) are relatively small yet require definitive identification during their resection, or more commonly their avoidance.
