Tag: M.W=450-500

Di Meo, Chiara published the artcilePolyaspartamide-Doxorubicin Conjugate as Potential Prodrug for Anticancer Therapy, Related Products of alcohols-buliding-blocks, the publication is Pharmaceutical Research (2015), 32(5), 1557-1569, database is CAplus and MEDLINE.

The purpose of this study was to synthesize a new polymeric prodrug based on α,β-poly(N-2-hydroxyethyl)(2-aminoethylcarbamate)-d,l-aspartamide copolymer bearing amine groups in the side chain (PHEA-EDA), covalently linked to the anticancer drug doxorubicin and to test its potential application in anticancer therapy. The drug was previously derivatized with a biocompatible and hydrophilic linker, leading to a doxorubicin derivative highly reactive with amino groups of PHEA-EDA. The PHEA-EDA-DOXO prodrug was characterized in terms of chem. stability. The pharmacokinetics, biodistribution and cytotoxicity of the product was investigated in vitro and in vivo on human breast cancer MCF-7 and T47D cell lines and NOD-SCID mice bearing a MCF-7 human breast carcinoma xenograft. Data collected were compared to those obtained using free doxorubicin. The final polymeric product is water soluble and easily hydrolysable in vivo, due to the presence of ester and amide bonds along the spacer between the drug and the polymeric backbone. In vitro tests showed a retarded cytotoxic effect on tumor cells, whereas a significant improvement of the in vivo antitumor activity of PHEA-EDA-DOXO and a survival advantage of the treated NOD-SCID mice was evidenced, compared to that of free doxorubicin. The features of the PHEA-EDA-DOXO provide a potential protection of the drug from the plasmatic enzymic degradation and clearance, an improvement of the blood pharmacokinetic parameters and a suitable body biodistribution. The data collected support the promising rationale of the proposed macromol. prodrug PHEA-EDA-DOXO for further potential development and application in the treatment of solid cancer diseases.

Pharmaceutical Research published new progress about 70539-42-3. 70539-42-3 belongs to alcohols-buliding-blocks, auxiliary class pyrrolidine,Ester,Amide,Inhibitor,Inhibitor, name is Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, and the molecular formula is C18H20N2O12, Related Products of alcohols-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Jahng, Wan Jin published the artcileLecithin Retinol Acyltransferase Forms Functional Homodimers, Recommanded Product: Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, the publication is Biochemistry (2002), 41(20), 6311-6319, database is CAplus and MEDLINE.

Membrane-bound lecithin retinol acyltransferase (LRAT), an essential enzyme in vitamin A processing, catalyzes the formation of retinyl esters from vitamin A and lecithin. Cloned and expressed LRAT has a mol. mass of 25.3 kDa. The enzyme is not homologous to known enzymes and is, therefore, of substantial interest mechanistically. Along these lines, the functional protomeric state of LRAT is of importance. Gel electrophoretic studies on LRAT in the presence of SDS and disulfide reducing agents show the expected 25 kDa monomer. However, gel electrophoresis in the absence of a reducing agent and/or strong denaturing conditions reveals substantial dimer formation. LRAT monomers can be efficiently and irreversibly cross-linked by thiol reactive bismaleimides in retinal pigment epithelial (RPE) membranes generating LRAT homodimers. Cross-linked LRAT homodimers are fully active catalytically. The experiments suggest that LRAT monomers interact in membranes and form functional homodimers through protein-protein interactions and disulfide bond formation.

Biochemistry published new progress about 70539-42-3. 70539-42-3 belongs to alcohols-buliding-blocks, auxiliary class pyrrolidine,Ester,Amide,Inhibitor,Inhibitor, name is Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, and the molecular formula is C18H20N2O12, Recommanded Product: Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Jahng, Wan Jin published the artcileLecithin retinol acyltransferase forms functional homodimers. [Erratum to document cited in CA137:59457], COA of Formula: C18H20N2O12, the publication is Biochemistry (2002), 41(23), 7528, database is CAplus.

In the legend of Figure 2, all millimolar (mM) concentrations should be micromolar (μM). In the legend of Figure 4, the concentrations of RPE and BMH in lane 3 should be 10 μM and those of RPE and BMH in lane 4 should be 50 μM. In footnote c of Table 1, C# is carbamidomethylated cysteine.

Biochemistry published new progress about 70539-42-3. 70539-42-3 belongs to alcohols-buliding-blocks, auxiliary class pyrrolidine,Ester,Amide,Inhibitor,Inhibitor, name is Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, and the molecular formula is C18H20N2O12, COA of Formula: C18H20N2O12.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Cen, Xufeng published the artcilePharmacological targeting of MCL-1 promotes mitophagy and improves disease pathologies in an Alzheimer’s disease mouse model, Formula: C18H14BrNO5S2, the publication is Nature Communications (2020), 11(1), 5731, database is CAplus and MEDLINE.

There is increasing evidence that inducing neuronal mitophagy can be used as a therapeutic intervention for Alzheimer’s disease. Here, we screen a library of 2024 FDA-approved drugs or drug candidates, revealing UMI-77 as an unexpected mitophagy activator. UMI-77 is an established BH3-mimetic for MCL-1 and was developed to induce apoptosis in cancer cells. We found that at sub-LDs, UMI-77 potently induces mitophagy, independent of apoptosis. Our mechanistic studies discovered that MCL-1 is a mitophagy receptor and directly binds to LC3A. Finally, we found that UMI-77 can induce mitophagy in vivo and that it effectively reverses mol. and behavioral phenotypes in the APP/PS1 mouse model of Alzheimer’s disease. Our findings shed light on the mechanisms of mitophagy, reveal that MCL-1 is a mitophagy receptor that can be targeted to induce mitophagy, and identify MCL-1 as a drug target for therapeutic intervention in Alzheimer’s disease.

Nature Communications published new progress about 518303-20-3. 518303-20-3 belongs to alcohols-buliding-blocks, auxiliary class Apoptosis,Bcl-2, name is 2-((4-(4-Bromophenylsulfonamido)-1-hydroxynaphthalen-2-yl)thio)acetic acid, and the molecular formula is C18H14BrNO5S2, Formula: C18H14BrNO5S2.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Yuan, Mingfeng published the artcileDexmedetomidine prevented Hemabate adverse reactions in cesarean section, Related Products of alcohols-buliding-blocks, the publication is Jiangsu Yiyao (2015), 41(21), 2597-2598, database is CAplus.

Dexmedetomidine prevented Hemabate adverse reactions in cesarean section was studied. After Hemabate in cesarean section, D group treated dexmedetomidine and C group was control group. BP, HR, RR, SpO2 were recoreded at room (T0), before Hemabeta (T1), after drug 10 min (T2). At T2, BP and HR were higher than T0, SpO2 of group D change was small, SpO2 of group C decreased. Adverse reaction of group D was lower than group C. Dexmedetomidine reduced Hemabate adverse reactions in cesarean section.

Jiangsu Yiyao published new progress about 58551-69-2. 58551-69-2 belongs to alcohols-buliding-blocks, auxiliary class Chiral,Alkenyl,Amine,Aliphatic cyclic hydrocarbon,Ester,Alcohol,Inhibitor,, name is 2-Amino-2-(hydroxymethyl)propane-1,3-diol (Z)-7-((1R,2R,3R,5S)-3,5-dihydroxy-2-((S,E)-3-hydroxy-3-methyloct-1-en-1-yl)cyclopentyl)hept-5-enoic acid, and the molecular formula is C9H13NO2, Related Products of alcohols-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Lin, Hanfeng published the artcileApplication of carboprost tromethamine in treatment of hypertension in pregnancy, Application In Synthesis of 58551-69-2, the publication is Fujian Yiyao Zazhi (2013), 35(5), 99-100, database is CAplus.

Objective: To investigate application of carboprost tromethamine in treatment of hypertension in pregnancy. Methods: 200 cases of patients with hypertension in pregnancy were selected as a treatment group, and 200 cases of normal pregnancy at the same period were selected as a control group. Two groups underwent lumbar epidural anesthesia for cesarean section surgery, the control group was instantly given oxytocin 20 IU injection for uterine wall after childbirth of fetus, the treatment group was one-time given carboprost tromethamine injection 250 μg after childbirth of fetus, and both groups were given 20 IU of oxytocin via continuous i.v. infusion for 6 h. The bleeding state, incidence of postpartum hemorrhage, Hb level, and blood pressure after childbirth were observed during surgery and after surgery within 2 h and 24 h. Results: Compared with the control group, the amount of bleeding within 2h, 24 h after surgery of the treatment group was lower, and incidence of postpartum hemorrhage was lower (P < 0.05). Blood pressure difference of the two groups was not statistically significant (P > 0.05) and the two groups had no significant adverse reactions. Conclusions: Carboprost tromethamine is an effective measure to prevent postpartum hemorrhage of hypertension in pregnancy.

Fujian Yiyao Zazhi published new progress about 58551-69-2. 58551-69-2 belongs to alcohols-buliding-blocks, auxiliary class Chiral,Alkenyl,Amine,Aliphatic cyclic hydrocarbon,Ester,Alcohol,Inhibitor,, name is 2-Amino-2-(hydroxymethyl)propane-1,3-diol (Z)-7-((1R,2R,3R,5S)-3,5-dihydroxy-2-((S,E)-3-hydroxy-3-methyloct-1-en-1-yl)cyclopentyl)hept-5-enoic acid, and the molecular formula is C25H47NO8, Application In Synthesis of 58551-69-2.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Bhattacherjee, Abhishek published the artcileArgpyrimidine-tagged rutin-encapsulated biocompatible (ethylene glycol dimers) nanoparticles: Application for targeted drug delivery in experimental diabetes (Part 2), Related Products of alcohols-buliding-blocks, the publication is International Journal of Pharmaceutics (Amsterdam, Netherlands) (2017), 528(1-2), 8-17, database is CAplus and MEDLINE.

Diabetes mellitus is characterized by hyperglycemia and associated complications. However, long-term diabetes control is not often sustained by currently available therapeutic approaches. Research on nanoparticle-mediated drug delivery systems is in progress. Here we have tested a ligand (argpyrimidine)-tagged drug (rutin)-encapsulated biocompatible (ethylene glycol dimers) nanoparticle for targeted drug delivery in streptozotocin-induced diabetic rats. Argpyrimidine, being an advanced glycation end product (AGE), directs the nanoparticles to interact with cell surface receptors of AGEs (RAGE) and delivers the drug into the cells. The bioflavonoid rutin possesses antihyperglycemic property, and has been used for nanocapsulation. Two doses of nanoparticles containing 20 mg rutin/kg body weight were administered (i.v. at 7 days interval) into streptozotocin-induced diabetic rats. Compared to free rutin, nanoparticle treatment appears to be significantly more effective in controlling the diabetogenic effects – hyperglycemia, hyperlipidemia, oxidative stress, etc, including heart-associated complications. This approach may thus be explored for drug delivery in the treatment of diabetes mellitus.

International Journal of Pharmaceutics (Amsterdam, Netherlands) published new progress about 70539-42-3. 70539-42-3 belongs to alcohols-buliding-blocks, auxiliary class pyrrolidine,Ester,Amide,Inhibitor,Inhibitor, name is Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, and the molecular formula is C18H20N2O12, Related Products of alcohols-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Zong, Fang published the artcileEfficacy of carboprost tromethamine combined with leonurus japonicus for prevention of postpartum hemorrhage in high-risk pregnant women: A protocol for systematic review and meta-analysis, Related Products of alcohols-buliding-blocks, the publication is Medicine (Philadelphia, PA, United States) (2021), 100(30), e26792, database is CAplus and MEDLINE.

No well-designed and systematic evaluation of the efficacy and safety of leonurus japonicus injection (LJI) in combination with carboprost tromethamine has been found. Therefore, we undertook a meta-anal. to assess the efficacy and safety of carboprost tromethamine combined with LJI for the prevention of postpartum hemorrhage in high-risk pregnant women to provide new evidence-based medical evidence for clin. treatment. This systematic review and meta-anal. would be performed according to Preferred Reporting Items for Systematic reviews and Meta-Analyses guidelines. The following databases including EMBASE, MEDICINE, Wanfang, China National Knowledge Infrastructure database, and Cochrane central controlled trial registries were searched by 2 reviewers from inception to July 2021. Mesh and keyword search terms were “motherwort,” “Yimucao,” “leonurus japonicas,””carboprost tromethamine,” and “postpartum hemorrhage”. Any cohort studies that assessed the efficacy and safety of carboprost tromethamine combined with LJI for the prevention of postpartum hemorrhage would be included. P05 was set as the level of significance. The review would add to the existing literature by showing compelling evidence and improved guidance in clinic settings.

Medicine (Philadelphia, PA, United States) published new progress about 58551-69-2. 58551-69-2 belongs to alcohols-buliding-blocks, auxiliary class Chiral,Alkenyl,Amine,Aliphatic cyclic hydrocarbon,Ester,Alcohol,Inhibitor,, name is 2-Amino-2-(hydroxymethyl)propane-1,3-diol (Z)-7-((1R,2R,3R,5S)-3,5-dihydroxy-2-((S,E)-3-hydroxy-3-methyloct-1-en-1-yl)cyclopentyl)hept-5-enoic acid, and the molecular formula is C10H10N2, Related Products of alcohols-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Ma, Li-hua published the artcileClinical observation of prophylaxis from uterine inertia postpartum hemorrhage by hemabate, Related Products of alcohols-buliding-blocks, the publication is Zhongguo Xueye Liubianxue Zazhi (2011), 21(4), 693-694, 769, database is CAplus.

The objective was to evaluate the effect of prophylaxis from uterine inertia postpartum hemorrhage by hemabate. 90 Cases of puerperal with the postpartum hemorrhage volume â‰?50mL, were divided randomly into the observation groups who were injected with hemabate 250μg in the uterus body immediately, and the control groups who were injected with oxytocin 20U in the uterus body and buccal sublingually misoprostol 400μ g, and the rate of postpartum hemorrhage and the hemorrhage volume of 2h postpartum or 2 to 24h postpartum were compared. Comparing with the control groups, the observation groups had a lower rate of postpartum hemorrhage, and the less hemorrhage volume of 2h postpartum and 2 to 24h postpartum, and the difference had a statistical significance. Hemabate is more effective than misoprostol to prevent postpartum hemorrhage, with the characteristics of high performance, quick effect, safety and convenience.

Zhongguo Xueye Liubianxue Zazhi published new progress about 58551-69-2. 58551-69-2 belongs to alcohols-buliding-blocks, auxiliary class Chiral,Alkenyl,Amine,Aliphatic cyclic hydrocarbon,Ester,Alcohol,Inhibitor,, name is 2-Amino-2-(hydroxymethyl)propane-1,3-diol (Z)-7-((1R,2R,3R,5S)-3,5-dihydroxy-2-((S,E)-3-hydroxy-3-methyloct-1-en-1-yl)cyclopentyl)hept-5-enoic acid, and the molecular formula is C25H47NO8, Related Products of alcohols-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Sawyer, Dennis E. published the artcileThe use of an in vitro sperm activation assay to detect chemically induced damage of human sperm nuclei, Name: Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, the publication is Reproductive Toxicology (1995), 9(4), 351-7, database is CAplus and MEDLINE.

We report that human sperm chem. damaged in vitro by treatment with a reversible crosslinker, ethylene glycol bis(sulfosuccinimidylsuccinate; SEGS), display abnormal chromatin decondensation when analyzed in the human sperm activation assay (HSAA). Less than 20% of SEGS-treated sperm fully decondensed, vs. 97% of control sperm. Chem. reversal of the crosslinks by treatment with 5 μM hydroxylamine restored full decondensation in 76% of treated sperm. These results demonstrate that chem. damaged sperm respond abnormally in the HSAA, and that chem. damage to sperm nuclei can be detected using the HSAA. Thus, there is potential for the HSAA to be used to detect chem. alterations of sperm nuclei from men exposed to environmental toxicants.

Reproductive Toxicology published new progress about 70539-42-3. 70539-42-3 belongs to alcohols-buliding-blocks, auxiliary class pyrrolidine,Ester,Amide,Inhibitor,Inhibitor, name is Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, and the molecular formula is C18H20N2O12, Name: Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts