Month: December 2022

Rasheed, Hafiz Majid published the artcileChemical profiling and anti-breast cancer potential of hexane fraction of Sphaeranthus indicus flowers, Category: esters-buliding-blocks, the main research area is Sphaeranthus flower extract anticancer breast cancer.

The current study aimed to determine the phytochems. and anti-breast cancer potential of Sphaeranthus indicus. S. indicus flowers were extracted with methanol followed by fractionation using n-hexane. For the chem. composition of n-hexane fraction, qual. phytochem. and GC-MS anal. were performed. The anti-proliferative activity was measured by MTT assay, whereas, cytotoxic and proapoptotic effects in MCF-7 (breast cancer) cells were determined using propidium iodide, 4,6-diamidino-2-phenylindole, dichlorofluorescin diacetate, and JC-1 staining through fluorescent microscopy. The phytochem. anal. indicated presence of phytosterols, oils and resins in the nhexane fraction. GC-MS anal. showed that n-hexane fraction comprises of 11 compounds including Me esters of caprylic acid, myristic acid, pentadecanoic acid, palmitic acid, margaric acid, stearic acid, oleic acid, elaidic acid, linoleic acid, linolenic acid and behanic acid. The tested fraction showed remarkable cytotoxic activity against breast cancer (MCF-7) cells while it was found less toxic towards non-cancerous (BHK-21) cells. Furthermore, morphol. assessment through fluorescent microscopy revealed cytotoxic and apoptotic effects by improved cell membrane permeability, increased reactive oxygen species level, compromised mitochondrial activity and condensation of chromatin network. Conclusion: The n-hexane fraction of S. indicus contains phytosterols, oils and fatty acid Me esters and produced apoptotic effect against breast cancer cells.

Tropical Journal of Pharmaceutical Research published new progress about Antitumor agents. 111-11-5 belongs to class esters-buliding-blocks, name is Methyl octanoate, and the molecular formula is C9H18O2, Category: esters-buliding-blocks.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Rasheed, Hafiz Majid published the artcileChemical profiling and anti-breast cancer potential of hexane fraction of Sphaeranthus indicus flowers, Recommanded Product: Methyl docosanoate, the main research area is Sphaeranthus flower extract anticancer breast cancer.

The current study aimed to determine the phytochems. and anti-breast cancer potential of Sphaeranthus indicus. S. indicus flowers were extracted with methanol followed by fractionation using n-hexane. For the chem. composition of n-hexane fraction, qual. phytochem. and GC-MS anal. were performed. The anti-proliferative activity was measured by MTT assay, whereas, cytotoxic and proapoptotic effects in MCF-7 (breast cancer) cells were determined using propidium iodide, 4,6-diamidino-2-phenylindole, dichlorofluorescin diacetate, and JC-1 staining through fluorescent microscopy. The phytochem. anal. indicated presence of phytosterols, oils and resins in the nhexane fraction. GC-MS anal. showed that n-hexane fraction comprises of 11 compounds including Me esters of caprylic acid, myristic acid, pentadecanoic acid, palmitic acid, margaric acid, stearic acid, oleic acid, elaidic acid, linoleic acid, linolenic acid and behanic acid. The tested fraction showed remarkable cytotoxic activity against breast cancer (MCF-7) cells while it was found less toxic towards non-cancerous (BHK-21) cells. Furthermore, morphol. assessment through fluorescent microscopy revealed cytotoxic and apoptotic effects by improved cell membrane permeability, increased reactive oxygen species level, compromised mitochondrial activity and condensation of chromatin network. Conclusion: The n-hexane fraction of S. indicus contains phytosterols, oils and fatty acid Me esters and produced apoptotic effect against breast cancer cells.

Tropical Journal of Pharmaceutical Research published new progress about Antitumor agents. 929-77-1 belongs to class esters-buliding-blocks, name is Methyl docosanoate, and the molecular formula is C23H46O2, Recommanded Product: Methyl docosanoate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Zhou, Tian-Jiao published the artcileA Harmless-Harmful Switchable and Uninterrupted Laccase-Instructed Killer for Activatable Chemodynamic Therapy, COA of Formula: C24H14Cl2O7, the main research area is doxorubicin methoxyhydroquinone laccase chemodynamic therapy cytotoxicity methylene blue photodegradation; chemodynamic therapy; iron-chlorin e6; laccase; photodegradation; superoxide radical.

Chemodynamic therapy (CDT) employs Fenton catalysts to kill cancer cells by converting intracellular hydrogen peroxide (H2O2) into hydroxyl radicals (OH·). Although many studies on H2O2 supplementation have been conducted to improve the therapeutic effect of CDT, few studies have focused on the application of superoxide radical (O2-·) in CDT, which may result in better efficacy. A major concern about O2-·-mediated CDT is its tendency to induce serious oxidative damage to normal tissues, which may be addressed by using a degradable O2-· scavenger. Here, a harmless-harmful switchable and uninterrupted laccase (LAC)-instructed killer (HULK) is constructed, which is the first CDT agent accelerated by LAC-instructed O2-· generation and possesses a harmless-harmful switchable effect because of the photodegradation of the O2-· scavenger iron-chlorin e6 (FeCe6). LAC-instructed substrate oxidation effectively catalyzes O2-· production with the help of intracellular reduction, thereby promoting the conversion of Fe3+ to Fe2+, accelerating the generation of OH·, and inducing tumor cell apoptosis and necrosis. The introduced O2-· scavenger FeCe6 is quickly photodegraded during irradiation, while LAC-instructed O2-· generation proceeds as before, resulting in activatable CDT. This work not only provides the first strategy for LAC-instructed O2-· generation but also presents new insight into activatable CDT.

Advanced Materials (Weinheim, Germany) published new progress about Antitumor agents. 2044-85-1 belongs to class esters-buliding-blocks, name is 2′,7′-Dichloro-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-3′,6′-diyl diacetate, and the molecular formula is C24H14Cl2O7, COA of Formula: C24H14Cl2O7.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Wannasarit, Saowanee published the artcileA virus-mimicking pH-responsive acetalated dextran-based membrane-active polymeric nanoparticle for intracellular delivery of antitumor therapeutics, Recommanded Product: Dodecyl 2-methylacrylate, the main research area is virus mimicking pH acetalated dextran nanoparticle antitumor drug delivery.

Achieving cellular internalization and endosomal escape remains a major challenge for many antitumor therapeutics, especially macromol. drugs. Viral drug carriers are reported for efficient intracellular delivery, but with limited choices of payloads. In this study, a novel polymeric nanoparticle (ADMAP) is developed, resembling the structure and functional features of a virus. ADMAP is synthesized by grafting endosomolytic poly(lauryl methacrylate-co-methacrylic acid) on acetalated dextran. The endosomolytic polymer mimics the capsid protein for endosomal escape, and acetalated dextran resembles the viral core for accommodating payloads. After polymer synthesis, the subsequent controlled nanopptn. on a microfluidic device yields uniform nanoparticles with high encapsulation efficiency. At late endosomal pH (5.0), the ADMAP particles successfully destabilize endosomal membranes and release the drug payloads synergistically, resulting in a greater therapeutic efficacy compared with that of free anticancer drugs. Further conjugation of a tumor-penetrating peptide enhances the antitumor efficacy toward 3D spheroids and finally leads to spheroid disintegration. The unique structure along with the synergistic endosomal escape and drug release make ADMAP nanoparticles favorable for intracellular delivery of antitumor therapeutics.

Advanced Functional Materials published new progress about Antitumor agents. 142-90-5 belongs to class esters-buliding-blocks, name is Dodecyl 2-methylacrylate, and the molecular formula is C16H30O2, Recommanded Product: Dodecyl 2-methylacrylate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Zhu, Jiawei published the artcileMitochondrial Ca2+-overloading by oxygen/glutathione depletion-boosted photodynamic therapy based on a CaCO3 nanoplatform for tumor synergistic therapy, Recommanded Product: 2′,7′-Dichloro-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-3′,6′-diyl diacetate, the main research area is catalase buthionine sulfoximine nanoparticle delivery calcium carbonate chlorin e6; Ca(2+)-buffering capacity; Ca(2+)-overloading; Mitochondrial dysfunction; Oxygen/GSH depletion; Photodynamic therapy.

The Ca2+ buffering capacity of mitochondria maintains the balance of cell physiol. activities. The exogenous reactive oxygen species (ROS) can be used to break the balance, resulting in mitochondrial dysfunction and irreversible cell apoptosis. Herein, the CaCO3-based tumor microenvironment (TME) responsive nanoplatform (CaNPCAT+BSO@Ce6-PEG) was designed for oxygen/GSH depletion-boosted photodynamic therapy (PDT) and mitochondrial Ca2+-overloading synergistic therapy. In acidic TME, CaCO3 decomposed and released the cargos (catalase (CAT), buthionine sulfoximine (BSO), chlorin e6 (Ce6), and Ca2+). The tumor hypoxia and reductive microenvironment could be significantly reversed by CAT and BSO, which greatly enhanced the PDT efficacy. The generated 1O2 during PDT process not only directly killed cancer cells but also destroyed the Ca2+ buffering capacity, leading to the mitochondrial Ca2+-overloading. The increased Ca2+ concentration promoted the process of oxidative phosphorylation and inhibited the production of ATP (ATP), resulting in the acceleration of cell death. Under the joint action of enhanced PDT and mitochondrial Ca2+-overloading, the CaNPCAT+BSO@Ce6-PEG NPs showed remarkable synergistic effects in tumor inhibition without any side effects. In the manuscript, a CaCO3-based nano-platform for tumor microenvironment response was designed. With the decomposition of CaNPCAT+BSO@Ce6-PEG NPs in the acidic tumor microenvironment, the released catalase (CAT) and buthionine sulfoximine (BSO) could relieve the tumor hypoxia and inhibit GSH production Under 660 nm laser irradiation, the photodynamic effect was enhanced and caused apoptosis. Meanwhile, the Ca2+ buffering capacity was destroyed which led to the mitochondrial Ca2+-overloading. The synergistic effect of enhanced PDT and mitochondrial Ca2+-overloading made the CaNPCAT+BSO@Ce6-PEG NPs present remarkable antitumor performance.

Acta Biomaterialia published new progress about Antitumor agents. 2044-85-1 belongs to class esters-buliding-blocks, name is 2′,7′-Dichloro-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-3′,6′-diyl diacetate, and the molecular formula is C24H14Cl2O7, Recommanded Product: 2′,7′-Dichloro-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-3′,6′-diyl diacetate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Olvera-Guillen, Roberto published the artcileSupramolecular poly(vinyl alcohol)-folate structure as functional layer and colloidal stabilizer of poly(vinyl acetate) nanoparticles with potential use as nanocarrier for hydrophobic antitumor agents, Formula: C24H14Cl2O7, the main research area is polyvinyl alc acetate folate nanoparticle stabilizer hydrophobic antitumor agent.

Poly(vinyl acetate) nanoparticles 50 ± 20 nm in diameter were synthesized by emulsion polymerization using poly(vinyl alc.) (PVA) as stabilizer, loaded with eugenol and phys. functionalized with folate in a post-reaction step. Interfacial tension and zeta potential measurements were done to provide evidence about the association between PVA and folate. In order to obtain the target particle size, the effect of the PVA molar mass on the colloidal stability of the latex was studied. The cytotoxic effect of these NPs was evaluated in vitro in the breast triple-neg. cancer cell line MDA-MB-231, and an apoptosis/necrosis assay by flow cytometry was carried out. The capability of the nanocarrier to increase the production of reactive oxygen species in cancer cells was determined by flow cytometry. Nanotoxicol. assessments of the NPs revealed that unloaded NPs were not cytotoxic, that functionalized-loaded NPs induced a decrease in cell viability by up to 70%, and that they induced apoptosis of breast cancer cells due to oxidative stress damage. Cytotoxicity significantly decreased in the absence of folate, suggesting the success of the phys. functionalization in the receptor-mediated drug delivery mechanism.

Journal of Nanoparticle Research published new progress about Antitumor agents. 2044-85-1 belongs to class esters-buliding-blocks, name is 2′,7′-Dichloro-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-3′,6′-diyl diacetate, and the molecular formula is C24H14Cl2O7, Formula: C24H14Cl2O7.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Moles, R. published the artcileWRN-targeted therapy using inhibitors NSC 19630 and NSC 617145 induce apoptosis in HTLV-1-transformed adult T-cell leukemia cells, Related Products of esters-buliding-blocks, the main research area is WRN NSC apoptosis HTLV Tcell leukemia cell; Adult T-cell leukemia/lymphoma (ATLL); Apoptosis; Cycle arrest; Human T-cell leukemia virus type 1 (HTLV-1); WRN helicase.

Background: Human T-cell leukemia virus type 1 (HTLV-1) infection is associated with adult T-cell leukemia/lymphoma (ATLL), a lymphoproliferative malignancy with a dismal prognosis and limited therapeutic options. Recent evidence shows that HTLV-1-transformed cells present defects in both DNA replication and DNA repair, suggesting that these cells might be particularly sensitive to treatment with a small helicase inhibitor. Because the “”Werner syndrome ATP-dependent helicase”” encoded by the WRN gene plays important roles in both cellular proliferation and DNA repair, we hypothesized that inhibition of WRN activity could be used as a new strategy to target ATLL cells. Methods: Our anal. demonstrates an apoptotic effect induced by the WRN helicase inhibitor in HTLV-1-transformed cells in vitro and ATL-derived cell lines. Inhibition of cellular proliferation and induction of apoptosis were demonstrated with cell cycle anal., XTT proliferation assay, clonogenic assay, annexin V staining, and measurement of mitochondrial transmembrane potential. Results: Targeted inhibition of the WRN helicase induced cell cycle arrest and apoptosis in HTLV-1-transformed leukemia cells. Treatment with NSC 19630 (WRN inhibitor) induces S-phase cell cycle arrest, disruption of the mitochondrial membrane potential, and decreased expression of anti-apoptotic factor Bcl-2. These events were associated with activation of caspase-3-dependent apoptosis in ATL cells. We identified some ATL cells, ATL-55T and LMY1, less sensitive to NSC 19630 but sensitive to another WRN inhibitor, NSC 617145. Conclusions: WRN is essential for survival of ATL cells. Our studies suggest that targeting the WRN helicase with small inhibitors is a novel promising strategy to target HTLV-1-transformed ATL cells.

Journal of Hematology & Oncology published new progress about Antitumor agents. 72835-26-8 belongs to class esters-buliding-blocks, name is (2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)methyl propionate, and the molecular formula is C8H9NO4, Related Products of esters-buliding-blocks.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Lau, Meng-Fei published the artcileIn vitro and in silico anticancer evaluation of a medicinal mushroom, Ganoderma neo-japonicum Imazeki, against human colonic carcinoma cells, COA of Formula: C17H34O2, the main research area is Ganoderma neojaponicum Imazeki anticancer human colonic carcinoma cell; Ganoderma neo-japonicum; anticancer; antioxidant; apoptosis; molecular docking.

Ganoderma neo-japonicum is a well-known medicinal mushroom in Asian countries. However, scientific validations on its curative activities are confined to cirrhosis and diabetes. In this study, the anticancer properties of G. neo-japonicum were evaluated using cellular and computational models. The ethanolic extract (EtOH) with a promising inhibitory effect was fractionated into four different fractions: hexane (Hex), chloroform (Chl), butanol (Btn), and aqueous (Aq). The active fractions were then subjected to cell apoptosis assessment and phytochem. profiling. Mol. docking was conducted to elucidate the affinity of selected constituents towards antiapoptotic Bcl-2 protein. The butanol fraction showed the highest antioxidant activities as well as total phenolic content. Both hexane and chloroform fractions exerted a potent cytotoxic effect on colonic carcinoma cells through the induction of apoptosis. Phytochem. anal. revealed that the chloroform fraction is terpenoid enriched whereas the hexane fraction comprises predominantly sterol constituents. Stellasterol and 1,25-dihydroxyvitamin D3 3-glycoside were demonstrated to have a high affinity towards Bcl-2 protein. Overall, G. neo-japonicum can be considered as a compelling therapeutic candidate for cancer treatment.

Biotechnology and Applied Biochemistry published new progress about Antitumor agents. 41114-00-5 belongs to class esters-buliding-blocks, name is Ethyl pentadecanoate, and the molecular formula is C17H34O2, COA of Formula: C17H34O2.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Nguyen, Duc Ba published the artcileApplication of plasma jet to the inhibition of the proliferation of hepatic malignant cells via reactive oxygen species generation, Safety of 2′,7′-Dichloro-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-3′,6′-diyl diacetate, the main research area is hepatic malignant cell proliferation dielec barrier plasma jet discharge.

In vitro treatment of hepatic malignant cells with plasma-activated medium conjugated with gemcitabine was investigated with a He plasma jet generated by a two-ring dielec. barrier discharge (DBD) reactor. The DBD reactor was operated by high-voltage pulses of alternating polarity (frequency: 20 kHz; pulse width: 4 us). The electron d. of plasma plume was estimated to be 9×1012 to 10×1012 cm-3, and the jet temperature was around 36°C. The plasma jet exhibited the inhibitory effects on the growth of hepatic malignant cells via the generation of reactive oxygen species, which could be potentially applicative in anticancer therapies. The optimization of the operating parameters and configuration of the plasma jet would help increase the possibility in practical cancer treatments.

Plasma Processes and Polymers published new progress about Antitumor agents. 2044-85-1 belongs to class esters-buliding-blocks, name is 2′,7′-Dichloro-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-3′,6′-diyl diacetate, and the molecular formula is C24H14Cl2O7, Safety of 2′,7′-Dichloro-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-3′,6′-diyl diacetate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Abeesh, Prathapan published the artcilePreparation and characterization of beta sitosterol encapsulated nanoliposomal formulation for improved delivery to cancer cells and evaluation of its anti-tumor activities against Daltons Lymphoma Ascites tumor models, Application of 2′,7′-Dichloro-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-3′,6′-diyl diacetate, the main research area is beta sitosterol nanoliposome lymphoma cell apoptosis tumor mitigation.

Beta sitosterol (BS) is a dietary phytosterol with promising therapeutic applications. The low bioavailability and rapid degradation of BS is the main challenges for their use in the food and pharmaceutical industries. Liposome mediated drug delivery systems are the useful approaches to improve the biopharmaceutical properties of BS. In this study, we had prepared nanoliposome encapsulated beta sitosterol (LBS) with improved bioavailability and stability. The prepared nanoliposomes had spherical vesicles, with mean particle size of 114.5 nm and had an encapsulation efficiency of 86%. Our in vitro study results showed that LBS treatment could induce apoptosis in lymphoma cell lines as evidenced by acridine orange/ethidium bromide and nuclear staining. Our in vivo studies involving exptl. tumor models revealed that LBS treatment could significantly (p < 0.01) reduce the tumor loads, improve the survival rate, and stabilize the body weights in Dalton's Lymphoma Ascites (DLA) tumor bearing mice when compared to BS. Hematol. and serum biochem. parameters also improved significantly (p < 0.01) after LBS administration than free drug. The overall study results revealed that LBS exhibits promising therapeutic efficacy in comparison with non-encapsulated BS in regulating exptl. tumor development as well as induction of lymphoma cell apoptosis. Journal of Drug Delivery Science and Technology published new progress about Antitumor agents. 2044-85-1 belongs to class esters-buliding-blocks, name is 2',7'-Dichloro-3-oxo-3H-spiro[isobenzofuran-1,9'-xanthene]-3',6'-diyl diacetate, and the molecular formula is C24H14Cl2O7, Application of 2′,7′-Dichloro-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-3′,6′-diyl diacetate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics