Tag: 300-400

Neuroprotective effect of coumarin nasal formulation: kindling model assessment of epilepsy was written by Muke, Suraj;Kaikini, Aakruti;Peshattiwar, Vaibhavi;Bagle, Sneha;Dighe, Vikas;Sathaye, Sadhana. And the article was included in Frontiers in Pharmacology in 2018.Application of 524-12-9 The following contents are mentioned in the article:

Traditional system of medicines has a promise in some of the medicines, which have been used for the treatment of epilepsy. Taking clue from the Ayurvedic system of medicines, we formulated coumarin fraction of EA, namely, coumarin nasal formulation (CNF) for its nasal delivery. CNF was analyzed by using high performance liquid chromatog. (HPLC) and UV absorption spectroscopy for its drug content determination In vitro drug release studies were performed in simulated nasal electrolyte solution (SNES) maintaining constant pH of 5.5 at 37°C. Irritation by CNF was evaluated using HET-CAM assay. Formulation was found to be non-irritant in HET-CAM assay. CNF was further assessed in vivo by measuring the progress and attainment of pentylenetetrazole (PTZ) kindling in mice. Neuronal changes were assessed by hematoxylin and eosin (H&E) and Nissl staining technique. Glial fibrillary acidic protein (GFAP) a neuroinflammatory marker and tumor necrosis factor alpha (TNF-a) an inflammatory marker were also measured. CNF (10 mg/kg, nasal route) when given as a pretreatment lowered seizure score and delayed the progression of seizure similar to diazepam. CNF decreased the PTZ induced oxidative damage, TNF-a as well as GFAP levels in the midbrain tissue particularly in hippocampus region. The results suggest that CNF may be a promising therapeutic approach to offer protection from sudden recurrent seizures alone or in combination with current drugs in management of epilepsy. This study involved multiple reactions and reactants, such as 1,8,9-Trihydroxy-3-methoxy-6H-benzofuro[3,2-c]chromen-6-one (cas: 524-12-9Application of 524-12-9).

1,8,9-Trihydroxy-3-methoxy-6H-benzofuro[3,2-c]chromen-6-one (cas: 524-12-9) belongs to benzofurans derivatives. Benzofuran is the “”parent”” of many related compounds with more complex structures. For example, psoralen is a benzofuran derivative that occurs in several plants. Benzofurans have also made significant and distinctive contributions to biology. They exhibit several biological activities that range from antioxidant, antitubercular, antiplasmodial, insecticidal.Application of 524-12-9

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Biosynthesis of precious metabolites in callus cultures of Eclipta alba was written by Khurshid, Razia;Khan, Taimoor;Zaeem, Afifa;Garros, Laurine;Hano, Christophe;Abbasi, Bilal Haider. And the article was included in Plant Cell, Tissue and Organ Culture in 2018.Electric Literature of C16H10O7 The following contents are mentioned in the article:

Eclipta alba (False daisy) is an important medicinal plant with well-known antihepatotoxic activity. However, no previous in vitro studies are available for its callus culture for increased production of antioxidant secondary metabolites. Herein, we maintained a competent protocol for callus culture of E. alba using stem and leaf explants grown on MS medium containing various concentrations of thidiazuron, 6-benzylaminopurine (BAP) either alone or in association with a-naphthalene acetic acid (NAA). Among all the applied plant growth regulators, BAP along with NAA resulted in maximal dry biomass of 18.0 and 13.8 g/l for stem and leaf explants, resp. Furthermore, the highest production of phenolics (375.7 mg/l for stem-associated callus and 298 mg/l for leaf-associated callus) and flavonoids (62.0 and 52.3 mg/l for stem- and leaf-associated callus, resp.) were found to be present in optimized callus culture. Antioxidant activity was also elucidated for both stem and leaf derived calli. The highest antioxidant activities (~93.5%) were witnessed for stem and leaf associated calli at set concentrations of 3.0 mg/l BAP + 1.0 mg/l NAA and 4.0 mg/l BAP, resp. High-performance liquid chromatog. analyses revealed optimum accumulation of coumarin (1.98 mg/g DW) and wedelolactone (49.63 mg/g DW) in leaf associated callus and desmethylwedelolactone (69.96 mg/g DW), β-amyrin (0.8179 mg/g DW) and eclalbatin (0.3202 mg/g DW) in stem associated callus at optimized concentration This study involved multiple reactions and reactants, such as 1,8,9-Trihydroxy-3-methoxy-6H-benzofuro[3,2-c]chromen-6-one (cas: 524-12-9Electric Literature of C16H10O7).

1,8,9-Trihydroxy-3-methoxy-6H-benzofuro[3,2-c]chromen-6-one (cas: 524-12-9) belongs to benzofurans derivatives. Benzofurans are only weakly aromatic in nature and they are cleaved by many oxidative and reductive conditions. Introduction of benzofurans in organic synthesis, particularly drug synthesis, involves generally the use of their metalated species as nucleophiles in addition reactions or in metal-catalysed cross-coupling reactions.Electric Literature of C16H10O7

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Cytotoxic activity of Christia vespertilionis root and leaf extracts and fractions against breast cancer cell lines was written by Lee, Joanna Jinling;Yazan, Latifah Saiful;Kassim, Nur Kartinee;Abdullah, Che Azurahanim Che;Esa, Nurulaidah;Lim, Pei Cee;Tan, Dai Chuan. And the article was included in Molecules in 2020.HPLC of Formula: 524-12-9 The following contents are mentioned in the article:

Christia vespertilionis, commonly known as ‘Daun Rerama’, has recently garnered attention from numerous sources in Malaysia as an alternative treatment. Its herbal decoction was believed to show anti-inflammatory and anti-cancer effects. The present study investigated the cytotoxicity of the extract of root and leaf of C. vespertilionis. The plant parts were successively extracted using the solvent maceration method. The most active extract was further fractionated to afford F1-F8. The cytotoxic effects were determined using MTT assay against human breast carcinoma cell lines (MCF-7 and MDA-MB-231). The total phenolic content (TPC) of the extracts were determined The antioxidant properties of the extract were also studied using DPPH and β-carotene bleaching assays. The Et acetate root extract demonstrated selective cytotoxicity especially against MDA-MB-231 with the highest TPC and antioxidant properties compared to others (p < 0.05). The TPC and antioxidant results suggest the contribution of phenolic compounds toward its antioxidant strength leading to significant cytotoxicity. F3 showed potent cytotoxic effects while F4 showed better antioxidative strength compared to others (p < 0.05). Qual. phytochem. screening of the most active fraction, F3, suggested the presence of flavonoids, coumarins and quinones to be responsible toward the cytotoxicity. The study showed the root extracts of C. vespertilionis to possess notable anti-breast cancer effects. This study involved multiple reactions and reactants, such as 1,8,9-Trihydroxy-3-methoxy-6H-benzofuro[3,2-c]chromen-6-one (cas: 524-12-9HPLC of Formula: 524-12-9).

1,8,9-Trihydroxy-3-methoxy-6H-benzofuro[3,2-c]chromen-6-one (cas: 524-12-9) belongs to benzofurans derivatives.Benzofuran is one of the most significant oxygen-containing heterocycles consisting of fused benzene and furan ring, which are widely presented in various naturally occurring and synthetically active compounds. Benzofurans are stable towards alkali and readily polymerize on treatment with sulfuric acid, due to which they are useful for the preparation of low cost chemically relatively inert resins.HPLC of Formula: 524-12-9

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Comparative botanical and phytochemical studies of ambiguous medicinal plant species of Wedelia and Eclipta (Fam. Asteraceae) used in ASU systems of medicine with special reference to in-silico screening of hepatoprotective potential of marker wedelolactone with acetaminophen targets was written by Arunachalam, C.;Arunadevi, R.;Murugammal, S.;Monika, N.;Susila, R.;Kumar, S. N. Sunil. And the article was included in Pharmacognosy Research in 2020.Category: benzofurans The following contents are mentioned in the article:

Context: In traditional medicine, Kesaraja (Ayurveda) or Manjal karisali (Siddha) is effective for jaundice. They are Wedelia chinensis (Osbeck) Merr. Philipp J., Wedelia trilobata (L.) Hitchc. and Eclipta prostrata (L.). The present study aimed to screen and characterize the potential species for therapeutic purpose. The whole plants, W. chinensis (Osbeck) Merr. Philipp J., W. trilobata (L.) Hitchc. and Eclipta prostrata (L.) (Asteraceae) were collected and botanically identified. Preliminary phytochem. anal. and high-performance thin-layer chromatog. finger printing with marker wedelolactone were done for the ethanolic extracts of these plants. Using ADMET SAR software, the pharmacokinetics of wedelolactone were predicted. Using Autodock 4.2 software, the binding energy of wedelolactone on targets of acetaminophen-induced hepatotoxicity namely PPAR-α, AMPK, JNK-1, EGFR, Nrf2, ALT, ALP, GGT, CAR, Frizzled receptor, FXR, ERK1, LXR, mitochondrial glutamate dehydrogenase, p53, mTOR C1, CYP1A2, CYP2E1, 5-lipoxygenase, thrombin, UCP1, GSK1, RXR and PXR was predicted. All the three plant species were pharmacognostically and chem. different. W. chinensis was found to possess more antioxidant potential than the other two plants. Based on the above observations, we conclude that the presence of marker compound wedelolactone might have attributed the potency of W. chinensis and E. prostrata in counteracting acetaminophen toxicity when compared with W. trilobata. This study involved multiple reactions and reactants, such as 1,8,9-Trihydroxy-3-methoxy-6H-benzofuro[3,2-c]chromen-6-one (cas: 524-12-9Category: benzofurans).

1,8,9-Trihydroxy-3-methoxy-6H-benzofuro[3,2-c]chromen-6-one (cas: 524-12-9) belongs to benzofurans derivatives.Benzofuran is one of the most significant oxygen-containing heterocycles consisting of fused benzene and furan ring, which are widely presented in various naturally occurring and synthetically active compounds. As benzofurans are prone to undergo ring opening of the heterocycle, examples of reduction of this type of aromatics by using dissolving metals are rather scarce.Category: benzofurans

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Sclerotiorin stabilizes the assembly of nonfibrillar Abeta42 oligomers with low toxicity, seeding activity, and Beta-sheet content was written by Wiglenda, Thomas;Groenke, Nicole;Hoffmann, Waldemar;Manz, Christian;Diez, Lisa;Buntru, Alexander;Brusendorf, Lydia;Neuendorf, Nancy;Schnoegl, Sigrid;Haenig, Christian;Schmieder, Peter;Pagel, Kevin;Wanker, Erich E.. And the article was included in Journal of Molecular Biology in 2020.Synthetic Route of C16H10O7 The following contents are mentioned in the article:

The self-assembly of the 42-residue amyloid-β peptide, Aβ42, into fibrillar aggregates is associated with neuronal dysfunction and toxicity in Alzheimer’s disease (AD) patient brains, suggesting that small mols. acting on this process might interfere with pathogenesis. Here, we present exptl. evidence that the small mol. sclerotiorin (SCL), a natural product belonging to the group of azaphilones, potently delays both seeded and nonseeded Aβ42 polymerization in cell-free assays. Mechanistic biochem. studies revealed that the inhibitory effect of SCL on fibrillogenesis is caused by its ability to kinetically stabilize small Aβ42 oligomers. These structures exhibit low β-sheet content and do not possess seeding activity, indicating that SCL acts very early in the amyloid formation cascade before the assembly of seeding-competent, β-sheet-rich fibrillar aggregates. Investigations with NMR WaterLOGSY experiments confirmed the association of Aβ42 assemblies with SCL in solution Furthermore, using ion mobility-mass spectrometry, we observed that SCL directly interacts with a small fraction of Aβ42 monomers in the gas phase. In comparison to typical amyloid fibrils, small SCL-stabilized Aβ42 assemblies are inefficiently taken up into mammalian cells and have low toxicity in cell-based assays. Overall, these mechanistic studies support a pathol. role of stable, β-sheet-rich Aβ42 fibrils in AD, while structures with low β-sheet content may be less relevant. This study involved multiple reactions and reactants, such as 1,8,9-Trihydroxy-3-methoxy-6H-benzofuro[3,2-c]chromen-6-one (cas: 524-12-9Synthetic Route of C16H10O7).

1,8,9-Trihydroxy-3-methoxy-6H-benzofuro[3,2-c]chromen-6-one (cas: 524-12-9) belongs to benzofurans derivatives. Benzofuran derivatives are one of the most important oxygen-containing heterocycles. Introduction of benzofurans in organic synthesis, particularly drug synthesis, involves generally the use of their metalated species as nucleophiles in addition reactions or in metal-catalysed cross-coupling reactions.Synthetic Route of C16H10O7

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Epigallocatechin-3-Gallate Attenuates Microglial Inflammation and Neurotoxicity by Suppressing the Activation of Canonical and Noncanonical Inflammasome via TLR4/NF-kappaB Pathway was written by Zhong, Xin;Liu, Mingyan;Yao, Weifan;Du, Ke;He, Miao;Jin, Xin;Jiao, Linchi;Ma, Guowei;Wei, Binbin;Wei, Minjie. And the article was included in Molecular Nutrition & Food Research in 2019.Electric Literature of C16H10O7 The following contents are mentioned in the article:

Scope : In this study, it has been investigated whether the neuroprotective efficacy of epigallocatechin-3-gallate (EGCG) is mediated by inhibition of canonical and noncanonical inflammasome activation via toll-like receptor 4 (TLR4)/NF-kappaB pathway both in LPS+Abeta-induced microglia in vitro and in APP/PS1 mice in vivo. Methods and results : In BV2 cells, EGCG inhibits the expressions of Iba-1, cleaved IL-1beta, and cleaved IL-18 induced by LPS+Abeta. Subsequently, it has been found that EGCG reduces the microglial expressions of caspase-1 p20, NLRP3, and caspase-11 p26. Furthermore, the expression levels of Toll-like receptor 4 (TLR4), p-IKK/IKK, and p-NF-kappaB/NF-kappaB were decreased after EGCG treatment. As expected, when a caspase-1 specific inhibitor Z-YVAD-FMK, and an IKK and caspase-11 inhibitor wedelolactone are used for blocking, Z-YVAD-FMK and wedelolactone exacerbate the inhibitory efficacy than using EGCG alone. Finally, consistent with the results obtained in BV2 cells, EGCG treatment reduces microglial inflammation and neurotoxicity by suppressing the activation of canonical NLRP3 and noncanonical caspase-11-dependent inflammasome via TLR4/NF-kappaB pathway in LPS+Abeta-induced rat primary microglia and hippocampus of APP/PS1 mice. Conclusion : EGCG attenuates microglial inflammation and neurotoxicity by inhibition of canonical NLRP3 and noncanonical caspase-11-dependent inflammasome activation via TLR4/NF-kappaB pathway. This study involved multiple reactions and reactants, such as 1,8,9-Trihydroxy-3-methoxy-6H-benzofuro[3,2-c]chromen-6-one (cas: 524-12-9Electric Literature of C16H10O7).

1,8,9-Trihydroxy-3-methoxy-6H-benzofuro[3,2-c]chromen-6-one (cas: 524-12-9) belongs to benzofurans derivatives. Benzofuran is the “”parent”” of many related compounds with more complex structures. For example, psoralen is a benzofuran derivative that occurs in several plants. In nature, benzofurans have occupied an important role among the plant phenols & several pharmacologically active compounds.Electric Literature of C16H10O7

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

In vitro tetraploidization for the augmentation of wedelolactone in Sphagneticola calendulacea (L.) Pruski was written by Kundu, Suprabuddha;Salma, Umme;Ali, Nasim Md.;Mandal, Nirmal. And the article was included in Acta Physiologiae Plantarum in 2018.Related Products of 524-12-9 The following contents are mentioned in the article:

A practical and reliable method for in vitro tetraploidization of Sphagneticola calendulacea (L.) Pruski [synonym Wedelia chinensis (Osbeck) Merrill] has been established to enhance the production of wedelolactone. Shoot tip and nodal explants from in vitro-grown culture (2n = 50) were exposed to the antimitotic chem., i.e., colchicine, at various concentrations (0, 0.025, 0.05, 0.1, 0.3, and 0.5%; w/v) for 12, 24, 36, 48, and 60 h. The treated explants were then incubated and proliferated on Murashige and Skoog (MS) medium fortified with 0.2 mg l^-1 thidiazuron and 0.05 mg l^-1 naphthalene acetic acid, followed by root induction in 1.0 mg l^-1 indole-3 acetic acid enriched 1/2MS medium. Treatment of shoot tips with 0.05% colchicine for 24 h supported the maximum rate of survival (63.33%) of explants as well as tetraploid induction (42.93%). Morphol., stomatal, and cytol. characteristics along with the secondary metabolite content of the in vitro tetraploids were compared to that of diploids. The recovered tetraploid plants possessed superior plant height, stem diameter, leaf size, root number, and increased length and width of stomata but decreased stomatal frequency. The tetraploid plants demonstrated twice the chromosome number (2n = 4x = 100) than the diploids as confirmed through cytol., spectrophotometry and flow cytometry. High-performance thin-layer chromatog. showed a significant enhancement in the wedelolactone content of tetraploid plants (541.48μg g^-1 of dried sample) in comparison to diploid plants (325.43μg g^-1 of dried sample), signifying the prospective of this technique for the trade value improvement. This study involved multiple reactions and reactants, such as 1,8,9-Trihydroxy-3-methoxy-6H-benzofuro[3,2-c]chromen-6-one (cas: 524-12-9Related Products of 524-12-9).

1,8,9-Trihydroxy-3-methoxy-6H-benzofuro[3,2-c]chromen-6-one (cas: 524-12-9) belongs to benzofurans derivatives. Benzofuran is the “”parent”” of many related compounds with more complex structures. For example, psoralen is a benzofuran derivative that occurs in several plants. They are also prone to polymerisation in the presence of concentrated mineral acids and Lewis acids.Related Products of 524-12-9

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

UPLC-MS/MS Assay for Quantification of Wedelolactone and Demethylwedelolactone in Rat Plasma and the Application to a Preclinical Pharmacokinetic Study. was written by Wang, Bao-E;Zhang, Lin-Tao;Yang, Sheng-Bao;Xu, Zeng-Liang. And the article was included in Combinatorial chemistry & high throughput screening in 2022.SDS of cas: 524-12-9 The following contents are mentioned in the article:

AIMS AND OBJECTIVE: Wedelolactone and demethylwedelolactone are the two major coumarin constituents of Herba Ecliptae. The objective of this work was to develop and validate a sensitive, rapid, and robust UPLC-MS/MS method for the simultaneous quantification of wedelolactone and demethylwedelolactone in rat plasma. MATERIALS AND METHODS: Wedelolactone and demethylwedelolactone were extracted from rat plasma by protein precipitation with acetonitrile. Electrospray ionization in negative mode and selected reaction monitoring (SRM) were used for wedelolactone and demethylwedelolactone at the transitions m/z 312.8â†?98.0 and m/z 299.1â†?70.6, respectively. Chromatographic separation was conducted on a Venusil C₁₈ column (50 mm × 2.1 mm, 5 μm) with isocratic elution of acetonitrile-0.1% formic acid in water (55:45, v/v) at a flow rate of 0.3 mL/min. A linear range was observed over the concentration range of 0.25-100 ng/mL for wedelolactone and demethylwedelolactone. RESULTS: They reached their maximum plasma concentrations (C_max, 74.9±13.4 ng/mL for wedelolactone and 41.3±9.57 ng/mL for demethylwedelolactone) at the peak time (T_max) of 0.633 h and 0.800 h, respectively. The AUC_0-t value of wedelolactone (260.8±141.8 ng h/mL) was higher than that of demethylwedelolactone (127.4±52.7 ng h/mL) by approximately 2-fold, whereas the terminal elimination half-life (t_1/2) of wedelolactone (2.20±0.59 h) showed the approximately same as that of demethylwedelolactone (2.08±0.69 h). CONCLUSION: Based on full validation according to US FDA guidelines, this UPLC-MS/MS method was successfully applied to a pharmacokinetic study in rats. This study involved multiple reactions and reactants, such as 1,8,9-Trihydroxy-3-methoxy-6H-benzofuro[3,2-c]chromen-6-one (cas: 524-12-9SDS of cas: 524-12-9).

1,8,9-Trihydroxy-3-methoxy-6H-benzofuro[3,2-c]chromen-6-one (cas: 524-12-9) belongs to benzofurans derivatives. Benzofuran derivatives have shown many biological activities, including antifungal and antimicrobial properties, and acting as antagonists of H3 receptors and angiotensin II. Substituted benzofurans find applications such as fluorescent sensors, oxidants, in drug discovery, and in another field of chemistry and agriculture.SDS of cas: 524-12-9

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Wedelolactone alleviates acute pancreatitis and associated lung injury via GPX4 mediated suppression of pyroptosis and ferroptosis was written by Fan, Rong;Sui, Jidong;Dong, Xuepeng;Jing, Biao;Gao, Zhenming. And the article was included in Free Radical Biology & Medicine in 2021.Application In Synthesis of 1,8,9-Trihydroxy-3-methoxy-6H-benzofuro[3,2-c]chromen-6-one The following contents are mentioned in the article:

Acute pancreatitis (AP) is an inflammatory disorder associated with multiple organ failure. Pyroptosis and ferroptosis are two newly recognized cell death, and whether pyroptosis and ferroptosis are involved in AP remain largely elusive. The nature compound Wedelolactone (Wed) exhibits strong anti-inflammatory and antioxidant activities, the present study aims to investigate the effect of Wed on AP and unravel whether Wed could protect against AP and relevant lung injury against pyroptosis and ferroptosis. Our results showed that the pyroptosis inhibitor disulfiram or ferroptosis inhibitor ferrostatin-1 significantly alleviated AP and associated lung injury in the taurocholate or caerulein-induced murine AP model. Administration with Wed ameliorated AP and lung injury as evidenced by improved pathol. injuries, reduced serum pancreatic digestive enzymes, and proinflammatory cytokines. The in vivo and in vitro data demonstrated that Wed broadly inhibited caspase1/caspase11 activation, reduced mature interleukin-1β (IL-1β) and N-terminal domain of gasdermin D (GSDMD-N) level. The oxidative stress and lipid peroxidation were also suppressed along with the up-regulation of the ferroptosis antagonism marker glutathione peroxidase-4 (GPX4) in Wed treatment group. Wed promoted the transcriptional activity and the selenium sensitivity of GPX4. Moreover, the protective effects of Wed in caerulein-stimulated pancreatic acinar cells were markedly abrogated by the down-regulation of GPX4. Collectively, our data suggest that pyroptosis and ferroptosis play crucial roles in AP. Wed mitigated AP and associated lung injury via GPX4 mediated suppression of pyroptosis and ferroptosis. This study involved multiple reactions and reactants, such as 1,8,9-Trihydroxy-3-methoxy-6H-benzofuro[3,2-c]chromen-6-one (cas: 524-12-9Application In Synthesis of 1,8,9-Trihydroxy-3-methoxy-6H-benzofuro[3,2-c]chromen-6-one).

1,8,9-Trihydroxy-3-methoxy-6H-benzofuro[3,2-c]chromen-6-one (cas: 524-12-9) belongs to benzofurans derivatives.Benzofuran is one of the most significant oxygen-containing heterocycles consisting of fused benzene and furan ring, which are widely presented in various naturally occurring and synthetically active compounds. They are also prone to polymerisation in the presence of concentrated mineral acids and Lewis acids.Application In Synthesis of 1,8,9-Trihydroxy-3-methoxy-6H-benzofuro[3,2-c]chromen-6-one

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Anti-cancer effects of wedelolactone: interactions with copper and subcellular localization was written by Kucirkova, Tereza;Stiborek, Marek;Ducka, Monika;Navratilova, Jarmila;Bogdanovic Pristov, Jelena;Popovic-Bijelic, Ana;Vojvodic, Snezana;Preisler, Jan;Kanicky, Viktor;Smarda, Jan;Spasojevic, Ivan;Benes, Petr. And the article was included in Metallomics in 2018.Application of 524-12-9 The following contents are mentioned in the article:

Wedelactone (WL), a plant polyphenolic derivative of coumestan, represents a promising anti-cancer agent. The underlying mechanisms of its action are not fully understood and appear to involve interplay with copper ions. This study examined coordination and redox interactions of WL with Cu²⁺ in phosphate buffer (pH 7), and in two breast cancer cell lines. EPR, UV-Vis and fluorescence spectroscopy showed that WL and Cu²⁺ build a coordination complex with 2 : 1 stoichiometry and distorted tetrahedral geometry. WL showed strong fluorescence that was quenched by Cu²⁺. The sequestration of the intracellular copper pool with neocuproine led to a significant drop in the cytotoxic effects of WL, whereas the co-application of Cu²⁺ and WL and the formation of an extracellular complex suppressed both the cytotoxic effects of WL and copper loading. Fluorescence microscopy showed that WL is mainly localized in the cytosol and significantly less in the nuclei. WL fluorescence was stronger in cells pretreated with neocuproine, implying that the complex of WL and Cu²⁺ is formed inside the cells. WL caused a two-fold increase in the lysosomal level of copper as well as copper-dependent lysosome membrane permeabilization. On the other hand, the protective effects of overexpression of thioredoxin 1 imply that WL exerts the main oxidative impact inside the nucleus. The interactions of WL with copper may be essential for therapeutic performance and selectivity against cancer cells, taking into account that a number of cancer types, including breast cancer, exhibit increased intratumoral copper levels or altered copper distribution. This study involved multiple reactions and reactants, such as 1,8,9-Trihydroxy-3-methoxy-6H-benzofuro[3,2-c]chromen-6-one (cas: 524-12-9Application of 524-12-9).

1,8,9-Trihydroxy-3-methoxy-6H-benzofuro[3,2-c]chromen-6-one (cas: 524-12-9) belongs to benzofurans derivatives. Benzofuran derivatives have shown many biological activities, including antifungal and antimicrobial properties, and acting as antagonists of H3 receptors and angiotensin II. Benzofurans are stable towards alkali and readily polymerize on treatment with sulfuric acid, due to which they are useful for the preparation of low cost chemically relatively inert resins.Application of 524-12-9

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem