Protective effect of total flavonoids of Engelhardia roxburghiana Wall. leaves against radiation-induced intestinal injury in mice and its mechanism.

Ethnopharmacological Relevance: Irradiation-induced intestinal injury (RIII) often occurs during radiotherapy in patients, which would result in abdominal pain, diarrhea, nausea, vomiting, and even death. Engelhardia roxburghiana Wall. leaves, a traditional Chinese herb, has unique anti-inflammatory, anti-tumor, antioxidant, and analgesic effects, is used to treat damp-heat diarrhea, hernia, and abdominal pain, and has the potential to protect against RIII.

Discovery of Natural Ursane-type SENP1 Inhibitors and the Platinum Resistance Reversal Activity Against Human Ovarian Cancer Cells: A Structure-Activity Relationship Study.

Platinum-resistant ovarian cancer is one of the most common and refractory gynecologic cancers around the world. The SENP1/JAK2 (small ubiquitin-like modifier-specific protease 1/Janus activating kinase 2) axis activation has been proposed as a critical mechanism in platinum-resistant ovarian cancer, and as such, SENP1 inhibitors become a feasible alternative to reverse platinum resistance. In this work, 29 commercially available natural ursane-type aglycones were tested for their SENP1 inhibitory activities, among which 12 aglycones showed IC activity at the concentration below 5 μM.

Ursolic Acid Derivative UA232 Promotes Tumor Cell Apoptosis by Inducing Endoplasmic Reticulum Stress and Lysosomal Dysfunction.

Due to increased drug and radiation tolerance, there is an urgent need to develop novel anticancer agents. In our previous study, we performed a series of structural modifications of ursolic acid (UA), a natural product of pentacyclic triterpenes, and found UA232, a derivative with stronger anti-tumor activity. experiments showed that UA232 inhibited proliferation, induced G/G arrest, and promoted apoptosis in human breast cancer and cervical cancer cells.

Targeted inhibition of acidic nucleoplasmic DNA-binding protein 1 enhances radiosensitivity of non-small cell lung cancer.

Acidic nucleoplasmic DNA binding protein 1 (AND-1, also known as WD repeat and HMG-box DNA-binding protein 1, WDHD1) plays an important role in DNA replication and repair, but the relationship between AND-1 and radiosensitivity is not well understood. This research explored the impact of AND-1 on the radiosensitivity of non-small cell lung cancer (NSCLC) for the first time. NSCLC cells were treated with AND-1 siRNA or a new AND-1 inhibitor, CH-3, and clonogenic survival assay was used to characterize cell radiosensitivity.

Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury.

Acute kidney injury (AKI) is associated with high morbidity and mortality. Cisplatin is a common chemotherapeutic, but its nephrotoxicity-driven AKI limits its clinical application. Currently, there are no specific and satisfactory therapies in the clinic for AKI.

Phosphate group functionalized magnetic metal-organic framework nanocomposite for highly efficient removal of U(VI) from aqueous solution.

The phosphate group functionalized metal-organic frameworks (MOFs) as the adsorbent for removal of U(VI) from aqueous solution still suffer from low adsorption efficiency, due to the low grafting rate of groups into the skeleton structure. Herein, a novel phosphate group functionalized metal-organic framework nanoparticles (denoted as FeO@SiO@UiO-66-TPP NPs) designed and prepared by the chelation between Zr and phytic acid, showing fast adsorption rate and outstanding selectivity in aqueous media including 10 coexisting ions. The FeO@SiO@UiO-66-TPP was properly characterized by TEM, FT-IR, BET, VSM and Zeta potential measurement.

Discovery and radiosensitization research of ursolic acid derivatives as SENP1 inhibitors.

SUMOylation and deSUMOylation plays an important role in DNA damage response and the formation of radiotherapy resistance. SENP1 is the main specific isopeptidase to catalyze deSUMOylation modification. Inhibiting SENP1 upregulates cancer cell radiosensitivity and it becomes a promising target for radiosensitization.

Correction to An Improved Synthesis of the Triethylene Glycol-Substituted 4-(-Methyl--Boc-Amino)Styrylpyridine.

[This corrects the article DOI: 10.1021/acsomega.0c01244.

An Improved Synthesis of the Triethylene Glycol-Substituted 4-(-Methyl--Boc-Amino)Styrylpyridine.

An improved five-step synthesis of triethylene glycol-substituted 4-(-methyl--Boc-amino)styrylpyridine () is described. Using cost-effective starting materials, the developed synthesis route was synthetic, efficient, and chromatographic purification-free. The key point of the work is the one-pot synthesis of -butyl methyl(4-vinylphenyl)carbamate through methylation and elimination in the NaH/THF system.

Ursolic acid derivative UA232 evokes apoptosis of lung cancer cells induced by endoplasmic reticulum stress.

Context: Ursolic acid (UA), a natural product, shows a broad spectrum of anticancer effects. However, the poor bioavailability and efficacy of UA limit its clinical application.

Objective: We developed novel analogues of UA with enhanced antitumor activities by the extensive chemical modification of UA.

Acetyl-CoA carboxylase (ACC) as a therapeutic target for metabolic syndrome and recent developments in ACC1/2 inhibitors.

: Acetyl-CoA Carboxylase (ACC) is an essential rate-limiting enzyme in fatty acid metabolism. For many years, ACC inhibitors have gained great attention for developing therapeutics for various human diseases including microbial infections, metabolic syndrome, obesity, diabetes, and cancer. : We present a comprehensive review and update of ACC inhibitors.

Design, synthesis and biological evaluation of novel 4-anilinoquinazoline derivatives as hypoxia-selective EGFR and VEGFR-2 dual inhibitors.

Tyrosine kinase inhibitors (TKIs) have achieved substantial clinical effects for cancer treatment while causing a number of adverse effects. Since hypoxia is an intrinsic difference between solid tumor and healthy tissues, one strategy to overcome the adverse effects of TKIs is to enhance the specificity of anti-tumor activity by selectively targeting hypoxic region of tumors. Herein, we designed and synthesized a series of novel 4-anilinoquinazoline derivatives by introducing 3-nitro-1,2,4-triazole group to the side chain of vandetanib with modification of aniline moiety.