Therapeutic Targeting of PPARγ in Nonalcoholic Fatty Liver Disease: Efficacy, Safety, and Drug Development.

Non-alcoholic fatty liver disease (NAFLD) is a metabolic-associated liver disorder characterized by a multi-faceted pathological progression involving fat accumulation, oxidative stress, and inflammation. Peroxisome proliferator-activated receptor gamma (PPARγ), a key nuclear receptor involved in lipid metabolism, insulin sensitivity regulation, and immune modulation, plays a significant role in both the development and treatment of NAFLD. This review summarizes the physiological functions of PPARγ in tissues such as adipose tissue, pancreas, intestine, and liver.

New cardiac glycosides from Adonis amurensis with potent antitumor activity.

Twenty-four cardiac glycosides - including six previously undescribed compounds (1-6) and eighteen known analogues (7-24) - were isolated from the whole herb of Adonis amurensis. Their structures were elucidated through comprehensive spectroscopic analysis (1D/2D NMR, HRMS) and acid hydrolysis. All compounds exhibited potent in vitro cytotoxicity against diverse cancer cell lines, with IC₅₀ values ranging from 0.

Degradation of NLRP3 by selective ROCK2 inhibitor alleviates acute lung injury.

Acute lung injury (ALI), characterized by uncontrolled inflammatory responses, is a critical condition with limited clinical treatment options. Activation of the NLRP3 inflammasome represents a pivotal event in ALI pathogenesis. Although targeting NLRP3 (The NOD-like receptor (NLR) family member containing a pyrin domain 3) inflammasome has been considered to be a potential therapy, the underlying mechanism through which pathway the pulmonary inflammation is modulated remains controversial.

Oxymatrine for inflammatory bowel disease in preclinical studies: a systematic review and meta-analysis.

Background: Inflammatory Bowel Disease (IBD) is a chronic, idiopathic inflammatory disorder of the intestines. Oxymatrine (OMT) is a naturally active substance found in the desiccated roots of . It possesses anti-tumor, antiviral, and anti-inflammatory properties.

Biomimetic rhCOL17-P334 Conjugate for Enhanced Wound Healing.

Wound healing remains a significant global health challenge, affecting millions annually and imposing substantial economic burdens. Most commercially available biomaterials for wound management primarily address external symptoms, including hemostasis, exudation, scarring, and infection. Advanced biomaterials derived from endogenous molecules aim to better replicate the native wound microenvironment, promoting enhanced repair.

Discovery of the First-in-Class Dual-Target ROCK/HDAC Inhibitor with Potent Antitumor Efficacy in Vivo That Trigger Antitumor Immunity.

Triple-negative breast cancer (TNBC) represents a highly aggressive and heterogeneous malignancy. Currently, multitarget drug approaches present a promising therapeutic approach for TNBC. Utilizing a combinatorial chemistry strategy to construct a virtual screening database, dual ROCK/HDAC-targeting benzothiophene compounds were identified.

Natural Derivatives of Selective HDAC8 Inhibitors with Potent Antitumor Efficacy against Breast Cancer.

HDAC8 is a therapeutic target with great promise for breast cancer. Here, we reported a novel compound corallorazine D from sp. XZB108, selectively inhibited HDAC8 (IC = 0.

Bipyridine Derivatives as NOP2/Sun RNA Methyltransferase 3 Inhibitors for the Treatment of Colorectal Cancer.

Based on the structure of caerulomycin A, 90 novel bipyridine derivatives were designed and synthesized. Among these, compound exerted strong antitumor effects in vivo and in vitro. Importantly, NOP2/Sun RNA methyltransferase 3 (NSUN3) protein was identified as the target specific binding to , which inhibits oxidative phosphorylation of mitochondrial energy metabolism and enhances glycolytic activity by binding to NSUN3.

Resveratrol for inflammatory bowel disease in preclinical studies: a systematic review and meta-analysis.

Inflammatory bowel disease (IBD) is a chronic condition that can be managed with treatment, but it is challenging to get IBD cured. Resveratrol, a non-flavonoid polyphenolic organic compound derived from various plants, has a potential effect on IBD. The current research was set out to investigate the therapeutic effects of resveratrol on animal models of IBD.

Cancer‑associated fibroblasts under therapy‑induced senescence in the tumor microenvironment (Review).

Current cancer treatments target tumor cells; however, the tumor microenvironment (TME) induces therapeutic resistance, tumor development and metastasis, thus rendering these treatments ineffective. Research on the TME has therefore concentrated on nonmalignant cells. Cancer-associated fibroblasts (CAFs) are a major TME component, which contribute to cancer progression due to their diverse origins, phenotypes and functions, including cancer cell invasion and migration, extracellular matrix remodeling, tumor metabolism modulation and therapeutic resistance.

Design, Synthesis, and Biological Evaluation of an Orally Bioavailable, Potent, and Selective ROCK2 Inhibitor for Psoriasis Treatment.

Psoriasis, a prevalent chronic skin disorder, remains a significant therapeutic obstacle. This study centers on rho-associated coiled-coil-containing kinase2 (ROCK2) as an advantageous target for treating psoriasis and identifies five potent and selective ROCK2 inhibitors (-). Notably, - outperform KD025 in ROCK2/ROCK1 selectivity by up to 216-fold.

Patients' perspectives on irritable bowel syndrome: a qualitative analysis based on social media in China.

Aim: To explore the perspectives, experience, and concerns of patients with irritable bowel syndrome (IBS) in China.

Methods: We used data mining to investigate posts shared in Baidu Tieba concerned with IBS; we collected the data through the crawler code, and mined the cleaned data's themes based on Latent Dirichlet allocation (LDA) and the Grounded theory.

Results: We found 5746 network posts related to IBS.

Diallyl trisulfide alleviates chemotherapy sensitivity of ovarian cancer via the AMPK/SIRT1/PGC1α pathway.

Platinum-based chemotherapy promotes drug resistance in ovarian cancer. We investigated the antichemoresistance characteristics of diallyl trisulfide (DATS) in cisplatin-resistant ovarian cancer cells, in vitro and in vivo. Previous preclinical studies have revealed that DATS regulates distinct hallmark cancer-signaling pathways.

Co-Crystals of Resveratrol and Polydatin with L-Proline: Crystal Structures, Dissolution Properties, and In Vitro Cytotoxicities.

Resveratrol (RSV) and polydatin (PD) have been widely used to treat several chronic diseases, such as atherosclerosis, pulmonary fibrosis, and diabetes, among several others. However, their low solubility hinders their further applications. In this work, we show that the solubility of PD can be boosted via its co-crystallization with L-proline (L-Pro).

Anti-Autophagy Mechanism of Zhi Gan Prescription Based on Network Pharmacology in Nonalcoholic Steatohepatitis Rats.

Zhi Gan prescription (ZGP) has been clinically proven to exert a favorable therapeutic effect on nonalcoholic steatohepatitis (NASH). This study purpose to reveal the underlying molecular mechanisms of ZGP action in NASH. Systematic network pharmacology was used to identify bioactive components, potential targets, and the underlying mechanism of ZGP action in NASH.

On-grating graphene surface plasmons enabling spatial differentiation in the terahertz region.

We propose a graphene-on-grating nanostructure to enable second-order spatial differentiation computation in the terahertz (THz) region. The differentiation operation is based on the interference between the direct reflected field and the leakage of two excited surface plasmon polaritons counter-propagating along the graphene sheet. With the spatial coupled-mode theory, we derive that the requirement for the second-order spatial differentiation is the critical coupling condition.

Plasmonic computing of spatial differentiation.

Optical analog computing offers high-throughput low-power-consumption operation for specialized computational tasks. Traditionally, optical analog computing in the spatial domain uses a bulky system of lenses and filters. Recent developments in metamaterials enable the miniaturization of such computing elements down to a subwavelength scale.