Light δD apatites reveal deep origin water in North China Craton intracontinental granites and basalts.

Water is essential to the formation of intracontinental granites, but its origin remains elusive. Here we address this scientific problem by analyzing D/H isotopes of apatites, hydrous minerals in Jurassic and Early Cretaceous granites and basalts from eastern North China Craton, where water was previously interpreted as derived from subducting slab. Results reveal extremely low δD values in pristine Early Cretaceous granitic (-203‰ to -127‰) and basaltic (-197‰ to -107‰) apatites, contrasting with relatively high δD values (-137‰ to -47‰) in Jurassic granites.

Synthesis and clinical application of representative small-molecule dipeptidyl Peptidase-4 (DPP-4) inhibitors for the treatment of type 2 diabetes mellitus (T2DM).

Diabetes mellitus is a chronic metabolic disorder characterized by high blood glucose levels, which can cause many diseases, including osteoporosis, fractures, arthritis, and foot complications. The inhibitors of dipeptidyl peptidase-4 (DPP-4), an enzyme involved in glucose metabolism regulation, are essential for managing Type 2 Diabetes Mellitus (T2DM). The inhibition of DPP-4 has become a promising treatment approach for T2DM because it can increase levels of active glucagon-like peptide-1 (GLP-1), leading to improved insulin secretion in response to glucose and reduced release of glucagon.

Fluorine in the pharmaceutical industry: Synthetic approaches and application of clinically approved fluorine-enriched anti-infectious medications.

The strategic integration of fluorine atoms into anti-infectious agents has become a cornerstone in the field of medicinal chemistry, owing to the unique influence of fluorine on the chemical and biological properties of pharmaceuticals. This review examines the synthetic methodologies that enable the incorporation of fluorine into anti-infectious drugs, and the resultant clinical applications of these fluorine-enriched compounds. With a focus on clinically approved medications, the discussion extends to the molecular mechanisms.

Synthetic Routes and Clinical Application of Representative Small-Molecule EGFR Inhibitors for Cancer Therapy.

The epidermal growth factor receptor (EGFR) plays a pivotal role in cancer therapeutics, with small-molecule EGFR inhibitors emerging as significant agents in combating this disease. This review explores the synthesis and clinical utilization of EGFR inhibitors, starting with the indispensable role of EGFR in oncogenesis and emphasizing the intricate molecular aspects of the EGFR-signaling pathway. It subsequently provides information on the structural characteristics of representative small-molecule EGFR inhibitors in the clinic.

A comprehensive review of small-molecule drugs for the treatment of type 2 diabetes mellitus: Synthetic approaches and clinical applications.

Type 2 diabetes mellitus (T2DM) is a long-term metabolic disorder characterized by the body's resistance to insulin and inadequate production of insulin. Small molecule drugs to treat T2DM mainly control blood sugar levels by improving insulin sensitivity, increasing insulin secretion, or reducing liver glycogen production. With the deepening of research on the pathogenesis of diabetes, many drugs with new targets and mechanisms of action have been discovered.

Synthesis and clinical application of new drugs approved by FDA in 2023.

In 2023, the U.S. Food and Drug Administration (FDA) granted approval to a total of 55 new drugs, comprising 29 new chemical entities (NCEs) and 25 new biological entities (NBEs).

Britannin as a novel NLRP3 inhibitor, suppresses inflammasome activation in macrophages and alleviates NLRP3-related diseases in mice.

Overactivation of the NLRP3 inflammasomes induces production of pro-inflammatory cytokines and drives pathological processes. Pharmacological inhibition of NLRP3 is an explicit strategy for the treatment of inflammatory diseases. Thus far no drug specifically targeting NLRP3 has been approved by the FDA for clinical use.

Harmonizing the craft of crafting clinically endorsed small-molecule BCR-ABL tyrosine kinase inhibitors for the treatment of hematological malignancies.

The advancement and practical use of small-molecule tyrosine kinase inhibitors (TKIs) that specifically target the BCR-ABL fusion protein have introduced a revolutionary era of precision medicine for the treatment of chronic myeloid leukemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL). This review offers a comprehensive exploration of the synthesis, mechanisms of action, and clinical implementation of clinically validated TKIs in the context of BCR-ABL, emphasizing the remarkable strides made in achieving therapeutic precision. We delve into the intricate design and synthesis of these small molecules, highlighting the synthetic strategies and modifications that have led to increased selectivity, enhanced binding affinities, and reduced off-target effects.

Synthesis and application of small molecules approved for the treatment of lymphoma.

Lymphoma is a form of cancer that impacts the lymphatic system, which plays a crucial role in defending the body against infections and illnesses. It is characterized by the atypical proliferation of lymphocytes, a type of white blood cell, which can form tumors in the lymph nodes, bone marrow, spleen, etc. Lymphoma is usually treated using a combination of targeted therapy, chemotherapy, and radiation therapy.

Synthesis and clinical application of small-molecule inhibitors of Janus kinase.

Janus kinase (JAK) plays a crucial role in intracellular signaling pathways, particularly in cytokine-mediated signal transduction, making them attractive therapeutic targets for a wide range of diseases, including autoimmune disorders, myeloproliferative neoplasms, and inflammatory conditions. The review provides a comprehensive overview of the development and therapeutic potential of small-molecule inhibitors targeting JAK family of proteins in various clinical trials. It also discusses the mechanisms of action, specificity, and selectivity of these inhibitors, shedding light on the challenges associated with achieving target selectivity while minimizing off-target effects.

Pre- and post-operative comprehensive nursing care versus conventional nursing care: An evaluation of quality of life, postoperative pain, adverse effects, and treatment satisfaction of patients who underwent surgeries and interventional therapies for liver cancer.

Interventional therapies including chemotherapies and radiotherapies are the most preferred treatment for liver cancer. However, these therapies have adverse effects. Therefore, careful care is required to relieve these adverse effects.

Two new stilbene glucosides and a new benzoic acid derivative from .

Two new stilbene glucosides, -3,5-dihydroxy-4-methoxystilbene 3--D-glucopyranoside (), -3,5-dihydroxy-4-methoxystilbene 3--D-glucopyranoside (), one new benzoic acid derivative, -4-hydroxy-3-hydroxymethyl-2-butenyl benzoate 4--D-glucopyranoside (), and four known compounds () were isolated from L. The structures of these compounds were elucidated on the basis of spectral data. Anti-inflammatory effects of compounds () were evaluated in terms of inhibition on production of NO, TNF-α and IL-6 in LPS-induced RAW 264.

One novel naphthalene derivative and other constituents with anti-complementary activities from the aerial parts of .

One novel naphthalene derivative, 2-octa-2',4',6'-atriynenaphthalene (), together with eighteen known compounds (-) were isolated from the aerial parts of L. Compounds , , , , - and were obtained from the family Lamiaceae for the first time, and compounds and were firstly identified from the genus of . All the isolates were evaluated for anti-complementary activities through the classical and alternative pathways, and the targets of the most active compounds on the complement activation cascade were also investigated.

Synthesis, antitumor and antibacterial activities of cordycepin derivatives.

Twelve novel cordycepin derivatives were designed and synthesized with modification at positions of 2', 5'-hydroxyl and amino groups of cordycepin. The results showed that the inhibitory activities of , , and on A549 were comparable to the positive control gefitinib, and the inhibitory activity of on A549 was better than that of gefitinib. Also, the inhibitory activities of twelve cordycepin derivatives against 1924, 4220 and 3289 were studied.

Clinical effects and gut microbiota changes of using probiotics, prebiotics or synbiotics in inflammatory bowel disease: a systematic review and meta-analysis.

Purpose: Probiotics have been reported to be beneficial for inflammatory bowel disease (IBD), but the types, number of strains, dosage, and intervention time of probiotics used remain controversial. Furthermore, the changes of gut microbiota in IBD's patients are also intriguing. Thus, this meta-analysis was to explore the clinical effects and gut microbiota changes of using probiotics, prebiotics and synbiotics in IBD.

Two new phenolic glycosides from the fruits of .

Two new phenolic glycosides () and eleven known compounds () were isolated from the fruits of Hook.f. using silica-gel column and preparative middle pressure liquid chromatography (MPLC).

[Research on the association between per-capita tobacco consumption among the permanent residents and lung cancer mortality in Henan province].

Objective: To study the relationship of per-capita tobacco consumption and lung cancer mortality in Henan province, and to provide evidence for policy development on tobacco control and reduction of lung cancer mortality.

Methods: Data regarding lung cancer mortality and per-capita tobacco consumption among household residents from 1992 to 2011, was collected from published almanacs in Henan and Henan Tumor Institutes. Trend Method was used to analyze the development of lung cancer in Henan province and the trend of per-capita tobacco consumption of residents in the household.

Spectroscopic parameter and molecular constant investigations on low-lying states of BeF radical.

The potential energy curves (PECs) of X(2)∑(+), A(2)Π(r) and B(2)∑(+) states of BeF radical have been investigated using the complete active space self-consistent-field (CASSCF) method, followed by the highly accurate valence internally contracted multireference configuration interaction (MRCI) approach at the correlation-consistent basis sets, cc-pV5Z for Be and aug-cc-pV6Z for F. Based on the PECs of X(2)∑(+), A(2)Π(r) and B(2)∑(+) states, the spectroscopic parameters (D(e), R(e), ω(e), ω(e)χ(e), α(e) and B(e)) have also been determined in the present work. With the PECs determined at the present level of theory, vibrational states have been predicted for each state when the rotational quantum number J equals zero (J = 0).

A TD-DFT study on the hydrogen bonding of three esculetin complexes in electronically excited states: strengthening and weakening.

Time-dependent density functional theory (TD-DFT) method was used to study the excited-state hydrogen bonding of three esculetin complexes formed with aprotic solvents. The geometric structures, molecular orbitals (MOs), electronic spectra and the infrared (IR) spectra of the three doubly hydrogen-bonded complexes formed by esculetin and aprotic solvents dimethylsulfoxide (DMSO), tetrahyrofuran (THF) and acetonitrile (ACN) in both ground state S(0) and the first singlet excited state S(1) were calculated by the combined DFT and TD-DFT methods with the COSMO solvation model. Two intermolecular hydrogen bonds can be formed between esculetin and the aprotic solvent in each hydrogen-bonded complex.

[Correlation of the methylation status of CpG islands in the promoter region of 10 genes with the 5-Fu chemosensitivity in 3 breast cancer cell lines].

Objective: To explore the relationship between the methylation status of CpG islands in the promoter region of 10 genes in breast cancer cells and their sensitivity to 5-fluouracil (5-Fu), and to identify the genes responsible for the 5-Fu resistance in breast cancer.

Methods: Three cell lines (differently resistant to chemotherapy) were used in this study: Bcap-37 (IC(50): 289.77 microg/ml), T47D (IC(50): 134.

[Experimental study on anatomy of adjacent structures of the optic canal].

Objective: To provide microanatomical data for optic canal decompression surgery or paranasal sinus surgery through anatomical study on adjacent structures of the optic canal.

Methods: It was a experimental study. (1) Fifty dry cadaveric adult heads (100 sides) were dissected.