Label-Free Detection of Programmed Death-Ligand 1 for Prognosis Using a Truncated Aptamer and SYBR Green I.

The rapid and accurate detection of programmed death-ligand 1 (PD-L1) expression is of great value in the diagnosis and treatment of tumors. ELISA-based traditional method is the gold standard for protein detection, but there are still some shortcomings, especially the antigen-antibody dependence, greatly increased the detection time and cost. This work constructed a label-free fluorescent probe for rapid and sensitive detection of PD-L1 using a truncated aptamer as recognition molecules and double-stranded DNA specific dyes (SYBR Green I) as signal units.

Targeting cholesterol metabolism in Cancer: From molecular mechanisms to therapeutic implications.

Cholesterol is an essential component of cell membranes and helps to maintain their structure and function. Abnormal cholesterol metabolism has been linked to the development and progression of tumors. Changes in cholesterol metabolism triggered by internal or external stimuli can promote tumor growth.

Unravelling the roles of Autophagy in OSCC: A renewed perspective from mechanisms to potential applications.

Oral squamous cell carcinoma (OSCC) is associated with a low survival rate and a high disability rate, making it a serious health burden, particularly in Southeast Asian countries. Therefore, improvements in the diagnosis, treatment, and prognosis prediction of OSCC are highly warranted. Autophagy has a significant impact on cancer development.

Taccalonolides: Structure, semi-synthesis, and biological activity.

Microtubules are the fundamental part of the cell cytoskeleton intimately involving in cell proliferation and are superb targets in clinical cancer therapy today. Microtubule stabilizers have become one of the effectively main agents in the last decades for the treatment of diverse cancers. Taccalonolides, the highly oxygenated pentacyclic steroids isolated from the genus of , are considered a class of novel microtubule-stabilizing agents.

Molecular-docking-guided design, palladium-catalyzed synthesis and anticancer activity of paclitaxel-benzoxazoles hybrids.

A series of new paclitaxel-benzoxazoles hybrids were designed based on both the molecular docking mode of beta-tubulin with paclitaxel derivatives (7a and 7g), and the activity-structure relationship of C-13 side chain in paclitaxel. Palladium-catalyzed direct Csp-H arylation of benzoxazoles with different aryl-bromides was used as the key synthetic strategy for the aryl-benzoxazoles moieties in the hybrids. Twenty-six newly synthesized hybrids were screened for their antiproliferative activity against human cancer cell lines such as human breast cancer cells (MDA-MB-231) and liver hepatocellular cells (HepG2) by the MTT assay and results were compared with paclitaxel.

Targeting Autophagy with Natural Compounds in Cancer: A Renewed Perspective from Molecular Mechanisms to Targeted Therapy.

Natural products are well-characterized to have pharmacological or biological activities that can be of therapeutic benefits for cancer therapy, which also provide an important source of inspiration for discovery of potential novel small-molecule drugs. In the past three decades, accumulating evidence has revealed that natural products can modulate a series of key autophagic signaling pathways and display therapeutic effects in different types of human cancers. In this review, we focus on summarizing some representative natural active compounds, mainly including curcumin, resveratrol, paclitaxel, Bufalin, and Ursolic acid that may ultimately trigger cancer cell death through the regulation of some key autophagic signaling pathways, such as RAS-RAF-MEK-ERK, PI3K-AKT-mTOR, AMPK, ULK1, Beclin-1, Atg5 and p53.

Targeting cancer epigenetic pathways with small-molecule compounds: Therapeutic efficacy and combination therapies.

Epigenetics mainly refers to covalent modifications to DNA or histones without affecting genomes, which ultimately lead to phenotypic changes in cells or organisms. Given the abundance of regulatory targets in epigenetic pathways and their pivotal roles in tumorigenesis and drug resistance, the development of epigenetic drugs holds a great promise for the current cancer therapy. However, lack of potent, selective, and clinically tractable small-molecule compounds makes the strategy to target cancer epigenetic pathways still challenging.

Lewis acid-mediated skeleton transformation of Euphorbia diterpenes: From lathyrane to euphoractane and myrsinane.

Natural euphoractane and myrsinane diterpene skeletons, together with an unnatural 5/7/7/4 fused-ring diterpene skeleton were furnished via BF·EtO-mediated transformation of lathyrane-type diterpene, Euphorbia factor L1. The skeleton transformation process was mainly involved in the cascade oxirane-opening (cyclopropane-opening)/oxe-Micheal addition reaction. The structures of three diterpenes were confirmed by comprehensive spectra analysis and single crystals X-ray diffraction.

Recent advances in microtubule-stabilizing agents.

Highly dynamic mitotic spindle microtubules are superb therapeutic targets for a group of chemically diverse and clinically successful anticancer drugs. Microtubule-targeted drugs disrupt microtubule dynamics in distinct ways, and they are primarily classified into two groups: microtubule destabilizing agents (MDAs), such as vinblastine, colchicine, and combretastatin-A4, and microtubule stabilizing agents (MSAs), such as paclitaxel and epothilones. Systematic discovery and development of new MSAs have been aided by extensive research on paclitaxel, yielding a large number of promising anticancer compounds.

Ultrasound-assisted extraction of total flavonoids from Aconitum gymnandrum.

Background: Aconitum gymnandrum is a Chinese traditional herb used as carminative and analgesic. In this study, A. gymnandrum was used as an experimental matrix.

1-Chloro-1H-1,2,3-benzotriazole.

The title compound, C6H4ClN3, is essentially planar, with a maximum deviation of 0.007 (3) Å. In the crystal, a short contact of 2.

8β-Acet-oxy-14α-benzo-yloxy-N-methyl-13β,15α-dihy-droxy-1α,6α,16β-trimeth-oxy-4β-(meth-oxy-meth-yl)aconitane: hypaconitine isolated from 'fuzi'.

The title compound, C(33)H(45)NO(10), has an aconitine carbon skeleton with four six-membered rings and two five-membered rings. The five-membered rings adopt envelope configurations and the six-membered N-containing heterocyclic ring displays a chair conformation. Two intra-molecular O-H⋯O hydrogen bonds occur.

[Perception and attitude of rural community to the construction of Asian elephant conservation corridors in Xishuangbanna].

By using contingent valuation method (CVM), an investigation was made from November 2007 to March 2008 on the perception and attitude of 196 households in 5 villages within 2 planned Asian elephant conservation corridors in Xishuangbanna to the construction of the corridors. 80.61% of the interviewees conditionally supported the corridors construction.

(25R)-5a-Spiro-stane-3,12-dione.

The title compound, C(27)H(40)O(4), was obtained from the oxidation of (25R)-3b-hydr-oxy-5a-spiro-stan-12-one (Hecogenin) by Jone's reagent. The mol-ecule contains six alicyclic and heterocyclic rings, all trans-fused, among which four six-membered rings adopt similar chair conformations while two five-membered rings assume an envelope conformation.

Synthesis and characterization of HPMC derivatives as novel duodenum-specific coating agents.

HPMC (Hydroxypropyl methylcellulose) was chemically modified, using maleic anhydrides, to obtain pH-sensitive HPMCAM (Hydroxypropyl methylcellulose acetate maleate) polymers for use as novel duodenum-specific coating agents. The pharmaceutical properties of HPMCAM, such as film forming, acid values, pH-sensitive values, water vapor permeability, tensile strength and Tg, were investigated, and found to show good film forming properties. The pH-sensitive values were 3.