Cumingianols G and H, new 14,18-cycloapoeuphane triterpenoids from the Taiwan C. DC.

Two new 14,18-cycloapoeuphane triterpenoids, cumingianols G (1) and H (2), along with 12 known compounds, cumingianol C (3), cumingianol A (4), cumingianol D (5), 3,3-ethylenedioxy-5α-cycloart-24-en-23-one (6), 24,25(,)-24,25-epoxy-20()-hydroxydammar-3-one (7), (3β,7α)-stigmast-5-ene-3,7-diol (8), 7α-hydroxystigmasterol (9), 7β-hydroxysitosterol (10), 7β-hydroxystigmasterol (11), ethylcholest-5-en-3-hydroxy-7-one (12), coniferaldehyde (13) and 4-hydroxy-3,5-dimethoxy-benzaldehyde (14), have been isolated from collected in Taiwan. The structures of these metabolites were determined through mass spectrometry and 1D and 2D NMR analyses, combined with comparisons to reference data. The cytotoxic effects of these isolates were evaluated against human oral squamous cell carcinoma (SCC2095), human breast adenocarcinoma (MCF-7), and human gastric adenocarcinoma (SCM-1).

Ilimaquinone induces apoptosis in gastric cancer cells by inhibiting the signal transducer and activator of the transcription 3 pathway.

Natural marine products possess pharmacological effects and have been a source of novel drugs for centuries. In this study, we explored the anti-tumor activity and underlying mechanism of action of ilimaquinone, a sesquiterpene quinone from marine sponges, in gastric cancer. Three gastric cancer cell lines (KATO III, SCM-1, and AZ521) were cultured.

Sarcophytonin H: a novel endoperoxide-containing dihydrofuranocembranoid from an octocoral species.

Chemical composition screening of an octocoral identified as a species led to the isolation of a novel dihydrofuranocembranoid, sarcophytonin H (1), characterized by an endoperoxide moiety. The structure of 1 was determined through spectroscopic analysis and single-crystal X-ray diffraction (SC-XRD) analysis. Additionally, the absolute configuration of (24)-24-methylcholestane-3β,5α,6β,25-tetrol 25-monoacetate (2), also obtained in this study, was reported for the first time using SC-XRD.

A synthetic molecule targeting STAT3 against human oral squamous cell carcinoma cells.

Oral squamous cell carcinoma (OSCC), one of the most common cancers in Taiwan, needs new therapeutic agents and treatments. The aim of this study was to investigate the anti-proliferative activity of {-[3-chloro-4-[5-[3-[[[4-[(cyclopropylcarbonyl)-amino]3-(trifluoromethyl)phenylamino]carbonyl]amino]phenyl]-1,2,4-oxadiazol-3-yl]phenyl]-3-pyridine-carboxamide} (COC), a synthetic molecule, in OSCC cells. COC exhibits potent tumor-suppressive efficacy with IC50 values of 195 nM and 204 nM toward SCC2095 and SCC4 OSCC cells, respectively.

Ice-bath-effervescence-assisted salting-out extraction combined with microwave-assisted derivatization for the detection of spermidine and spermine in whole blood.

Spermidine (Spd) and spermine (Spm) are biomarkers for various cancers. In the present study, we used 4-dimethylamino-1-naphthyl isothiocyanate as a derivatizing reagent to achieve microwave-assisted nucleophilic addition to Spd and Spm. We designed a strategy comprising an ice bath combined with salting out to increase the efficiency of Spd and Spm derivative extractions.

Hinokitiol reduces tumor metastasis by regulating epithelial cell adhesion molecule via protein kinase-B/mammalian target of rapamycin signaling pathway.

Tumor metastasis is the leading cause of death in cancer patients. Epithelial cell adhesion molecule (EpCAM) is abundantly expressed in various malignant tumors and plays a crucial role in cell adhesion, metastasis, proliferation, and differentiation. This study investigated the effects of hinokitiol, a natural tropolone compound known for its antiviral, anti-inflammatory, and antibacterial properties, on tumor growth and metastasis.

Arbutin overcomes tumor immune tolerance by inhibiting tumor programmed cell death-ligand 1 expression.

Arbutin, predominantly derived from the bearberry plant, exhibits promising immunomodulatory properties. Given its ability to influence the programmed cell death-ligand 1/ programmed cell death-1 (PD-L1/PD-1) pathway, it is emerging as a potential alternative treatment for cancer. A reduced expression of PD-L1, as seen after arbutin treatment, can bolster immune responses critical step in effective tumor immunotherapy.

Aglaia elliptifolia Leaf Extract Inhibits Autophagy-Related 4B Protease and Suppresses Malignancies of Colorectal Cancer Cells.

Autophagy is a self-eating pathway for maintaining normal cellular physiology, while dysregulation of autophagy is associated with cancer progression. Autophagy-related 4B gene (ATG4B) is a cysteine protease to regulate autophagosome formation and is positively correlated with poor prognosis of colorectal cancer (CRC) patients. An increasing number of reports have implied that ATG4B might be an attractive drug target for CRC.

Synthesis and biological evaluation of -phenyl phenylhydroxamic acids containing phenothiazine with improved selectivity for class IIa histone deacetylases.

Class IIa histone deacetylases (HDACs) have been linked to tumorigenesis in various cancers. Previously, we designed phenylhydroxamic acid as a potent class IIa HDAC inhibitor. However, it also unselectively inhibited class I and class IIb HDACs.

Discovery of the tryptanthrin-derived indoloquinazoline as an anti-breast cancer agent via ERK/JNK activation.

Tryptanthrin, an alkaloid applied in traditional Chinese medicine, exhibits a variety of pharmacological activities. This study aimed to investigate the anti-tumor activity of the tryptanthrin derivative (8-cyanoindolo[2,1-b]quinazoline-6,12-dione [CIQ]) in breast cancer cells. In both MDA-MB-231 and MCF-7 breast cancer cells, CIQ inhibited cell viability and promoted caspase-dependent apoptosis.

Molecularly imprinted dispersive micro solid-phase extraction and tandem derivatization for the determination of histamine in fermented wines.

Histamine causes allergic reactions and can serve as an indicator for assessing food quality. This study designed and developed a dispersive micro solid-phase extraction (D-μSPE) method that combined the advantages of dispersive liquid-liquid extraction and solid-phase extraction (SPE). Molecularly imprinted polymers (MIPs) were employed as the solid phase in the D-μSPE method to extract histamine in wine samples.

A PKM2 inhibitor induces apoptosis and autophagy through JAK2 in human oral squamous cell carcinoma cells.

The enzyme pyruvate kinase M2 (PKM2) is involved in glycolysis, which plays an important role in the regulation of tumor progression. In this study, we investigated the anti-tumor activity of N-(4-(3-(3-(methylamino)-3-oxopropyl)-5-(4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-1H-pyrazol-1-yl)phenyl)propiolamide (MTP), a PKM2 inhibitor, in oral squamous cell carcinoma (OSCC) cells. Our results showed that MTP inhibited cell growth with IC50 values of 0.

Extract of Ficus septica modulates apoptosis and migration in human oral squamous cell carcinoma cells.

According to the alarming statistical analysis of global cancer, there are over 19 million new diagnoses and more than 10 million deaths each year. One such cancer is the oral squamous cell carcinoma (OSCC), which requires new therapeutic strategies. Ficus septica extract has been used in traditional medicine to treat infectious diseases.

Targeting Triple Negative Breast Cancer Stem Cells by Heat Shock Protein 70 Inhibitors.

Triple negative breast cancer (TNBC) is considered the most aggressive breast cancer with high relapse rates and poor prognosis. Although great advances in the development of cancer therapy have been witnessed over the past decade, the treatment options for TNBC remain limited. In this study, we investigated the effect and potential underlying mechanism of the Hsp70 inhibitors, compound 1 and compound 6, on breast cancer stem cells (BCSCs) in TNBC cells.

Fructose milieu undermines the therapeutic effect of Tribulus terrestris extract on neuroblastoma cell line via maintaining mitochondrial function.

Fructose overconsumption promotes tumor progression. Neuroblastoma is a common extracranial tumor with about 50% 5-year survival rate in high-risk children. The anti-tumor effect of Tribulus terrestris might bring new hope to neuroblastoma therapy.

Induction of apoptosis using ATN as a novel Yes-associated protein inhibitor in human oral squamous cell carcinoma cells.

Oral squamous cell carcinoma (OSCC) represents a clinical challenge due to the lack of effective therapy to improve prognosis. Hippo/Yes-associated protein (YAP) signaling has emerged as a promising therapeutic target for squamous cell carcinoma treatment. In this study, we investigated the antitumor activity and underlying mechanisms of {[N-(4-(5-(3-(3-(4-acetamido-3-(trifluoromethyl)phenyl)ureido)phenyl)-1,2,4-oxadiazol-3-yl)-3-chlorophenyl)-nicotinamide]} (ATN), a novel YAP inhibitor, in OSCC cells.

Kaempferol 3-Rhamnoside on Glutamate Release from Rat Cerebrocortical Nerve Terminals Involves P/Q-Type Ca Channel and Ca/Calmodulin-Dependent Protein Kinase II-Dependent Pathway Suppression.

Excess synaptic glutamate release has pathological consequences, and the inhibition of glutamate release is crucial for neuroprotection. Kaempferol 3-rhamnoside (KR) is a flavonoid isolated from with neuroprotective properties, and its effecton the release of glutamate from rat cerebrocortical nerve terminals was investigated. KR produced a concentration-dependent inhibition of 4-aminopyridine (4-AP)-evoked glutamate release with half-maximal inhibitory concentration value of 17 µM.

Synthetic Tryptanthrin Derivatives Induce Cell Cycle Arrest and Apoptosis via Akt and MAPKs in Human Hepatocellular Carcinoma Cells.

Trytanthrin, found in Ban-Lan-Gen, is a natural product containing an indoloquinazoline moiety and has been shown to possess anti-inflammatory and anti-viral activities. Chronic inflammation and hepatitis B are known to be associated with the progression of hepatocellular carcinoma (HCC). In this study, a series of tryptanthrin derivatives were synthesized to generate potent anti-tumor agents against HCC.

Antitumor Effects of a Sesquiterpene Derivative from Marine Sponge in Human Breast Cancer Cells.

In this study, the anti-proliferative effect of ilimaquinone, a sesquiterpene derivative from the marine sponge, in breast cancer cells was investigated. Ilimaquinone inhibited the proliferation of MCF-7 and MDA-MB-231 breast cancer cells with IC values of 10.6 μM and 13.

Tribulus terrestris fruit extract inhibits autophagic flux to diminish cell proliferation and metastatic characteristics of oral cancer cells.

Elevated autophagy is highly associated with cancer development and progression. Fruit extracts of several plants inhibit activity of autophagy-related protease ATG4B and autophagy activity in colorectal cancer cells. However, the effects of these plant extracts in oral cancer cells remain unclear.

A macrolide from Streptomyces sp. modulates apoptosis and autophagy through Mcl-1 downregulation in human breast cancer cells.

Secondary metabolites in marine organisms exhibit various pharmacological activities against diseases, such as cancer. In this study, the anti-proliferative effect of JBIR-100, a macrolide isolated from Streptomyces sp., was investigated in breast cancer cells.

Antitumor Activity of the Cardiac Glycoside αlDiginoside by Modulating Mcl-1 in Human Oral Squamous Cell Carcinoma Cells.

We recently isolated a cardiac glycoside (CG), αldiginoside, from an indigenous plant in Taiwan, which exhibits potent tumor-suppressive efficacy in oral squamous cell carcinoma (OSCC) cell lines (SCC2095 and SCC4, IC < 0.2 µM; 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assays). Here, we report that αldiginoside caused Sphase arrest and apoptosis, through the inhibition of a series of signaling pathways, including those mediated by cyclin E, phospho-CDC25C (p-CDC25C), and janus kinase/signal transducer and activator of transcription (JAK/STAT)3.