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Three pairs of enantiomers and one achiral molecule that are new ethylated derivatives of sulfur and nitrogen-containing compounds named mantidisamides E–H (1–4), along with twenty known ones (5–24), were derived from the ethanol extract of Tenodera sinensis Saussure. The structures of these new compounds and their absolute configurations were assigned on the basis of spectroscopic analyses and computational methods. The assessment of activities in NRK-52e cells induced by TGF-β1 demonstrated that the previously undescribed compounds 1 and 2 exhibited a significant capacity to inhibit the expression of proteins (fibronectin, collagen I, and α-SMA). Moreover, the biological activity of these compounds was found to increase with rising concentrations. Notably, compounds 1–4 should be artifacts; however, undescribed compounds 1 and 2, which possessed obvious biological activity, might be attractive for chemists and biologists due to the potential for more detailed exploration of their properties. It is worth mentioning that compounds 1 and 2 remain novel structures even in the absence of the ethoxy group. [ABSTRACT FROM AUTHOR]

Background and Purpose: The mammalian target of rapamycin (mTOR) pathway plays critical roles in intrinsic chemoresistance by regulating Fanconi anaemia complementation group D2 (FANCD2) expression. However, the mechanisms by which mTOR regulates FANCD2 expression and related inhibitors are not clearly elucidated. Extracts of Centipeda minima (C. minima) showed promising chemosensitizing effects by inhibiting FANCD2 activity. Here, we have aimed to identify the bioactive chemosensitizer in C. minima extracts and elucidate its underlying mechanism. Experimental Approach: The chemosensitizing effects of arnicolide C (ArC), a bioactive compound in C. minima, on non‐small cell lung cancer (NSCLC) were investigated using immunoblotting, immunofluorescence, flow cytometry, the comet assay, small interfering RNA (siRNA) transfection and animal models. The online SynergyFinder software was used to determine the synergistic effects of ArC and chemotherapeutic drugs on NSCLC cells. Key Results: ArC had synergistic cytotoxic effects with DNA cross‐linking drugs such as cisplatin and mitomycin C in NSCLC cells. ArC treatment markedly decreased FANCD2 expression in NSCLC cells, thus attenuating cisplatin‐induced FANCD2 nuclear foci formation, leading to DNA damage and apoptosis. ArC inhibited the mTOR pathway and attenuated mTOR‐mediated expression of E2F1, a critical transcription factor of FANCD2. Co‐administration of ArC and cisplatin exerted synergistic anticancer effects in the A549 xenograft mouse model by suppressing mTOR/FANCD2 signalling in tumour tissues. Conclusion and Implications: ArC suppressed DNA cross‐linking drug‐induced DNA damage response by inhibiting the mTOR/E2F1/FANCD2 signalling axis, serving as a chemosensitizing agent. This provides insight into the anticancer mechanisms of ArC and offers a potential combinatorial anticancer therapeutic strategy. [ABSTRACT FROM AUTHOR]

Investigation on the chemical components of Valeriana jatamansi Jones (Caprifoliaceae), a new lignan with pyran-ring, dipsalignan G (1), along with eight known compounds (2–9) were isolated. Their structures were elucidated by extensive analysis of 1D, 2D NMR and HR-ESI-MS spectroscopic data. Additionally, possible biosynthetic pathway of 1 was proposed. Finally, biological evaluation results showed that 8 had significant scavenging ability to ABTS and DPPH free radicals, with IC50 values of 1.35 ± 0.01 and 2.94 ± 0.01 μg/ml, respectively. [ABSTRACT FROM AUTHOR]

Three new N -alkylated amino acid derivatives, penichrysoamides A-C (1 – 3), along with a new citric acid derivative, penichrysoacid A (4), a new chromanone lactone penichrysoacid B (5), and a new amide derivative, penichrysoamide D (6), as well as seven known benzamide derivatives (7 – 13), were isolated from the endophytic fungus Penicillium chrysogenum derived from the insect Periplaneta americana. The structures of these compounds, including their absolute configurations, were elucidated using spectroscopic and computational techniques. Biological evaluation revealed that compounds 8 – 13 exhibited significant COX-2 inhibitory activity, with IC 50 values ranging from 275 nM to 1350 nM. Three new N -alkylated amino acid derivatives, penichrysoamides A-C (1 – 3), along with a new citric acid derivative, penichrysoacid A (4), a new chromanone lactone penichrysoacid B (5), and a new amide derivative, penichrysoamide D (6), as well as seven known benzamide derivatives (7 – 13), were isolated from the endophytic fungus Penicillium chrysogenum derived from the insect Periplaneta americana. The structures of these compounds, including their absolute configurations, were elucidated using spectroscopic and computational techniques. Biological evaluation revealed that compounds 8 – 13 exhibited significant COX-2 inhibitory activity, with IC 50 values ranging from 275 nM to 1350 nM. [Display omitted] [ABSTRACT FROM AUTHOR]

Pinuskesiols A–F (1 – 6), six new structurally diverse abietane diterpenoids were isolated from Pinus yunnanensis resins. Their structures including absolute configurations were characterized by using spectroscopic and computational methods. All the compounds bear a carbonyl functionality at C-4 with 1 and 2 behaving as a lactone thereof. The isopropyl group is attached to C-13 via O -atom in 3. In addition, the presence of a Δ 5(6) double bond and a ketone at C-7 makes 2 a large conjugated system. Biological evaluation revealed that 1 , 2 , and 4 could concentration-dependently inhibit iNOS and COX-2 expression in lipopolysaccharide-induced RAW 264.7 cells with 2 to be the most active toward COX-2 inhibition. Pinuskesiols A–F (1 – 6), six new structurally diverse abietane diterpenoids were isolated from Pinus yunnanensis resins. Their structures including absolute configurations were characterized by using spectroscopic and computational methods. All the compounds bear a carbonyl functionality at C-4 with 1 and 2 behaving as a lactone thereof. The isopropyl group is attached to C-13 via O -atom in 3. In addition, the presence of a Δ 5(6) double bond and a ketone at C-7 makes 2 a large conjugated system. Biological evaluation revealed that 1 , 2 , and 4 could concentration-dependently inhibit iNOS and COX-2 expression in lipopolysaccharide-induced RAW 264.7 cells with 2 to be the most active toward COX-2 inhibition. [Display omitted] [ABSTRACT FROM AUTHOR]

Five new norneolignans sinkianlignans G-K (1 – 5), one phenolic compound ferulagenol A (6) and seven known compounds (7 – 13) were isolated from Ferula sinkiangensis. All the norneolignans were racemic mixtures, and chiral HPLC was used to further separate them. Their structures were assigned, including absolute configurations, using spectroscopic and computational methods. Biological evaluation showed that compounds 1 – 9 had significant COX-2 inhibitory activity with IC 50 values ranging from 3.00 μ M to 23.19 μ M. Five new norneolignans sinkianlignans G-K (1 – 5), one phenolic compound ferulagenol A (6) and seven known compounds (7 – 13) were isolated from Ferula sinkiangensis. All the norneolignans were racemic mixtures, and chiral HPLC was used to further separate them. Their structures were assigned, including absolute configurations, using spectroscopic and computational methods. Biological evaluation showed that compounds 1 – 9 had significant COX-2 inhibitory activity with IC 50 values ranging from 3.00 μ M to 23.19 μ M. [Display omitted] [ABSTRACT FROM AUTHOR]

Five undescribed polyprenylated xanthones ( 1 , 3 , 4 , 22 , and 23 ) and 27 known compounds were isolated from Garcinia resins, and the antifungal activities of 15 of them were investigated. Compound 7 exhibited notable in vitro antifungal effects against Magnaporthe grisea with an IC 50 value of 3.54 μg/mL, superior to isoprothiolane (10.30 μg/mL), and showed an excellent protective efficiency of 78.4% at 200 μg/mL against RB (rice blast), equivalent to isoprothiolane (87.2%). Its antifungal activity may be related to the destruction of the cell membrane and the effect of absorption and utilization of sugar by the mycelium, which was proven by the transcriptome sequencing and preliminary mechanism, showing a good application prospect for replacing agrochemical fungicides in the control of RB disease.

Aspongopyrimidine A ( 1 ), a hexa-1,3-diene-histidine-hexanoic acid adduct featuring a 4,5-dihydro-2 H -10λ 4 -imidazo[5,1- f ]pyrrolo[2,1- b ]pyrimidine motif, was isolated from the insect Aspongopus chinensis . The structure was clarified by spectroscopic and computational methods and X-ray diffraction. Peralkylation of N -atoms in histidine by two C6 units makes 1 an inner salt with a 5/6/5 tricyclic system. Biological evaluation found that 1 exerts activity against Alzheimer's disease targeting MAPRE3 through a chemical proteomics approach. This study revealed unusual modifications of amino acids as the fundamental units of protein.