Triangesinenolides A-C: Trimeric Phthalides with Anti-Renal Fibrosis Potential from .

Trimeric phthalides in nature are rarely reported. This research successfully isolated three novel trimeric phthalides, triangesinenolides A-C (-), from . These compounds, derived from -ligustilide via diverse linkage patterns, display intricate polycyclic skeletons.

Structure-activity relationship and biofilm formation-related gene targets of oleanolic acid-type saponins from Pulsatilla chinensis against Candida albicans.

In the course of our investigations of antifungal natural products, the structure-activity relationship and antifungal activities of oleanolic acid-type saponins (1-28) from Pulsatilla chinensis against human and plant pathogenic fungi were elucidated. The analysis of structure-activity relationship of oleanolic acid-type saponins showed that the free carboxyl at C-28 was essential for their antifungal activities; the free hydroxyl group at the C-23 site of oleanolic acid-type saponins played a crucial role in their antifungal activities; the oligosaccharide chain at C-3 oleanolic acid-type saponins showed significant effects on antifungal efficacy and a disaccharide or trisaccharide moiety at position C-3 displayed optimal antifungal activity. The typical saponin pulchinenoside B3 (16, PB3) displayed satisfactory antifungal activity against human and plant pathogenic fungi, especially, C.

Senkyunolide B exhibits broad-spectrum antifungal activity against plant and human pathogenic fungi via inhibiting spore germination and destroying the mature biofilm.

Background: Aspergillus infection seriously jeopardizes the health and safety of life of immunocompromised patients. The emergences of antifungal resistance highlight a demand to find new effective antifungal drugs. Angelica sinensis is a medicine-food herb and phthalides are its characteristic components.

New dihydro-β-agarofuran sesquiterpenoids from Tripterygium wilfordii and their anti-inflammatory activity.

Twenty seven dihydro-β-agarofuran sesquiterpenoids, including fifteen new congeners, wilforsinines I-W (1-9, 12-13, 24-27), and twelve known compounds were isolated from the dried root of Tripterygium wilfordii. The structures of the new sesquiterpenoids, wilforsinines I-W, were elucidated by extensive spectroscopic data analysis. The anti-inflammatory activity of isolates 1-27 were evaluated by examining their inhibitory effects on nitric oxide (NO) production in LPS-induced RAW 264.

Discovery of Anti-TNBC Agents Targeting PTP1B: Total Synthesis, Structure-Activity Relationship, and Investigations of Jamunones.

Twenty-three natural jamunone analogues along with a series of jamunone-based derivatives were synthesized and evaluated for their inhibitory effects against breast cancer (BC) MDA-MB-231 and MCF-7 cells. The preliminary structure-activity relationship revealed that the length of aliphatic side chain and free phenolic hydroxyl group at the scaffold played a vital role in anti-BC activities and the methyl group on chromanone affected the selectivity of molecules against MDA-MB-231 and MCF-7 cells. Among them, jamunone M (JM) was screened as the most effective anti-triple-negative breast cancer (anti-TNBC) candidate with a high selectivity against BC cells over normal human cells.

Amycolasporins and Dibenzoyls from Lichen-Associated and Their Antibacterial and Anti-inflammatory Activities.

Eleven metabolites, six echinosporins (-), four dibenzoyls (-), and an aromatic compound (), were isolated from the fermentation broth of lichen-associated . The structures of the new compounds (-, -) were elucidated by comprehensive spectroscopic analysis including data from experimental and calculated ECD spectra. Amycolasporins A-C () demonstrated antibacterial activities against , , and with MIC values of 25 or 100 μg/mL.

A semisynthetic borrelidin analogue BN-3b exerts potent antifungal activity against Candida albicans through ROS-mediated oxidative damage.

In the process of investigating the antifungal structure-activity relationships (SAR) of borrelidin and discovering antifungal leads, a semisynthetic borrelidin analogue, BN-3b with antifungal activity against Candida albicans, was achieved. In this study, we found that oxidative damage induced by endogenous reactive oxygen species (ROS) plays an important role in the antifungal activity of BN-3b. Further investigation indicated that BN-3b stimulated ROS accumulation, increased malondialdehyde (MDA) levels, and decreased reduced/oxidized glutathione (GSH/GSSG) ratio.

Actinofuranones D-I from a Lichen-Associated Actinomycetes, , and Their Anti-Inflammatory Effects.

Six new metabolites, actinofuranones D-I (compounds ⁻), were isolated together with three known compounds-JBIR-108 (), E-975 (), and E-492 ()-from a fermentation broth of derived from the lichen . The structures of the new compounds ⁻ were established using comprehensive NMR spectroscopic data analysis, as well as UV, IR, and MS data. The anti-inflammatory activity of these isolated compounds were evaluated by examining their ability to inhibit nitric oxide (NO) production in LPS-stimulated RAW 264.

Heronamides G-L, polyene macrolactams from .

Six new polyene macrolactams, heronamides G-L (1-6), one new polyenoic acid derivative, niveamide B (10), together with four known compounds, BE-14106-6 (7), BE-14106 (8), GT32-B (9), and niveamide (11), were isolated from the fermentation broth of . Their planar structures were elucidated by detailed analysis of spectroscopic data. The absolute configurations of compounds 1-6 were determined by calculated ECD spectra and analysis of the possible biosynthetic pathways.

Violacin A, a new chromanone produced by Streptomyces violaceoruber and its anti-inflammatory activity.

A new chromanone derivative, named violacin A (1), was isolated from the fermentation broth of Streptomyces violaceoruber as a potential anti-inflammatory compound. The structure of violacin A was established using comprehensive NMR spectroscopic data analysis together with UV, IR, and MS data. The anti-inflammatory effects and action mechanisms of violacin A were investigated in vitro.