Recent advances in target identification technology of natural products.

Natural products, characterized by their structural diversity, broad spectrum of biological activities, and safe yet effective therapeutic potential, have become pivotal resources in drug research and development. However, the target proteins of many natural products remain unidentified, a significant challenge that impedes their development into viable drug candidates. Therefore, the target identification is crucial for elucidating the pharmacological mechanisms of natural products and facilitating their therapeutic applications.

Phenolic compounds from sappan lignum and their anti-neuroinflammatory activities.

Caesappanols A-F (1-6), six undescribed phenolic compounds, including two dibenzofurans (1, 2), three biphenols (3-5), and one homoisoflavan (6), along with ten known compounds (7-16), were isolated from Sappan Lignum, the heartwood of Caesalpinia sappan L. Compounds 1 and 2 represent the initial discovery of dibenzofuran skeletons within this herb. Structural elucidation of these compounds was achieved through comprehensive analysis of 1D NMR, 2D NMR, and mass spectrometry data.

(+)/(-)-Corydecumbenpines A and B, two pairs of dimeric phthalide-benzophenanthridine alkaloids with cytotoxicity from Corydalis decumbens.

Four pairs of previously undescribed enantiomers, including two pairs of dimeric phthalide-benzophenanthridine alkaloid and two pairs phthalides derivatives, corydecumbenpines A-D, were isolated from the rhizomes of Corydalis decumbens. Their planar structures were elucidated by extensive spectroscopic analysis including UV, IR, HRESIMS, 1D and 2D NMR. Optically pure compounds were obtained by chiral chromatography and their absolute configurations were determined by single-crystal X-ray crystallography and comparison of experimental and calculated ECD spectra.

Corydalis decumbens and tetrahydropalmatrubin inhibit macrophages inflammation to relieve rheumatoid arthritis by targeting Fosl2.

Ethnopharmacological Relevance: Corydalisdecumbens (Thunb.) (CD) is a traditional Chinese medicine and as a single herb or formula has been used to treat RA for decades. Rheumatoid arthritis (RA) is a persistent, systemic autoimmune inflammatory disease.

Mitochondrial Electron Flow Dynamics Imaging for Assessing Mitochondrial Quality and Drug Screening.

Mitochondrial quality control is paramount for cellular development, with mitochondrial electron flow (Mito-EF) playing a central role in maintaining mitochondrial homeostasis. However, unlike visible protein entities, which can be monitored through chemical biotechnology, regulating mitochondrial quality control by invisible entities such as Mito-EF has remained elusive. Here, a Mito-EF tracker (Mito-EFT) with a four-pronged probe design is presented to elucidate the dynamic mechanisms of Mito-EF's involvement in mitochondrial quality control.

Therapeutic Potential of Carbon Dots Derived from Phytochemicals as Nanozymes Exhibiting Superoxide Dismutase Activity for Anemia.

Anemia is a potentially life-threatening blood disorder caused by an insufficient erythroblast volume in the circulatory system. Self-renewal failure of erythroblast progenitors is one of the key pathological factors leading to erythroblast deficiency. However, there are currently no effective drugs that selectively target this process.

Euchrestifolines A-O, fifteen novel carbazole alkaloids with potent anti-ferroptotic activity from Murraya euchrestifolia.

Fifteen novel carbazole alkaloids, euchrestifolines A-O (1-15), were obtained from Murraya euchrestifolia. Their structures were elucidated by spectroscopic analysis, Mosher's ester, calculated ECD, and transition metal complex ECD methods. Notably, euchrestifolines A-C (1-3) are the first naturally occurring pyrrolidone carbazoles to be identified, while euchrestifolines D-F (4-6) represent rare carbazole alkaloids containing a phenylpropanyl moiety; euchrestifoline G (7) features a unique benzopyranocarbazole skeleton.

Antrodia cinnamomea triterpenoids attenuate cardiac hypertrophy via the SNW1/RXR/ALDH2 axis.

Aldehyde dehydrogenase 2 (ALDH2), a pivotal enzyme in the metabolism of toxic aldehydes produced by oxidative stress, has been demonstrated to play a cardioprotective role in cardiovascular diseases. Antrodia cinnamomea triterpenoids (ACT) is a medicinal mushroom with anti-inflammatory and antioxidant properties, and our previous study found that ACT can exert anti-fatty liver effects by regulating ALDH2. This study aimed to elucidate the impact of ACT and its monomer on cardiac hypertrophy and investigate the relationship between its pharmacological mechanism and ALDH2.

Total glucosides of Picrorhizae Rhizome alleviate non-alcoholic steatohepatitis (NASH) by specifically targeting acyl-CoA oxidase 1.

Nonalcoholic steatohepatitis (NASH), a chronic liver disease characterized by the accumulation of fat in the liver, is highly prevalent on a global scale. In this study, we investigated the effects of total glucosides of Picrorhizae Rhizome (TGPR), the primary active ingredients in traditional Chinese herbal medicine derived from Pennell. TGPR is known for its efficiency in attenuating NASH, in mouse models induced by methionine-choline deficient (MCD) diet or high-fat diet (HFD).

NO inhibitory constituents from Glycosmis craibii var. glabra.

Six novel compounds, comprising three quinolones (1a, 1b, and 2) and three flavanones (3-5), along with seven known analogs (6-13), were isolated from the 95% EtOH extract of the stems and leaves of Glycosmis craibii var. glabra. The structures of the new compounds were elucidated using HR-ESI-MS, UV, and 1D and 2D nuclear magnetic resonance (NMR) data analysis.

Tamarixetin ameliorates cerebral ischemia-reperfusion injury via suppressing nicotinamide adenine dinucleotide phosphate oxidase 2/nucleotide-binding oligomerization domain like receptor family pyrin domain-containing 3 inflammasome activation.

Tamarixetin, a natural dietary flavone, exhibits remarkable potential for the treatment of ischemic stroke. The present article aimed to explore the impact of tamarixetin on ischemic stroke and elucidate the underlying mechanisms. Effects of tamarixetin on ischemic stroke were evaluated in rats using the middle cerebral artery occlusion and reperfusion (MCAO/R) model, by assessing the neurological deficit scores, brain water content, brain infraction, and neuronal damage.

Chemoproteomic Strategy Identifies PfUCHL3 as the Target of Halofuginone.

The human malaria parasite Plasmodium falciparum (P. falciparum) continues to pose a significant public health challenge, leading to millions of fatalities globally. Halofuginone (HF) has shown a significant anti-P.

Multifunctional sprayable carboxymethyl chitosan/polyphenol hydrogel for wound healing.

The use of facile methods to synthesize environmentally friendly and multifunctional hydrogel dressings is still a major challenge in development. Herein, Turkish gall extract (TGE) and carboxymethyl chitosan (CMCS) were combined and sprayed using a dual syringe to form a multifunctional TGE-CMCS hydrogel (TC gel) in one step through abundant hydrogen bonding between functional groups as a green approach. TC gel showed rapid gelation at 19.

Enhanced optical imaging and fluorescent labeling for visualizing drug molecules within living organisms.

The visualization of drugs in living systems has become key techniques in modern therapeutics. Recent advancements in optical imaging technologies and molecular design strategies have revolutionized drug visualization. At the subcellular level, super-resolution microscopy has allowed exploration of the molecular landscape within individual cells and the cellular response to drugs.

Erratum: Author correction to 'Pharmacologically targeting molecular motor promotes mitochondrial fission for anti-cancer' [Acta Pharm Sin B 11 (2021) 1853-1866].

[This corrects the article DOI: 10.1016/j.apsb.

Small-molecule targeting PKM2 provides a molecular basis of lactylation-dependent fibroblast-like synoviocytes proliferation inhibition against rheumatoid arthritis.

Fibroblast-like synoviocytes (FLS) play an important role in rheumatoid arthritis (RA)-related swelling and bone damage. Therefore, novel targets for RA therapy in FLS are urgently discovered for improving pathologic phenomenon, especially joint damage and dyskinesia. Here, we suggested that pyruvate kinase M2 (PKM2) in FLS represented a pharmacological target for RA treatment by antimalarial drug artemisinin (ART).

Mercuric sulfide nanoparticles suppress the neurobehavioral functions of Caenorhabditis elegans through a Skp1-dependent mechanism.

Cinnabar is the naturally occurring mercuric sulfide (HgS) and concerns about its safety have been grown. However, the molecular mechanism of HgS-related neurotoxicity remains unclear. S-phase kinase-associated protein 1 (Skp1), identified as the target protein of HgS, plays a crucial role in the development of neurological diseases.

Cayratia albifolia C.L.Li exerts anti-rheumatoid arthritis effect by inhibiting macrophage activation and neutrophil extracellular traps (NETs).

Background: Cayratia albifolia C.L.Li (CAC), commonly known as "Jiao-Mei-Gu" in China, has been extensively utilized by the Dong minority for several millennia to effectively alleviate symptoms associated with autoimmune diseases.