A phytochem. study of Silene firma Siebold & Zucc led to the isolation of 30 compounds, including five anthraquinones (1-5), four alkaloids (6-9), six triterpenoids (10-15), twelve sterols (16-27) and three flavonoids (28-30).The structures of these isolated compounds were identified using NMR spectroscopy (¹H and ¹³C) by comparison with previously reported data.To the best of our knowledge, compounds 8, 9, 14, 15, 18, 20, 24-26, 29, and 30 were reported from this plant for the first time.The chemotaxonomic significance of the isolates was also discussed.

2025-01-24·JOURNAL OF ORGANIC CHEMISTRY

Visible Light-Induced Divergent Deoxygenation/Hydroxymethylation of Pyridine N-Oxides

Article

作者: Guo, Hao ; Feng, Changhao ; Ding, Aishun

This study explores the deoxygenation of pyridine N-oxides and presents a one-step photoredox method for the direct synthesis of 2-hydroxymethylated pyridines from pyridine N-oxides. Mechanism studies elucidate the role of the catalyst and provide evidence of the possible electron transfer process and the formation of key radicals. A range of pyridine derivatives, particularly 2-hydroxymethyl-substituted pyridines, which may be difficult to obtain, can be synthesized in a single step.

2025-01-01·JOURNAL OF ETHNOPHARMACOLOGY

Investigation of the anti-inflammatory, anti-pruritic, and analgesic effects of sophocarpine inhibiting TRP channels in a mouse model of inflammatory itch and pain

Article

作者: Wang, Ranjing ; Verkhratsky, Alexei ; Zhou, Dan ; Nie, Hong ; Zhang, Zhe ; Zeng, Hekun

ETHNOPHARMACOLOGICAL RELEVANCE:

Sophocarpine is a bioactive compound extracted from the dried root of Sophorae Flavesentis Aiton, a plant that has been used for thousands of years for various conditions including skin itch and pain. Its antipruritic and analgesic effects are suggested in publications, while the molecular mechanisms underneath interacting with TRP channels are not understood.

AIM OF THE STUDY:

We investigated the anti-inflammatory, antipruritic, and analgesic effects of sophocarpine in a murine inflammatory itch and pain model to elucidate the underlying mechanisms.

MATERIALS AND METHODS:

We evaluated sophocarpine's anti-pruritic and analgesic effects by monitoring mice's scratching and wiping behaviors, and the anti-inflammatory effect by measuring psoriasis area and severity index (PASI) score. The mRNA and protein expression of TRPA1/TRPV1 was analyzed by real-time quantitative polymerase chain reaction and western blotting. We further investigated the relationship between sophocarpine and TRPA1/TRPV1 in mice administered allyl-isothiocyanate (AITC) or capsaicin and by molecular docking.

RESULTS:

We found that sophocarpine decreased scratching bouts, wipes, and the PASI score, reduced the TNF-α and IL-1β in the skin and TRPA1 and TRPV1 in the trigeminal ganglion. Pretreatment of sophocarpine decreased AITC-induced scratching bouts and wipes and capsaicin-induced wipes. We also found potential competitive bindings between sophocarpine and AITC/capsaicin to TRPA1/TRPV1.

CONCLUSIONS:

Sophocarpine is a potential competitive inhibitor of TRPA1 and TRPV1 channels eliciting strong anti-inflammatory, anti-pruritic, and analgesic effects, suggesting its significant therapeutic potential in treating diseases with inflammatory itch and pain.

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适应症	最高研发状态	国家/地区	公司	日期
心肌疾病	临床2期	-	上海仁玑医院管理有限公司	-
心肌疾病	临床2期	-	上海医药集团股份有限公司	-
镇痛	临床前	中国	暨南大学	2025-01-30
炎症	临床前	中国	暨南大学	2025-01-30
瘙痒	临床前	中国	暨南大学	2025-01-30