Abstract
Dipeptidyl peptidase I (DPPI) and chymase, the granulo-proteases produced and released by mast cells, are important targets of anti-inflammatory drug research and development. Cortex Dictamni is a definite nature drug with anti-inflammatory activity, but the mechanism is unclear and effects of Cortex Dictamni on DPPI and chymase are unknown. This study focuses on effects of Cortex Dictamni aqueous extract (CDAE) on DPPI and chymase activities using cell model, bio-molecular interactions and the Molecular docking study by Discovery Studio (DS) analysis. The results showed that CDAE could significantly inhibit DPPI and chymase activities in vitro and in living rat spleen lymphocytes. Molecular docking simulation demonstrated that Troxerutin, the one of the active compounds of Cortex Dictamni, formed a hydrogen bond with amino acid ILE429 and a strong hydrophobic interaction with TYR64 CYS234 PRO279 ALA382 of DPPI. These interactions allow Troxerutin to form a stable complex with the DPPI, implicating that Troxerutin might be a potential natural inhibitor of DPPI. Dictamnoside M, another active compound of Cortex Dictamni formed hydrogen bonds and hydrophobic interactions within the binding pocket of chymase domain and form a stable complex with the chymase. Dictamnoside M maybe a potential natural inhibitor of chymase. This study suggested a new nature inhibitor Cortex Dictamni and its active components with the anti-inflammatory effects.
Highlights
Materials and MethodsCortex Dictamni was bought from a Chinese medicine shop (Tongrentang) and powdered using a new-style grinder for Chinese medicine (Changshu Chinese Traditional Medicine Machinery Co., Ltd., China). 100g of crude Cortex Dictamni powder were boiled with distilled water for 40 minutes and filtered three times with cotton gauze
The activities of DPP1 and chymase are strongly related to the development of inflammation
This study focuses on effects of Cortex Dictamni aqueous extract (CDAE) on Dipeptidyl peptidase I (DPPI) and chymase activities using cell model, bio-molecular interactions and the Molecular docking study by Discovery Studio (DS) analysis
Summary
Cortex Dictamni was bought from a Chinese medicine shop (Tongrentang) and powdered using a new-style grinder for Chinese medicine (Changshu Chinese Traditional Medicine Machinery Co., Ltd., China). 100g of crude Cortex Dictamni powder were boiled with distilled water for 40 minutes and filtered three times with cotton gauze. Cortex Dictamni was bought from a Chinese medicine shop (Tongrentang) and powdered using a new-style grinder for Chinese medicine (Changshu Chinese Traditional Medicine Machinery Co., Ltd., China). 100g of crude Cortex Dictamni powder were boiled with distilled water for 40 minutes and filtered three times with cotton gauze. The water was removed by a rotary vacuum evaporator in total filtrates of CDAE. The half solid extract concretes (from 100g of crude powder) were re-suspended in total volume 50 ml of DMEM to make 1g/mL backup solution of CDAE. Backup solution of CDAE was stored at −80 °C for the night and put in a freeze-dryer for two days, stored at −80 °C (T .Wei et al, 2018 )
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