Study on Anti-Inflammatory Activity of Niloticin by Targeting MD-2 Based on Computer-Aided Drug Design and Biolayer Interferometry

Niloticin is an active compound from Cortex phellodendri, but its antiinflammatory activity has not yet been explored. The aim of the present study was to assess the drug potential of niloticin and to study the MD-2-targeting mechanism of its anti-inflammatory activity. Niloticin’s drug potential was analyzed using the Traditional Chinese Medicine Systems Pharmacology Database. Molecular docking and biolayer interferometry technology were used to explore the anti-inflammatory mechanism of niloticin by targeting myeloid differentiation protein 2 (MD-2), which mediates a series of Toll-Like Receptor (TLR) 4-dependent inflammatory responses. The cytokines involved in the LPSTLR4/ MD-2-NF-κB pathway were evaluated by ELISA, RT-PCR, and western blot. The results showed that niloticin has drug potential and could bind to MD- 2. Niloticin had no impact on cell viability. Niloticin could significantly decrease the levels of NO, IL-6, TNF-a, and IL-1β (P<0.01) induced by LPS. IL-1β, IL-6, iNOS, TNF-a, and COX-2 mRNA expression levels were decreased by niloticin (all P<0.01). Compared with the control group, TLR4, p65, MyD88, p-p65, and iNOS expression levels induced by LPS were suppressed by niloticin (all P<0.01). In conclusion, niloticin is a potential MD-2 antagonist. It might interact with MD-2 to play an anti-inflammatory role by suppressing the activation of the LPS-TLR4/MD-2-NF-κB signaling pathway.

Ethnopharmacology, Phytochemistry and Pharmacological Properties of Cortex Phellodendri Chinensis: A Comprehensive Review

Ethnopharmacological Relevance: Cortex Phellodendri Chinensis (CPC), a traditional Chinese medicine known as “HuangBai” in China, are being widely employed as its health benefits. CPC has the function of clearing heat and expelling dampness, purging fire and removing toxin, detumescencing and removing necrotic tissue, which have the treatment for a variety of diseases. Aim of The Study: The present review is intended to summarize the current researches on the phytochemistry, pharmacological significances and medicinal uses of CPC, hoping to provide reference and scientific basis for the research of bioactive ingredients, quality markers of CPC, as well as further development and utilization in treatment of human diseases with CPC. Materials and Methods: Extensive search of various documents and electronic databases such as Pubmed, Royal Society of Chemistry, Science Direct, Springer, Web of Science, and Wiley, etc., were done to obtain data. Other online academic libraries, e.g. Google Scholars, Scopus and national pharmacology literature were also been employed to learn more information about CPC. Additional information was derived from herbal classic books, Chinese pharmacopoeia, Postgraduate theses, China national knowledge internet, etc. Results: The comprehensive analysis of the electronic database and literatures demonstrated that CPC is a valuable herbal medicine with multiple pharmacological effects. Phytochemical and pharmacological analysis indicated alkaloids are the major bioactive ingredients in CPC. However, there are no reports on the research of quality markers of CPC, which means in a short time, there will emerge many studies to fill this gap. Under the guidance of traditional Chinese medicines theory, CPC is usually combined with other traditional Chinese medicines into prescriptions for various clinical use. Conclusions: This review summarized the results from current researches about the basic characteristics of CPC, such as bioactive constituents, pharmacological effect and mechanism of action, which are still being studied and explored in order to realize the optimal medical practice. Meanwhile, it points out the existed problems of the current researches of CPC and puts forward some suggestions for the future research of CPC.

Huang-Lian Jie-Du decoction: a review on phytochemical, pharmacological and pharmacokinetic investigations

Huang-Lian Jie-Du decoction (HLJDD), a famous traditional Chinese prescription constituted by Rhizoma Coptidis, Radix Scutellariae, Cortex Phellodendri and Fructus Gradeniae, has notable characteristics of dissipating heat and detoxification, interfering with tumors, hepatic diseases, metabolic disorders, inflammatory or allergic processes, cerebral diseases and microbial infections. Based on the wide clinical applications, accumulating investigations about HLJDD focused on several aspects: (1) chemical analysis to explore the underlying substrates responsible for the therapeutic effects; (2) further determination of pharmacological actions and the possible mechanisms of the whole prescription and of those representative ingredients to provide scientific evidence for traditional clinical applications and to demonstrate the intriguing molecular targets for specific pathological processes; (3) pharmacokinetic feature studies of single or all components of HLJDD to reveal the chemical basis and synergistic actions contributing to the pharmacological and clinically therapeutic effects. In this review, we summarized the main achievements of phytochemical, pharmacological and pharmacokinetic profiles of HLJDD and its herbal or pharmacologically active chemicals, as well as our understanding which further reveals the significance of HLJDD clinically.