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Tanshinones and diethyl blechnics with anti-inflammatory and anti-cancer activities from Salvia miltiorrhiza Bunge (Danshen)

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ABSTRACT

1–45–1844444: Four novel compounds () as well as fourteen reported compounds () were isolated and purified from Salvia miltiorrhiza Bunge (Danshen). The structures of novel compounds were determined by 1D and 2D NMR, HRESIMS data, etc. The anti-inflammatory properties of all the compounds on RAW264.7 macrophages and their cytotoxicity on H1299 and Bel-7402 cell lines coupled with a structure-activity relationship (SAR) were investigated. Compound demonstrated the best anti-inflammatory activity and was chosen for further research. Compound greatly suppressed secretion of nitric oxide (NO), tumor necrosis factor (TNF)-α and interleukin-6 (IL-6) in the RAW264.7 macrophages stimulated by LPS. Additionally, the protein expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) was decreased and the nuclear translocation of NF-κB was attenuated after treatment with compound in vitro. Compound was able to dramatically inhibit LPS-induced activation of JNK1/2 and ERK1/2 and remarkably disrupted the TLR4 dimerization in LPS-induced RAW264.7 macrophages. Thus, the new compound suppressed LPS-induced inflammation partially is due to the blocking TLR4 dimerization. In addition, the anti-cancer activity investigation indicated that most of isolated compounds exhibited cytotoxicity and the SAR analysis showed that the intact D ring was indispensable and unsaturated D ring played vital role.

No MeSH data available.


Structures of compounds 1–18.
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Mentions: Danshen has been one of the most widely investigated herbs worldwide at present. To date, over 20,000 publications related to Danshen could be retrieved from the SciFinder database. Furthermore, more than 100 compounds have been identified from Danshen. Classified in terms of structural characteristics and chemical properties, the compounds isolated from Danshen can be categorized as water-soluble and lipid-soluble constituents13. Water-soluble constituents, including salvianolic A-G or lithospermic acid B, mainly exhibit cardiovascular protective activities1415. While the lipid-soluble constituents, including tanshinone IIA, dihydrotanshinone I, or cryptotanshinone, show remarkable properties of anti-cancer and anti-inflammation16171819. In this study, accompanied by fourteen known compounds (5–18), four novel compounds (1–4) (Fig. 1) were obtained from Danshen. Four compounds were structurally elucidated and the isolated compounds were used to investigate their anti-inflammatory and anticancer activities.


Tanshinones and diethyl blechnics with anti-inflammatory and anti-cancer activities from Salvia miltiorrhiza Bunge (Danshen)
Structures of compounds 1–18.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC5036060&req=5

f1: Structures of compounds 1–18.
Mentions: Danshen has been one of the most widely investigated herbs worldwide at present. To date, over 20,000 publications related to Danshen could be retrieved from the SciFinder database. Furthermore, more than 100 compounds have been identified from Danshen. Classified in terms of structural characteristics and chemical properties, the compounds isolated from Danshen can be categorized as water-soluble and lipid-soluble constituents13. Water-soluble constituents, including salvianolic A-G or lithospermic acid B, mainly exhibit cardiovascular protective activities1415. While the lipid-soluble constituents, including tanshinone IIA, dihydrotanshinone I, or cryptotanshinone, show remarkable properties of anti-cancer and anti-inflammation16171819. In this study, accompanied by fourteen known compounds (5–18), four novel compounds (1–4) (Fig. 1) were obtained from Danshen. Four compounds were structurally elucidated and the isolated compounds were used to investigate their anti-inflammatory and anticancer activities.

View Article: PubMed Central - PubMed

ABSTRACT

1–45–1844444: Four novel compounds () as well as fourteen reported compounds () were isolated and purified from Salvia miltiorrhiza Bunge (Danshen). The structures of novel compounds were determined by 1D and 2D NMR, HRESIMS data, etc. The anti-inflammatory properties of all the compounds on RAW264.7 macrophages and their cytotoxicity on H1299 and Bel-7402 cell lines coupled with a structure-activity relationship (SAR) were investigated. Compound demonstrated the best anti-inflammatory activity and was chosen for further research. Compound greatly suppressed secretion of nitric oxide (NO), tumor necrosis factor (TNF)-α and interleukin-6 (IL-6) in the RAW264.7 macrophages stimulated by LPS. Additionally, the protein expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) was decreased and the nuclear translocation of NF-κB was attenuated after treatment with compound in vitro. Compound was able to dramatically inhibit LPS-induced activation of JNK1/2 and ERK1/2 and remarkably disrupted the TLR4 dimerization in LPS-induced RAW264.7 macrophages. Thus, the new compound suppressed LPS-induced inflammation partially is due to the blocking TLR4 dimerization. In addition, the anti-cancer activity investigation indicated that most of isolated compounds exhibited cytotoxicity and the SAR analysis showed that the intact D ring was indispensable and unsaturated D ring played vital role.

No MeSH data available.