| The research was focused on the chemical constituents and biological activities of Chinese traditional medicine Blumea balsamifera and Agarwood of Aquilaria sinensis.As one of the important traditional Chinese medicines,B.balsamifera,first recorded in Bencao Shiyi,has the medicinal effects of dehumidification,expectoration,cough,hemostasis and so on.To date,the research on B.balsamifera has focused on volatile oils and flavonoids,rather than diterpenoids,and their biological activities remain unclear.Agarwood is a precious traditional Chinese medicine,which has attracted great attention in the past decades due to its important role in the pharmaceutical or in the perfume industries.The previous study found that the main chemical substances of agarwood are sesquiterpenes and 2-（2-phenethyl）chromone.It is not clear whether agarwood contains other types of active small molecules.Therefore,it is necessary to discover new pharmacodynamic substances.This study mainly focused on the chemical components and biological activities of B.balsamifera and agarwood,aiming to enrich the structural diversity of small molecular substances and provide basis for clarifying the pharmacodynamic substance basis of them.In all,83 compounds,including 30 new compounds were isolated and identified from the above two kinds of traditional medicine though a variety of chromatographic methods together with the spectroscopy technology.41 compounds were isolated from B.balsamifera,including 9 new compounds（including two new skeletons）.Compound 1 is an unprecedented carbon skeleton featuring a 6/10 bicyclic system with an oxygen bridge between C-8 and C-9 and an epoxy ring located at C-7 and C-8.This kind of diterpenoid skeleton was first discovered.Compound 2 is a rare tricyclic carbon rearranged skeleton possessing a methyl at C-8 instead of C-10,compared to the common pimapine-type diterpenes.Compound 3 is a new roseane-type diterpenoid.Compounds 4–8 are new pimapine-type diterpenoids,of which 6 is a highly oxidized diterpenoid.Compound 15 is a rearranged abietane-type diterpenoid characterized by an oxygen bridge between C-9 and C-10.Bioactivity studies showed that compounds 7 and 15 could dose-dependently inhibited the production of TNF-α,IL-6 and nitrite oxide（NO）in RAW264.7 cells induced by lipopolysaccharide（LPS）,showing their anti-inflammatory activities.Compound 7 also inhibited the phosphorylation of NF-κB.It is suggested that the natural products of B.balsamifera have a certain therapeutic effect on inflammation.42 compounds were isolated from agarwood,including 21 new compounds.The main types of compounds were sesquiterpene and 2-（2-phenylethyl）chromone.Compounds 1–5 are a class of sesquiterpene polymers featuring unusual furaneol rings connecting sesquiterpene units.Compounds 6–10 are a series of sesquiterpenoid-chromone heterohybrids,among which 6 features an unusual pyridine nucleus,and 7 possesses a rare sesquiterpenoid-chromone skeleton via a C–C bond.Compounds 14 and 15 are 2-（2-phenylethyl）chromone dimers.Compound 42 is a2-（2-phenylethyl）chromone containing three epoxy rings.Bioactivity studies showed that compounds 2 and 3 could dose-dependently inhibit the production of TNF-α,IL-6,NO and the activation of NF-κB in LPS-induced RAW264.7 cells,showing their anti-inflammatory activities.Compounds 6 and 7 could significantly inhibit the expression of extracellular matrix components and α-SMA at low concentrations in TGF-β1 induced two types of kidney cells featuring selective inhibition of Smad3 instead of Smad2 phosphorylation,showing their potential in renal fibrosis.The above findings enriched the diversity of small molecular structures of B.balsamifera and Agarwood,and provided a basis for elucidating their medicinal substances.The discovery of biological activity will help to explain the traditional medicinal properties of them,providing lead compounds for the development of possible anti-inflammatory and anti-renal fibrosis drugs. |
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