Tanshinone and phenolic acids are the most important active substances of Salvia miltiorrhiza, and the insight into their transcriptional regulatory mechanisms is an essential process to increase their content in vivo. SmMYB36 has been found to have important regulatory functions in the synthesis of tanshinone and phenolic acid, paradoxically, its mechanism of action in S. miltiorrhiza is not clear. Here, we demonstrated that SmMYB36 functions as a promoter of tanshinones accumulation and a suppressor of phenolic acids through the generation of SmMYB36 overexpressed and chimeric SmMYB36-SRDX (EAR repressive domain) repressor hairy roots in combination with transcriptomic-metabolomic analysis. SmMYB36 directly down-regulate the key enzyme gene of primary metabolism, SmGAPC, up-regulate the tanshinones biosynthesis branch genes SmDXS2, SmGGPPS1, SmCPS1 and down-regulate the phenolic acids biosynthesis branch enzyme gene, SmRAS. Meanwhile, SmERF6, a positive regulator of tanshinone synthesis activating SmCPS1, was up-regulated and SmERF115, a positive regulator of phenolic acid biosynthesis activating SmRAS, was down-regulated. Furthermore, the seven acidic amino acids at the C-terminus of SmMYB36 are required for both self-activating domain and activation of target gene expression. As a consequence, this study contributes to reveal the potential relevance of transcription factors synergistically regulating the biosynthesis of tanshinone and phenolic acid.

Pertyolides A (1) and B (2), two unprecedented C₁₇-eudesmanolides with extended side chains, and one rare C₁₇-guaianolide, pertyolide C (3), along with 15 known sesquiterpene lactones were isolated from the whole plant of Ainsliaea pertyoides. Their structures were elucidated by extensive spectroscopic analysis. The absolute configuration of compound 1 was assigned by X-ray crystallography. All isolates were evaluated for their cytotoxic activities against four human tumor cell lines A549, HCT116, MGC803, CCRF-CEM, and only alantolactone (5) showed significant inhibitions against the tumor cell lines tested.

Amorpha-4,11-diene synthase (ADS) catalyzes the first committed step in the artemisinin biosynthetic pathway, which is the first catalytic reaction enzymatically and genetically characterized in artemisinin biosynthesis. The advent of ADS in Artemisia annua is considered crucial for the emergence of the specialized artemisinin biosynthetic pathway in the species. Microbial production of amorpha-4,11-diene is a breakthrough in metabolic engineering and synthetic biology. Recently, numerous new techniques have been used in ADS engineering; for example, assessing the substrate promiscuity of ADS to chemoenzymatically produce artemisinin. In this review, we discuss the discovery and catalytic mechanism of ADS, its application in metabolic engineering and synthetic biology, as well as the role of sesquiterpene synthases in the evolutionary origin of artemisinin.

Three new diterpenoids (1–3) (two abietane type diterpenoids and a paralianone type diterpenoid), together with four known compounds (4–7) were isolated from the whole plants of Euphorbia peplus. Their structures were elucidated through spectroscopic analysis and physicochemical characteristics. The cytotoxic activities of compounds 1–7 against five human tumour cell lines were evaluated, however, they were inactive at the concentration of 40 μM. The compound 3 enhanced lysosomal biogenesis with Lyso Tracker staining intensity of 132.6%.

One new limonoid, toonaciliatone A (1), and one new tirucallane-type triterpenoid, toonaciliatine A (4), along with three known compounds, methyl-3β-acetoxy-1-oxomelic-14(15)-enate (2), perforin A (3), and cholest-14-ene-3,7,24,25-tetrol-21,23-epoxy-21-methoxy-4,4,8-trimethyl-3-(3-methyl-2-butenoate) (5), were isolated from the leaves of Toona ciliata. The structures of the new compounds were established by spectroscopic methods.