Zhong-Hua Gao

Kadcoccitones A and B, Two New 6/6/5/5-Fused Tetracyclic Triterpenoids from Kadsura coccinea

A pair of new triterpenoid epimers, kadcoccitones A (1) and B (2), together with a new biogenetically related compound kadcoccitone C (3), were isolated from Kadsura coccinea. The epimers featured an unprecedented carbon skeleton with a 6/6/5/5-fused tetracyclic ring system unit and a C(9) side chain. Their structures were determined by spectroscopic data, ECD calculation, and single-crystal X-ray diffraction. Compounds 1 and 3 showed anti-HIV-1 activity with an EC(50) value of 47.91 and 32.66 μg/mL, respectively.

Six new lignans from the leaves and stems of Schisandra sphenanthera

Six new lignans, schisphenlignans F-K (1-6), together with ten known ones, were isolated from the leaves and stems of Schisandra sphenanthera. Their structures were elucidated on the basis of spectroscopic methods, including extensive NMR, MS and CD spectra. In addition, some compounds were tested for their acute activity on insulin sensitivity in 3T3-L1 differentiated adipocytes and anti-HIV-1 activity.

Four new indole alkaloids from Plantago asiatica.

Four new indole alkaloids, plasiaticines A-D (1–4), together with two known ones, were isolated from the seeds of Plantago asiatica. The structures of the new compounds were elucidated on the basis of comprehensive analysis of spectroscopic data. All compounds were tested for their cytotoxic activity, and all compounds except 4 were tested for their acetylcholinesterase (AChE) inhibitory activities.Graphical abstract

Plasiatine, an Unprecedented Indole–Phenylpropanoid Hybrid from Plantago asiatica as a Potent Activator of the Nonreceptor Protein Tyrosine Phosphatase Shp2

Plasiatine (1), isolated from the seeds of Plantago asiatica, is an unprecedented indole analogue linked to a phenylpropanoid moiety via a carbon bond that builds up a novel heteromeric construction with a C19N2 scaffold. Its structure was determined by spectroscopic data and computational evidence. Notably, experimental assay demonstrated that 1 significantly enhanced the activity of the nonreceptor protein tyrosine phosphatase Shp2 in vitro in a concentration-dependent manner with an EC50 value of 0.97 μM, and activated phosphorylation of ERK, a known target of Shp2. Moreover, plasiatine (1) promoted hepatocellular HepG2 cells migration. Molecular docking suggested that plasiatine (1) binds to the catalytic cleft of Shp2. These results identified plasiatine (1) as the first small molecule Shp2 activator, and it warrants further investigation as a novel pharmaceutical tool to study the function of Shp2 in tumorigenesis.

Phenolic constituents from Parakmeria yunnanensis and their anti-HIV-1 activity

Three new phenolic compounds, yunnanensins A–C (1–3), together with fourteen known ones (4–17), were isolated from the leaves and stems of Parakmeria yunnanensis. The structures of new compounds were established on the basis of extensive spectroscopic analyses. Several compounds showed weak anti-HIV-1 activity.

Two new neolignans from Manglietia insignis

Two new neolignans, manneoinsigins A (1) and B (2), together with four known lignans, were isolated from the leaves and stems of Manglietia insignis. The new compounds were established on the basis of extensive spectroscopic analyses. All compounds except 2 were tested for their cytotoxic activity. Compound 3 showed weak cytotoxic activity against the HL-60 human tumor cell line with the IC50 value of 23.5 µM.Graphical abstract

Four new lignans from the leaves and stems of Schisandra propinqua var. sinensis

Four new tetrahydrofuran lignans, schpropinrins A-D (1–4), together with five known ones, were isolated from the leaves and stems of Schisandra propinqua var. sinensis. Their structures, including absolute configurations, were characterized by means of spectroscopic analysis and ECD calculation. Compounds 1–4 featured a ketal or hemiketal substructure at C-7 and all of the isolates were tested for their anti-HIV integrase activity.