Context Litsea cubeba (Lour.) Pers. (Lauraceae) has long been used as a folk remedy in Traditional Chinese Medicine (TCM) for the treatment of rheumatic diseases. Previous studies from our laboratory indicated that L. cubeba extract showed anti-arthritic activity in rats. Objective To study L. cubeba chemically and biologically and to find the potential constituents responsible for its anti-arthritic effect. Materials and methods The compounds were isolated from the root of L. cubeba by column chromatography which eluted with PE:EtOAc gradient system, and the structures were elucidated by detailed spectroscopic data analysis; the anti-inflammatory activity of the isolated compounds was evaluated by lipopolysaccharide (LPS)-induced RAW 264.7 cells and the TNF-α and NO level were measured by ELISA (commercial kit); The iNOS and COX-2 mRNA expression were measured by RT-PCR and the phosphorylation of IκBα, IKKβ, P38 and Akt were determined by western blots. Results A novel 9-fluorenone, 1-ethoxy-3,7-dihydroxy-4,6-dimethoxy-9-fluorenone (1), together with 4 known compounds, namely pinoresinol (2), syringaresinol (3), 9,9′-O-di-(E)-feruloyl-meso-5,5′-dimethoxysecoisolariciresinol (4) and lyoniresinol (5) were isolated from the root of L. cubeba for the first time. The IC₅₀ for NO inhibition on compounds 1 and 4 were 56.1 ± 1.2 and 32.8 ± 2.3 μM, respectively. The IC₅₀ for TNF-α inhibition were 28.2 ± 0.9 and 15.0 ± 1.0 μM, respectively. Both 1 and 4 suppress mRNA expression of iNOS, COX-2 and protein phosphorylation of IκBα, IKKβ in LPS-induced RAW 264.7 cells. Discussion and conclusion Compounds 1 and 4 isolated from L. cubeba exhibited potent anti-inflammatory activity through the NF-κB signal pathway.

The purpose of this study was to investigate chemical composition and cytotoxic activities of essential oils from Zingiber striolatum Diels flowers, leaves and stems. 73, 68 and 66 compounds representing 97.0%, 94.8% and 93.7% of flowers, leaves and stems essential oils were identified using GC-FID and GC-MS, respectively. The main constituents of the flowers oil were β-phellandrene (28.5%), α-humulene (14.7%), β-pinene (8.2%), β-elemene (5.5%), humulene oxide II (3.5%), cryptone (3.3%) and tricosane (3.2%). The predominant components in the leaves oil were hexahydrofarnesyl acetone (24.7%), α-humulene (12.2%), phytol (11.9%), humulene oxide II (6.3%), β-pinene (4.3%), sandaracopimaradiene (3.1%) and β-elemene (3.0%). The stems oil contained mainly α-humulene (15.6%), humulene oxide II (7.9%), hexahydrofarnesyl acetone (7.4%), phytol (7.2%), humulene oxide I (4.1%), β-elemene (3.8%) and 4-terpineol (3.2%). The cytotoxic activity against human leukemic (K562), prostatic carcinoma (PC-3) and lung cancer (A549) cell lines of essential oils was assessed using MTT assay. The essential oils of flowers, leaves and stems exhibited significant cytotoxicity against K562 (IC50: 12.94–37.89 μg/mL), PC-3 (IC50: 69.06–82.56 μg/mL) and A549 (IC50: 45.73–66.12 μg/mL) cell lines. This is the first report on the chemical constituents and cytotoxic activities of Z. striolatum flowers, leaves and stems essential oils.

Described herein is the development of a facile and efficient methodology for the synthesis of novel turmerone motif-fused 3,3′-pyrrolidinyl-dispirooxindoles 3–5 via a multicomponent 1,3-dipolar cycloaddition of dienones 2 with azomethine ylides (thermally generated in situfrom isatins and proline or thioproline or sarcosine). Products bearing four or three consecutive stereocenters consist of two oxindole moieties and a pyrrolidinyl core, including vicinal spiroquaternary stereocenters fused in one ring structure were smoothly obtained in high yields (up to 93% yield) with good diastereoselectivity (up to >20:1). Another valuable application of this method was for the design of new hybrid architectures for biological screening through the adequate fusion of these sub-units of turmerone and 3,3′-pyrrolidinyl-dispirooxindole, generating drug-like molecules.

The drying process of Uncariae Ramulus Cum Uncis (URCU), a kind of traditional Chinese medicine, was studied in a scale dryer in laboratory at 65°C. It was observed that the alkaloids content of URCU firstly showed a tendency of increasing and then decreasing after reaching the peak at the 570th minute in the process of constant temperature drying. Moreover, the coagulation time of rabbit determined by test tubes has been adopted to study the effect imposed by the content of alkaloids on the anticoagulating activity of URCU. In addition, the software of Minitab was also utilized to fit the correlation between the content of alkaloids and the anticoagulating activity of URCU. The results obtained demonstrated that anticoagulant activities were available in both rhynchophylline and isorhynchophylline, among which the latter was the stronger one, while procoagulant activity was shown in corynoxeine. The case study can provide a useful reference for the research on drying other Chinese herbal medicines (CHMs) and further study on URCU.

Described herein is an environmentally benign method for the synthesis of multisubstituted 3-alkoxylated-2-oxindoles 3 via direct alkoxylation of 3-halooxindoles 1. A wide variety of such multisubstituted 3-alkoxylated-2-oxindole scaffolds were smoothly obtained in good yields (up to 94%) by heating in an oil bath at 35 °C for 24 h. A particularly valuable feature of this method was the development of environment-friendly chemistry using alcohols 2 as both the substrates and solvents in the presence of a catalytic amount of base.