Synthesis of 1-O-acyl- and 1-oxo-kamebanin analogues and their cytotoxic activity.

A series of 1-O-acyl- and 1-oxo-kamebanin analogues were prepared from kamebanin, isolated from Rabdosia excisa and their cytotoxicity was assayed on HL60 promyelocytic leukemia cells and HCT116 human colon cancer cells. The structure-activity relationship study showed that the presence of 1-O-acyl groups of a C3-C5 carbon chain increased the cytotoxic activity.

Comparison of the anti-colitis activities of Qing Dai/Indigo Naturalis constituents in mice.

Qing Dai/Indigo Naturalis (QD) has been shown to ameliorate ulcerative colitis (UC) in clinical trials; however, its mechanism remains elusive. This study investigates the effects of QD on murine dextran sulfate sodium salt-induced colitis. Oral administration of QD protected the animals from colitis as manifested by weight loss, diarrhea, and rectal bleeding. QD was distinguishingly more effective than 5-aminosalicylate. Focused microarray analysis of genes expressed in the distal colon suggested that QD influences the inflammatory pathway. Anti-inflammatory activity of QD was confirmed by the suppression of nitric oxide (NO) production in response to interleukin-1ß in cultured hepatocytes. Some of the constituents in QD, such as tryptanthrin (TRYP) and indigo, suppressed NO production. TRYP maintained body weight but did not inhibit bleeding. Indigo, on the other hand, partially ameliorated bleeding, but did not maintain body weight. The combination of TRYP and indigo did not show additive ameliorating activity. The methanol extract of QD showed an anti-colitis activity like that of TRYP. In contrast, the methanol-insoluble QD fraction moderately ameliorated diarrhea and bleeding. Combining these two fractions resulted in full anti-colitis activity. Further clarification of the active constituents will help in the discovery of a safe and potent prescription for UC.

In vitro study of ultrasound radiation force-driven twinkling sign using PVA-H gel and glass beads tissue-mimicking phantom.

The twinkling sign observed in ultrasound coded-excitation imaging (e.g., GE B-Flow) has been reported in previous research as a potential phenomenon to detect micro calcification in soft tissue. However, the mechanism of the twinkling sign has not been clearly understood yet. We conducted an in vitro experiment to clarify the mechanism of the twinkling sign by measuring a soft tissue-mimicking phantom with ultrasonic and optical devices. A soft tissue-mimicking phantom was made of poly(vinyl alcohol) hydro (PVA-H) gel and 200-µm-diameter glass beads. We applied ultrasound to the phantom using medical ultrasound diagnostic equipment to observe the twinkling sign of glass beads. Optical imaging with a laser sheet and a high-speed camera was performed to capture the scatter lights of the glass beads with and without ultrasound radiation. The scatter lights from the glass beads were quantified and analyzed to evaluate their oscillations driven by the ultrasound radiation force. The twinkling sign from the glass beads embedded in the PVA-H gel soft tissue phantom was observed in ultrasound B-Flow color imaging. The intensity and oscillation of the scattered lights from the glass beads showed significant difference between the cases with and without ultrasound radiation. The results showed a close relationship between the occurrence of the twinkling sign and the variations of the scatter lights of glass beads, indicating that ultrasound radiation force-driven micro oscillation causes the twinkling sign of micro calcification in soft tissue.

Synthesis of rabdokunmin C analogues and their inhibitory effect on NF-κB activation.

A series of rabdokunmin C analogues were prepared and their inhibitory effect on NF-κB activation was assayed. One of them, 18-acetyl-12-deoxy-11,12-dehydrorabdokunmin C (16) was found to be a promising candidate for an anti-inflammatory agent.