Design, synthesis, and antitumor activity of desmosdumotin C analogues.

Desmosdumotin C (Des C), a natural product isolated from the roots of , has shown good antitumor activity. A three dimensional quantitative structure-activity relationship (QSAR) study using the comparative molecular field analysis (CoMFA) method was performed on 32 Des C analogues. Based on the QSAR, 18 new Des C analogues were designed and synthesized.

Willingness to pay per quality-adjusted life year: is one threshold enough for decision-making?: results from a study in patients with chronic prostatitis.

Objective: To estimate the willingness to pay (WTP) per quality-adjusted life year (QALY) ratio with the stated preference data and compare the results obtained between chronic prostatitis (CP) patients and general population (GP).

Methods: WTP per QALY was calculated with the subjects' own health-related utility and the WTP value. Two widely used preference-based health-related quality of life instruments, EuroQol (EQ-5D) and Short Form 6D (SF-6D), were used to elicit utility for participants' own health.

Health-related quality of life in Chinese patients with chronic prostatitis/chronic pelvic pain syndrome.

Objective: To examine the health-related quality of life (HRQoL) and factors associated with HRQoL in Chinese patients with chronic prostatitis/chronic pelvic pain syndrome (CP/CPPS) using two generic preference-based HRQoL instruments, EQ-5D (plus EQ-VAS) and SF-6D, with the results compared with general population.

Method: CP/CPPS patients were recruited from two tertiary referral hospitals, and the general populations were randomly approached. After informed consent, subjects were interviewed using EQ-5D, EQ-VAS and SF-6D, and their socio-demographic and medical information was solicited.

Validation and comparison of EuroQol and short form 6D in chronic prostatitis patients.

Objective: Generic, preference-based health-related quality of life (HRQoL) instruments is increasingly used in health-care decision-making process. However, to our knowledge, no such HRQoL instrument has been validated or used in chronic prostatitis. We therefore aimed to assess and compare the psychometric properties of EuroQol (EQ-5D) and Short Form 6D (SF-6D) among chronic prostatitis patients in China.

Anti-nociceptive activity of aqueous fraction from the MeOH extracts of Paederia scandens in mice.

Aim Of The Study: We examined the effects of the aqueous fraction (AF) on nociception models mice induced by the chemical and the thermal stimuli so as to elucidate the analgesic activity and provide scientific basis for the clinical use of Paederia scandens.

Materials And Methods: The AF of MeOH extract from P. scandens was evaluated on anti-nociceptive activity in mice using chemical and thermal models of nociception.

[Progress in study of flavonoids from Annonaceae and biological activities of these compounds].

More than 50 new flavonoids derived from Annonaceae are reported in the last two decades. Many genuses in Annonaceae contain flavonoids having structural novelty and broad pharmacological activities. Due to the pharmacological interest of some of these compounds, chemical investigations on this topic have grown considerably in the decades.

Stellettins L and M, cytotoxic isomalabaricane-type triterpenes, and sterols from the marine sponge Stelletta tenuis.

Two new isomalabaricane-type triterpenes, stellettins L (1) and M (2), and three new sterols (3-5) were isolated from the marine sponge Stelletta tenuis collected in the South China Sea. Chemical structures were established from spectroscopic data and comparison with known compounds. In addition, spectroscopic data reported for the known sterol 24-methylene-27-methylcholest-5-en-3beta-ol-7-one (6) were revised.

Antitumor agents 259. Design, syntheses, and structure-activity relationship study of desmosdumotin C analogs.

Desmosdumotin C (1) and its analogs previously showed potent, selective in vitro anticancer activity. To explore structure-activity relationships of 1 and further increase potency and selectivity, 15 novel analogs (7-15 and 21-26) were synthesized and evaluated for cytotoxity against several human tumor cell lines, as well as inhibition of human endothelial (HUVEC) replication. 4-Bromo-3',3',5'-tripropyl analog 26 showed significant cytotoxity against A549, A431, 1A9, and HCT-8 with ED50 values of 1.

Total synthesis and bioactivity of unique flavone desmosdumotin B and its analogs.

The first total synthesis of a unique flavone natural product, desmosdumotin B (1), was accomplished. Furthermore, three novel flavonoids, 6-8, and a novel chalcone, 9, were synthesized. The new compounds were evaluated as in vitro inhibitors of human cancer cell growth.

Antitumor agents 243. Syntheses and cytotoxicity of desmosdumotin C derivatives.

New analogs of desmosdumotin C (1), in which other aromatic rings replaced the terminal phenyl group and the A-ring was modified, were synthesized. Compounds 2-9, 13, and 16 were evaluated in vitro against human tumor cell replication. The 4-bromophenyl analog (2) showed potent cytotoxic activity in four different tumor cell lines.

Anti-AIDS agents. Part 57: Actein, an anti-HIV principle from the rhizome of Cimicifuga racemosa (black cohosh), and the anti-HIV activity of related saponins.

Actein (1), a tetracyclic triterpenoid from the rhizome of Cimicifuga racemosa (black cohosh), and 82 related triterpenoid and steroidal saponins isolated from higher plants were evaluated for anti-HIV activity as a continuing study to discover potential anti-AIDS agents from natural products. Actein showed potent activity and another twelve saponins showed moderate activity. The active compounds included two steroidal, seven tetracyclic triterpenoid, and four pentacyclic triterpenoid compounds.

Intercedensides A-C, three new cytotoxic triterpene glycosides from the sea cucumber Mensamaria intercedens Lampert.

Three new triterpene glycosides, intercedensides A (1), B (2), and C (3), were isolated from the sea cucumber Mensamria intercedens Lampert, which is found in the South China Sea, and their structures have been elucidated by spectroscopic analysis (NMR and ESIMS) and chemical transformations. Intercedensides A (1) and C (3) have a conjugated double bond (22E,24-diene) in the side chain of the aglycon. Intercedenside B (2) has two beta-D-xylose and two sulfate groups in the carbohydrate chain.

Antitumor agents. Part 218: Cappamensin A, a new In vitro anticancer principle, from Capparis sikkimensis.

A new inhibitor of in vitro tumor cell replication, cappamensin A (1) (2H-1,4-benzoxazin-3(4H)-one, 6-methoxy-2-methyl-4-carbaldehyde), was isolated from the roots of Capparis sikkimensis subsp. formosana using bioactivity-guided fractionation. The structure of 1 was established by spectroscopic methods, including 2D NMR analyses.

[Studies on the chemical constituents from marine brown alga Ishige okamurai (3)].

Objective: To study the chemical constituents of Ishige okamurai.

Method: Compounds were isolated by Pyricularia oryzae bioassay-guided fractionation method in combination with extraction and partitionation as well as multi-chromatography. Their structures were determined by spectral analysis and chemical evidence.

Anti-AIDS agents 54. A potent anti-HIV chalcone and flavonoids from genus Desmos.

Sixteen flavonoids and their derivatives isolated from Desmos spp. were evaluated for inhibition of HIV replication in H9 lymphocyte cells. 2-Methoxy-3-methyl-4,6-dihydroxy-5-(3'-hydroxy)cinnamoylbenzaldehyde (12) and lawinal (6) demonstrated potent anti-HIV activity with EC(50) values of 0.

Anti-AIDS agents 49. Synthesis, anti-HIV, and anti-fusion activities of IC9564 analogues based on betulinic acid.

The betulinic acid derivative IC9564 inhibits human immunodeficiency virus (HIV)-1 entry. Among a series of IC9564 derivatives, 5 and 20 were the most promising compounds against HIV infection with EC(50) values of 0.33 and 0.