A new poly-substituted benzaldehyde from the leaves of Lysimachia fordiana Oliv.

A new poly-substituted benzaldehyde, 1, and a known compound quercetin (2) were isolated from the leaves of Lysimachia fordiana Oliv. The structure of compound 1, named fordianol, was determined as 2-heptyl-3,6-dihydroxy-4- methoxybenzaldehyde on the basis of spectroscopic methods. Fordianol did not inhibit the growth of SWO-38 (human brain neuroglioma), MCF-7 (human breast cancer) or HeLa (human cervical carcinoma) cell lines.

Inhibitory activities of three annonaceous acetogenins on NADH oxidase of chicken liver mitochondria.

Annonaceous acetogenins (ACG) are natural products found in the plant family Annonaceae and which strongly inhibited mitochondrial complex I. The inhibition of NADH oxidase of chicken liver mitochondria by three different structural ACG was studied here, and ACG was shown to have potent inhibitory activities similar to rotenone for NADH oxidase. The IC(50) values indicated that bis-adjacent tetrahydrofuran (THF) type squamocin C was more potent than non-adjacent bis-THF type squamostatin B, and the latter was more potent than non-THF type compound 1 in the assay. The roles of structural factors of ACG such as the terminal gamma-lactone, the features of other ring moieties and hydroxyl groups, as well as the alkyl chain were simply discussed in this study.

[Antitumor effect of anuoning].

BACKGROUND & OBJECTIVE: The authors' previous studies have demonstrated that anuoning bullatacin and squamocin have anticancer activity in vitro. Squamocin could induce apoptosis of HL-60 cells. The purpose of this paper was to investigate cytotoxicity and antitumor effect of anuoning. METHODS: MTT assay was used to examine the growth inhibition of anuoning on human colon carcinoma cell line (HT-29), human nasopharyngeal carcinoma cell line (SUNE1, CNE2), human liver carcinoma (bel-7402), human breast adenocarcinoma cell line (MCF-7) and human lung adenocarcinoma cell line (GLC-82). The models of mice S-180 sarcoma and HepS were used for in vivo antitumor test. RESULTS: The IC50 of anuoning on CNE2, bel-7402, HT-29, SUNE1 cell were 0.044, 0.068, 0.446, and 1.617 micrograms/ml, respectively. The IC50 of anuoning on MCF-7 cell and GLC-82 cell were 1.857 and 3.481 micrograms/ml, respectively. Under the doses of 15, 30, and 60 micrograms/kg, i.p., qd x 10 d, the average tumor inhibitory rates of anuoning to mice tumor HepS were 36.9%, 51.8%, and 57.9%, respectively (P < 0.05). Under the same concentration, the average tumor inhibitory rates of anuoning on mice S-180 sarcoma were 43.0%, 52.1%, and 61.0%, respectively (P < 0.05). CONCLUSIONS: The results indicate that the anuoning possess cell growth inhibition activity to various human tumor cells in vitro and antitumor effect in vivo.

Involvement of caspase-3 activation in squamocin-induced apoptosis in leukemia cell line HL-60.

Annonaceous acetogenins have potent antitumor effect in vitro and in vivo. Squamocin is one of the annonaceous acetogenins and has been reported to have antiproliferative effect on cancer cells. Our results from this study showed that squamocin inhibited proliferation of HL-60 cells with IC50 value of 0.17 microg/ml and induced apoptosis of HL-60 cells. Investigation of the mechanism of squamocin-induced apoptosis revealed that treatment of HL-60 cells with squamocin resulted in extensive nuclear condensation. DNA fragmentation, cleavage of the death substrate poly (ADP-ribose) polymerase (PARP) and induction of caspase-3 activity. Pretreatment of HL-60 cells with caspase-3 specific inhibitor DEVD-CHO prevented squamocin-induced DNA fragmentation, PARP cleavage and cell death. The expression levels of protein bcl-2, bax have no change in response to squamocin treatment in HL-60 cells, whereas stress-activated protein kinase (SAPK/JNK) was activated after treatment with squamocin in HL-60 cells. These results suggest that apoptosis of HL-60 cells induced by squamocin requires caspase-3 activation and is related to SAPK activation.

[Inhibition of oxygen consumption by annonaceous acetogenins in liver cell respiration and their structure-activity relationship].

AIM: To study the inhibition of oxygen consumption by annonaceous acetogenins (ACG) and their structure-activity relationship (SAR). METHODS: The inhibition of oxygen consumption in chicken liver cell respiration by different structural ACG was studied by using oxygen electrode technique. RESULTS: Six ACG showed potent inhibitory effects like rotenone which was a classical inhibitor of mitochondrial complex I, and was more potent than complex IV inhibitor KCN. The IC50 values of six ACG for inhibiting oxygen consumption suggested that bistetrahydrofuran (THF) ACG was 7-11 times more active than non-THF ACG, and A1-type ACG was more potent than A2-type ACG. CONCLUSION: The terminal gamma-lactone was crucial for the inhibition of oxygen consumption. The distance between THF and gamma-lactone, the hydroxyl groups in the alkyl chain, were the important factors of SAR, but the 4-OH group possibly played some negative role in the exhibit of potent activity.