3,5-Bis(benzylidene)-1-[4-2-(morpholin-4-yl)ethoxyphenylcarbonyl]-4-piperidone hydrochloride: a lead tumor-specific cytotoxin which induces apoptosis and autophagy.

A number of N-4-(2-aminoethoxy)phenylcarbonyl derivatives of various 3,5-bis(benzylidene)-4-piperidones 2-5 demonstrated noteworthy cytotoxic potencies towards human HL-60 leukemic cells as well as human HSC-2 and HSC-4 squamous cell carcinomas. In general, toxicity towards HGF, HPC, and HPLF normal cells was substantially lower. The highest selective toxicity was noted when the terminal base is morpholine.

Non-apoptotic cell death induced by nutritional starvation in J774.1 mouse macrophage-like cell line.

The growth and amino acid utilization of a mouse macrophage-like cell line J774.1 was investigated in two different culture media supplemented with 10% fetal bovine serum (FBS). The J774.

Tumor-specific cytotoxicity and type of cell death induced by gefitinib in oral squamous cell carcinoma cell lines.

Gefitinib is an orally active, selective epidermal growth factor receptor-tyrosine kinase inhibitor. The present study was aimed at evaluating the antitumor activity of gefitinib alone or in combination with other antitumor agents. Gefitinib showed higher cytotoxicity against five human tumor cell lines (HSC-2, HSC-3, HSC-4, T98G and U87MG) than against three human normal oral cells (gingival fibroblast HGF, pulp cell HPC and periodontal ligament fibroblast HPLF).

Estimation of relationship between structure of newly synthesized dihydroimidazoles determined by a semiempirical molecular-orbital method and their cytotoxicity.

A semiempirical molecular-orbital method (CAChe 4.9, PM5) was applied to delineate the relationship between the cytotoxicity (evaluated by 50% cytotoxic concentration, CC(50)) of twelve dihydroimidazole derivatives, their molecular weight and the eleven chemical parameters (descriptors) determined by CONFLEX/PM5 method. There was no correlation between the CC(50) value and heat of formation, dipole moment, E(HOMO), E(LUMO), absolute hardness (eta), absolute electron negativity (chi), reaction index (omega), length of substituted group in all cell lines tested.

A clinical pilot study of lignin--ascorbic acid combination treatment of herpes simplex virus.

Antiviral drugs as well as natural remedies have been used to reduce symptoms and the rate of recurrences of herpes simplex virus type 1 (HSV-1) infection, a common disease. To evaluate anti-HSV-1 activity of a pine cone lignin and ascorbic acid treatment, a clinical pilot study was carried out. Forty-eight healthy patients of both genders between 4 and 61 years old (mean: 31+/-16 years), with active lesions of HSV-1, took part in the study.

Triterpene glycosides from the whole plant of Anemone hupehensis var. japonica and their cytotoxic activity.

Three new triterpene glycosides (1-3), together with eight known triterpene glycosides (4-11), were isolated from the whole plant of Anemone hupehensis var. japonica (Ranunculaceae). The structures of the new compounds were determined on the basis of spectroscopic analysis and the results of hydrolytic cleavage experiments.

Amurensiosides A-K, 11 new pregnane glycosides from the roots of Adonis amurensis.

Five new pregnane tetraglycosides, amurensiosides A-E (1-5), two new pregnane hexaglycosides, amurensiosides F (6) and I (9), two new 18-norpregnane hexaglycosides, amurensiosides G (7) and H (8), and two new pregnane octaglycosides, amurensiosides J (10) and K (11), were isolated from the MeOH extract of the roots of Adonis amurensis. The structures of the new compounds were determined on the basis of extensive spectroscopic analysis, including two-dimensional (2D) NMR data, and the results of hydrolytic cleavage. The isolated compounds were evaluated for their cytotoxic activity against HSC-2 human oral squamous cell carcinoma cells.

[Effect of anesthetics on malignant tumor cells (A review)].

The influence of surgery and anesthesia on aspects of malignant tumor has received considerable attention in recent years. It is suggested that in vitro studies, clinically available anesthetics, such as intravenous anesthetics, local anesthetics and opioids have, more or less, possible antitumor potential against human malignant tumor cells. Although natural killer (NK) cells play an important role in tumor and metastasis surveillance, the reported effects of the anesthetics on the NK cell activity in human are controversial.

Steroidal glycosides from Furcraea foetida and their cytotoxic activity.

Two new spirostanol glycosides (1, 2) and a new furostanol glycoside (3), together with nine known steroidal glycosides (4-12) were isolated from the leaves of Furcraea foetida (Agavaceae). The structures of the new compounds were determined by spectroscopic analysis and the results of hydrolytic cleavage. The isolated compounds were evaluated for their cytotoxic activities against HL-60 human leukemia cells, A549 human lung adenocarcinoma cells, HSC-2 human oral squamous carcinoma cells, and HSC-4 human oral squamous carcinoma cells.

Chemical constituents of the bulbs of Habranthus brachyandrus and their cytotoxic activities.

The bulbs of Habranthus brachyandrus (Amaryllidaceae) have been extensively analyzed for their chemical constituents, resulting in the isolation of eight flavan derivatives (1-8), four of which are new naturally occurring compounds; a new hydroxybutyric acid glucoside (9); three known phenolic compounds (10-12); and six known alkaloids (13-18). The structures of the new compounds were determined on the basis of spectroscopic analysis, including two-dimensional (2D) NMR data, and chemical evidence. The isolated compounds and a few derivatives were evaluated for their cytotoxic activities against HL-60 human promyelocytic leukemia cells and HSC-2 human oral squamous cell carcinoma cells.

Effect of Sasa senanensis Rehder extract on NO and PGE2 production by activated mouse macrophage-like RAW264.7 cells.

Alkaline extract of Sasa senanensis Rehder (SE) has shown diverse biological activity. As an extension, whether SE affects the function of activated macrophages was investigated. SE inhibited the nitric oxide (NO) production by lipopolysaccharide (LPS)-activated mouse macrophage-like RAW264.

Inhibition of NO production in LPS-stimulated mouse macrophage-like cells by benzo[b]cyclohept[e] [1,4]oxazine and 2-aminotropone derivatives.

The aim of this study was to investigate whether a total of twenty benzo[b]cyclohept[e][1,4]oxazines and their S-analogs, and 2-aminotropone derivatives affect the function of activated macrophages. These compounds inhibited the production of pro-inflammatory substances such as nitric oxide (NO) by lipopolysaccharide (LPS)-activated mouse macrophage-like RAW264.7 cells to different extents.

Antitumor potential of three herbal extracts against human oral squamous cell lines.

Three Chinese herbal extracts of Drynaria baronii, Angelica sinensis and Cornus officinalis Sieb. et Zucc (referred to as DB, AS, CO, respectively) were investigated for their antitumor potential. These extracts showed very weak cytotoxicity against all nine cultured human cells (normal and tumor cells), but with some tumor-specific cytotoxicity displayed by DB and CO.

Tumor-specific cytotoxic activity of 1,2,3,4-tetrahydroisoquinoline derivatives against human oral squamous cell carcinoma cell lines.

The tumor-specific cytotoxicity and the type of cell death induced by thirty-eight newly synthesized tetrahydroisoquinoline derivatives in human oral squamous cell carcinoma cell lines were investigated. 6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)(3,4-dimethoxyphenyl) methanone that has bulky substituents (such as 3,4-dimethoxybenzoyl group) (TQ9) and ethyl 2-benzyloxycarbonyl-1,2,3,4-tetrahydroisoquinoline-1-carboxylate that has ethoxycarbonyl group and benzyloxycarbonyl group (TD13) showed the highest tumor-specific cytotoxicity (TS=12.5 and 5.

Triterpene glycosides from the tubers of Anemone coronaria.

Six new triterpene glycosides (1-6), together with 11 known ones (7-17), have been isolated from a glycoside-enriched fraction prepared from the tubers of Anemone coronaria L. (Ranunculaceae). On the basis of extensive spectroscopic analysis, including 2D NMR data, and the results of hydrolytic cleavage, the structures of 1-6 were determined to be 3beta-[(O-beta-D-glucopyranosyl-(1-->4)-O-[alpha-L-rhamnopyranosyl-(1-->2)]-alpha-L-arabinopyranosyl)oxy]-2beta,23-dihydroxyolean-12-en-28-oic acid (1), 3beta-[(O-beta-D-glucopyranosyl-(1-->3)-O-alpha-L-rhamnopyranosyl-(1-->2)-O-[beta-D-glucopyranosyl-(1-->4)]-alpha-L-arabinopyranosyl)oxy]-23-hydroxyolean-12-en-28-oic acid (2), 3beta-[(O-beta-D-glucopyranosyl-(1-->4)-O-[alpha-L-rhamnopyranosyl-(1-->2)]-alpha-L-arabinopyranosyl)oxy]-23-hydroxyolean-12-en-28-oic acid O-beta-D-glucopyranosyl-(1-->6)-beta-D-glucopyranosyl ester (3), 3beta-[(O-beta-D-glucopyranosyl-(1-->4)-O-[alpha-L-rhamnopyranosyl-(1-->2)]-alpha-L-arabinopyranosyl)oxy]-2beta,23-dihydroxyolean-12-en-28-oic acid O-alpha-L-rhamnopyranosyl-(1-->4)-O-beta-D-glucopyranosyl-(1-->6)-beta-D-glucopyranosyl ester (4), 3beta-[(O-beta-D-glucopyranosyl-(1-->4)-O-[alpha-L-rhamnopyranosyl-(1-->2)]-alpha-L-arabinopyranosyl)oxy]-2beta-hydroxyolean-12-en-28-oic acid O-alpha-L-rhamnopyranosyl-(1-->4)-O-beta-D-glucopyranosyl-(1-->6)-beta-D-glucopyranosyl ester (5), and 3beta-[(O-beta-D-glucopyranosyl-(1-->4)-O-[alpha-L-rhamnopyranosyl-(1-->2)]-alpha-L-arabinopyranosyl)oxy]-23-hydroxyolean-18-en-28-oic acid O-alpha-L-rhamnopyranosyl-(1-->4)-O-beta-D-glucopyranosyl-(1-->6)-beta-D-glucopyranosyl ester (6), respectively.

Re-evaluation of anti-inflammatory activity of mastic using activated macrophages.

Mastic is a resinous exudate obtained from the stem and the main leaves of Pistacia lentiscus. Mastic has shown several beneficial pharmaceutical properties such as antibacterial and apoptosis-modulating activities. The aim of this study was to investigate whether mastic affects the function of activated macrophages.

Effect of Scutellariae radix ingredients on prostaglandin E(2) production and COX-2 expression by LPS-activated macrophage.

We previously reported that Sairei-to concentration-dependently modified lipopolysaccharide (LPS)-stimulated prostaglandin E(2) (PGE(2)) production in mouse macrophage-like RAW264.7 cells. Among twelve major ingredients of Sairei-to, Scutellariae radix inhibited the LPS-stimulated PGE(2) production to the greatest extent, followed by Zingiberis rhizoma, Glycyrrhizae radix, Atractylodis lanceae rhizoma and Pinelliae tuber.

Effect of three herbal extracts on NO and PGE2 production by activated mouse macrophage-like cells.

Three Chinese herbal extracts, Drynaria baronii, Angelica sinensis and Cornus officinalis Sieb. et Zucc (referred to as DB, AS, CO, respectively), were investigated for their possible anti-inflammatory activity. DB, AS and CO inhibited nitric oxide (NO) production by lipopolysaccharide (LPS)-activated mouse macrophage-like RAW264.

Estimation of relationship between the structure of 1,2,3,4-tetrahydroisoquinoline derivatives determined by a semiempirical molecular-orbital method and their cytotoxicity.

A semiempirical molecular-orbital method (CAChe 4.9, PM5) was applied to delineate the relationship between the cytotoxicity (evaluated by 50% cytotoxic concentration, CC(50)) of nineteen 1,2,3,4-tetrahydroisoquinoline derivatives, their molecular weight and the sixteen chemical parameters (descriptors) determined by CONFLEX/PM5 method. There was little or no correlation between the CC(50) in HL-60 cells and the heat of formation, stability of hydration (DeltaH), dipole moment, electron affinity, ionization potential, highest occupied molecular orbital energy (E(HOMO)), lowest unoccupied molecular orbital energy (E(LUMO)), absolute hardness (eta, softness and hardness of the molecule) or molecular weight (r(2)<0.

Advantages of second line estramustine for overall survival of hormone-refractory prostate cancer (HRPC) patients.

There is no effective standard therapy for the treatment of hormone-refractory prostate cancer (HRPC), and treatments vary among different medical institutions with efforts to improve results. The present retrospective investigation was performed to assess the outcomes of second line, third line, and fourth line therapies. A total of 142 patients with HRPC were treated at Nagoya City University Hospital and its affiliate hospitals during the 10 years between October 1996 and August 2006.

2-(3-Aryl-2-propenoyl)-3-methylquinoxaline-1,4-dioxides: a novel cluster of tumor-specific cytotoxins which reverse multidrug resistance.

A series of 2-(3-aryl-2-propenoyl)-3-methylquinoxaline-1,4-dioxides 3a-l were prepared by condensation of various aryl aldehydes with 2-acetyl-3-methylquinoxaline-1,4-dioxide 2. These compounds inhibit the growth of human Molt 4/C8 and CEM T-lymphocytes and the IC(50) values are mainly in the 5-30 microM range. The quinoxaline 1,4-dioxide 3j inhibited the growth of 58 human tumor cell lines, particularly leukemic and breast cancer neoplasms.

Effect of simulated orthodontic forces on fluoride-induced cytotoxicity in MC3T3-E1 osteoblast-like cells.

The effects of simulated orthodontic forces such as centrifugal force or water pressure on sodium fluoride (NaF)-induced cytotoxicity against mouse osteoblast-like cells MC3T3-E1 were investigated. Loading with centrifugal force (44.5 g/cm2) or water pressure (5 g/cm2) slightly reduced the cell proliferation and additively enhanced the cytotoxic activity of millimolar concentrations of NaF.

Selective antibacterial and apoptosis-modulating activities of mastic.

Mastic is a resinous exudate obtained from the stem and the main leaves of Pistacia lentiscus. We have reported the antiplaque effect of mastic-containing chewing gum on the oral cavity. We hypothesize that mastic may be a multifunctional food which has some beneficial pharmaceutical properties.

Declined asparagine synthetase mRNA expression and enhanced sensitivity to asparaginase in HL-60 cells committed to monocytic differentiation.

During 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced differentiation of human promyelocytic leukemia HL-60 cells toward maturing monocytes/macrophages, asparagine synthetase (ASNS) mRNA expression declined time and dose-dependently. The effect of TPA was inhibited by inhibitors for PKC and MEK 1/2, but not by those for JNK and p38 MAPK. Combination treatment with TPA and asparaginase synergistically enhanced the growth retardation accompanied by apoptotic cell death characterized by internucleosomal DNA fragmentation.