A new component of antitumor action TG has been isolated from the ethyl acetate extract of Tripterygium wilfordii (besides Triptolide, Tripdiolide and Triptonide). TG was shown in this study to have obvious antitumor effects. The average life span of H22, S180, EAC and breast carcinoma-bearing mice treated with TG ip x 2 days were 100% more than those of the control mice (P less than 0.01) TG was able to inhibit tumor growth of S37-bearing mice at the dose of 150 mg/kg per day, ig x 3, its inhibitory rate was 42% (P less than 0.01). TG could also inhibit squamous epithelial lung carcinoma induced by 3-methylcholanthrene. The inhibitory rate was 65.13% (P less than 0.05). TG had remarkable killing effect on human HL60 and Daudi cells and two direction effects on function M phi of mouse abdominal cavity in vitro.

Using mutational and anti-mutational synchronous in SOS inductest (+/- S9), We found that 7 out of 11 kinds of commonly eaten vegetables had the ability to inhibit mutagenicity caused by chemical drugs such as Mitomycin C, Bleomycinia, Fluorouracil, Cis-Diaminodichloroplatinum, Arabinosylcytosin and mustargen, They were garlic, green Chinese onion, onion, garlic bulb, tomato, cucumber and water radish. The other 4 lacking this ability were rape, chinese toon, ginger and asparagus lettuce stalk. We believe that our results can be helpful in the preparation. of cancer patients' diet, who are receiving chemotherapy and in the prevention of cancer.

Chemosensitivity testing of adenocystic, tongue and gingiva cancer cell lines to 14 antitumor drugs using a tetrazolium-based colorimetric assay (MTT assay) was carried out and the values of the relative antitumor activity (RAA) of the drugs were compared. Adriamycin (ADM), methotrexate (MTX) and fluorouracil (5-FU) showed the most potent RAA against the cell lines while Cantharidin (CTD) did not show RAA. The rank orders of other 10 drugs against each cell line differed from each another.

Two new compounds hancogenin B (V) and hancoside A (VI) and four known compounds glucogenin C (I), cynatratoside A (II), glaucogenin A (III) and anhydrohirundigenin (IV) were isolated from the roots of Cynanchum hancockianum (Maxim) Al. Iljinski. Their structures were identified on the basis of spectral evidence. The fragmentation ways of 13:14, 14:15-secopregnenes in EIMS were outlined and the antitumor activity of II and the antiendotoxic activity of VI were also preliminarily tested in vitro.

C1027, a new macromolecular peptide antitumor antibiotic produced by Streptomyces globisporus C1027, shows extremely potent cytotoxicity to cultured cancer cells. The antibiotic is composed of an apoprotein and a chromophore and the latter serves as the active part of the compound. C1027 was separated into apoprotein and chromophore by methanol extraction and the separated parts can be reconstituted to form the active C1027 molecule in phosphate buffer. For determination of the specificity of C1027 reconstitution, the apoprotein was incubated with epirubicin and the chromophore was incubated with H16, a McAb directed against hepatoma cells. Notably, the reconstitution of C1027 occurred neither between apoprotein and epirubicin nor between chromophore and IgG molecule. In addition, bovine serum albumin showed no competition with C1027 apoprotein in binding to the chromophore. Various methods for linking C1027 to McAb were studied and two kinds of immunoconjugates have been prepared: (1) direct conjugate was made by linking C1027 to McAb, using SPDP as a linker agent, (2) assembled conjugate was made by linking and reconstitution, including 3 steps. Firstly, the chromophore was extracted with methanol and stored at -70 degrees C in drak. Secondly, the apoprotein was conjugated to McAb by SPDP and finally the extracted chromophore was added to the McAb-apoprotein conjugate. Determined by clonogenic assay, the IC50 values for hepatoma cells were 42 pmol/L, and 5.5 pmol/L, respectively, for direct conjugate and assembled conjugate. The IC50 value of M3-C1027 assembled conjugate prepared by linking the irrelevant McAb M3 to C1027 was 1,400 pmol/L.(ABSTRACT TRUNCATED AT 250 WORDS)

Arteannuin B (I) was converted to hydroxy lactones (VII, VIII) by a mixture of formic acid and sulfuric acid. Compound VI and Compound VII both showed activity against leukemia P 388 cell in vitro. The rate of growth inhibition were 97.5% and 11.8% for (VI) and 80% and 52.6% for (VII) at the concentration of 10 and 1 micrograms/ml respectively. It seems that the antileukemia activity of 6-membered lactone is higher than that of 5-membered and the methylene group is necessary for the antileukemia activity.

Twelve compounds were isolated from Annona squamosa. Their structures were identified as liriodenine (AS-1), moupinamide (AS-2), -(-)-kauran-16 alpha-ol-19-oic acid (AS-3), 16 beta, 17-dihydroxy-(-)-kauran-19-oic acid (AS-4), anonaine (AS-5), 16 alpha, 17-dihydroxy-(-)-kauran-19-oic acid (AS-6), (-)-isokaur-15(16)-en-17,19-dioic acid (AS-7), squamosamide (AS-8), 16 alpha-methoxy-(-)-kauran-19-oic acid (AS-9), sachanoic acid (AS-10), (-)-kauran-19-al-17-oic acid (AS-11), daucosterol (AS-12). Among them, AS-8 is a new amide, AS-9 is a new natural product.

The biotransformation of etheofazine (EDMTP), a new anticancer drug, was studied by using isolated perfused rat liver. Two main metabolites were separated from the perfusate by HPLC and TLC and their chemical structures were determined by MS, 1H-NMR and IR. EDMTP-I is the parent compound. EDMTP-II is 7-ethyl-8-aminotheophylline. EDMTP-II was also separated and identified from the blood of mice after iv of 10 mg/kg. Species difference of biotransformation of EDMTP between rat and mouse seems to be not significant in this study.

Some beta-germanyl-alpha-amino acid derivatives were prepared from the reaction of HGeCl3 with substituted oxazolines. The compositions of the above compounds were studied using IR, element analysis and so on. Experimental results were as follows: for 1-substituted-2-amino-2-carboxyethylgermanium susquioxide (such as IIIb), the po LD50 for mice was found to be above 10 g/kg. When given ip, a maximum inhibition of 50% of the growth of S180 was obtained for IIIb, whereas an inhibition of 42% was achieved for 5-Fu under the same experimental condition.

Pseudohainanensine (HH08) is a synthetic compound which is active against L-1210. In order to study the pharmacokinetic characteristics of this compound in rats, 3', 4'-dideuteropseudohainanensine (DH08) was synthesized and used as internal standard in GC-MS determination for quantitative analysis of alkaloid HH08 in the blood of rats that had been given HH08 at a dosage of 10 mg/kg intravenously. Experiments demonstrated that the detection limit of HH08 was 3 micrograms/ml and the peak concentration in the blood was 13.1 +/- 0.2 micrograms/ml after a single intravenous injection (one min. after injection). The biological half life time can be divided into two phases; the fast phase (alpha) 2.61 min, and the slow phase (beta) 42.59 min. Two hours after the injection no drug could be detected in the blood.

There are only a few reports in the literature on photodynamic effects of HPD on gene expression and the repair of DNA damage. Previously, we suggested that nuclear transcription activity was markedly suppressed by HPD plus light. In this study, we investigated the photodynamic effect or DNA repair synthesis as measured by unscheduled DNA synthesis (UDS) in hepatoma cells. The results indicated that DNA repair capacity was greatly inhibited by HPD plus light. When hepatoma cells were pretreated with HPD of different concentrations and then exposed to the same light dose, significant inhibitions of UDS over control were seen and appeared in a dose-dependent fashion. In addition, while hepatoma cells following the exposure to HPD of the same concentration were irradiated with different time, the UDS was markedly decreased as the duration of irradiation was prolonged. However, no changes were observed when either HPD or light was used alone. The present study also included an experiment to determine whether HPD combined with vitamin C gives an enhanced photosensitization. It was found that vitamin C significantly potentiated the suppressing effect on DNA repair synthesis.

The interaction between (HPD) photodynamic therapy and 4 cytotoxic drugs on human gastric poorly differentiated mucinous adenocarcinoma cell line MGc 80-3 was studied. As the cells were blocked by 4 cytotoxic drugs (vincristine, mitomycin, bleomycin A5 and 5-Fluorouracil) in different phases, HPD was located in different sites in these cells. The photodynamic effect was potentiated when the cytotoxic drugs were administered before but not after the application of HPD plus light. The synchronous cells would absorb HPD more than the asynchronous cells.

As a continuing part of our study on the chemistry and antitumor activity of podophyllotoxin, 11 new C-4 S-substituted podophyllotoxin derivatives were synthesised and screened in vitro against L1210 leukemia and KB cells. Thus, 4'-demethylepipodophyllotoxin was reacted with thiols in the presence of BF3. Et2O or trifluroacetic acid to give thioethers. In addition, 4-bromo-4-deoxy-4'-demethylepipodophyllotoxin, when reacted with thiols, also gave rise to corresponding thioether (4-alkylthio-4-deoxy-4'-demethylepipodophyllotoxins). Compounds 10 and 12 have the same activity as etoposide in the inhibition against L1210 leukemia, and compounds 9, 10, 12 and 15 also have comparable activity with etoposide against KB cells.

Parasitic blood supply in 85 patients with hepatic carcinoma was demonstrated by selective angiography and CT. The hepatic carcinomas in the posterior segment of the right hepatic lobe and the lateral segment of the left hepatic lobe were partially fed by the inferior phrenic arteries in 48 patients. The hepatic carcinomas in the inferior portion of the right hepatic lobe were partially fed by the omental arteries in 37 patients. The development of parasitic blood supply depends more upon the location of the tumor than the occlusion of hepatic artery. Although the hepatic artery is occluded, the tumor may still receive blood supply from its parasitic arteries and continue to grow steadily. Therefore, in patients with double arterial blood supply, transcatheter double arterial (hepatic artery and parasitic arteries) infusion and embolization (TDAIE) should be applied for treatment. TDAIE was used in 33 of 85 cases and the preliminary result was quite satisfactory.

The purpose of this paper is to observe the blocking effect of topically subepithelial injected drug and Vit A acid painting on chemically induced oral precancerous lesion and to prove, on a certain extent, the hypothesis that subepithelial connective tissue could exert great influence on the differentiation of the epithelium. A total of 49 syrian hamster was used as experimental animal. Both buccal pouches of all animals were painted thrice weekly with 0.5% DMBA in acetone for 6 weeks. Then, they were divided into two groups: Control group and Experimental group. In the latter group, 70.8% precancerous lesions turned into normal epithelial tissue, whereas those untreated animals developed carcinoma by 62%.

Liposomes encapsulating homoharringtonine were prepared using soybean phospholipids, egg yolk phospholipids and phospholipids from human red cell membrane, respectively. The quantity of homoharringtonine encapsulated by phospholipids from human red cell membrane was greater than that encapsulated by the other two types of liposomes, so this kind of phospholipid was used for further studies. The liposomes containing homoharringtonine (HH) were covalently coupled with HI30 (CD45). The mixture was separated by gel column chromatography. HI30-HH-liposomes demonstrated a sensitive targeting function with an immune activity equal to that observed with original HI30 in indirect immunofluorescence tests using the human cell line CEM-M3.