To study the internalization law of immunotargeting drug for hepatocellular carcinoma and its significance.

To detect DNA damage caused by fotemustine (Fot).

Using Video Enhancement Contrast (VEC) microscopy, we recorded the morphological changes of same HL-60 cell in the processes of apoptosis induced by harringtonine. Our results show that all of apoptotic cells need several nucleus blebs before their chromatin condensation. Every nucleus bleb is induced by a relative membrane bleb. The number of membrane blebs is much higher than that of nucleus blebs, so there are only some of membrane blebs which can induce nucleus blebs. It suggested that membrane and nucleus blebs probably are related to apoptotic chromatin condensation. After HL-60 cells pretreated with cytochalasin B(CB), apoptotic chromatin condensation delayed eight hours, but no membrane bleb, nucleus bleb and apoptotic body formed eventually. So membrane and nucleus blebs during apoptosis are related to microfilament re-organization and can accelerate apoptotic chromatin condensation, but are unnecessary for apoptotic chromatin condensation. All this suggested that nuclear changes and cytoplasmic changes during HL-60 cell apoptosis are independent.

Vitamin A and its analogus, the retinoids, are agents that are known to induce differentiation and inhibit growth on cell in vitro and in vivo. These agents show promise as prophylactic and therapeutic ones in human cancer and were noted extensively by scholars abroad, but the research has just been developed in recent years in our country. Retinamide (named briefly R II), a kind of new retinoids made in China, can induce differentiation and inhibit growth of cell, but its toxic effect is smaller than its maternal chemical compound (retinoic acid). Using automatic image analysis technology, polyacrylamide gel LDH isoenzyme electrophoresis, radioimmunoassay and condensing reaction of Con A, we have observed induction of differentiation of the R II on SGC-7901 cells. Our experiments indicate that R II can inhibit cell proliferation, decrease obviously average DNA content and nuclear area, reduce CEA secretion and condensing of the cells, and change LDH isozymoraphy of SGC-7901 cell with promoting H-type LDH and reducing M-type LDH. The change of morphology under light microscope by R II showed that the cells spread, flattened and partially lined up, and the alkalophilic quality of cytoplasm became weak. These results suggest that SGC-7901 cell under the action of R II should undergo the changes of reverse differentiation in morphological, physiological and bio-chemical aspects.

Antitumor-I (AT-I) is known as an effective traditional Chinese medicine to be used in combination with chemotherapeutic agents against tumor. It was demonstrated that AT-I could inhibit tumor growth and modulate IL-2, IL-6 and NK cell activities. In order to improve its preparation, we got the alcohol extract from AT-I (AEA-I) by using natural pharmaceutical alcohol extract method, and compared the effect of AEA-I on cytokins with that of AT-I. The results show that AEA-I has a good positive correlation with AT-I on IL-2 and IL-6 activities of mice in vivo.

Retinoids are capable of modulating cellular differentiation and proliferation. Retinoids mediate gene function through a series of nuclear receptors. The retinoic acid receptor beta (RAR beta) has been shown to play an important role in the differentiation of a number of cell types. RAR beta is either absent or expressed at extremely low levels in a number of tumor types including breast carcinoma. It was demonstrated that transfection of RAR beta gene in breast carcinoma cell with its subsequent expression resulted in inhibition of cell growth. Retinoic acid significantly inhibited monolayer growth of the breast carcinoma cells expressing RAR beta, while it had no effect on the growth of the control cells. The RAR beta expressing cells formed much smaller and fewer colonies in soft agar and were significantly less tumorigenic in nude mice than the controls. These results suggest that RAR beta may function as a tumor suppressor in breast carcinoma cells.

Amsacrine (AMSA) was a high effective medicine of acute leukemia treatment. But it could lead to severe phlebitis with venous drip. 44 patients were treated 71 courses with AMSA. After we used fasting venous drip and diluting high concentration AMSA, occurrence of phlebitis remarkably decreased and patients of phlebitis could be cured with early comprehensive nursing.

The reasons for poor appetite and nutritional disorder in cancer patients were analyzed in this study. It is concluded that special emphasis should be put on nutritional support by both doctors and patients as early as possible. Clinical practices evidence showed that through parenteral or enteral nutrition supporting according to the patients' condition, not only enhance the patients' endurance to antineoplastic therapy but also improve their quality of life.

To conduct preclinical studies and phase I trial of the recombinant human granulocyte-macrophage colony-stimulating factor (rhGM-CSF).

The technology for processing steamed Garcinia hunburyi with high pressure was synthetically selected by using orthogonal experiment design, based on the indexes of anti-inflammatory, bacteriocidal, anti-tumour effects and gambagic acid content. The result shows that the best way is to steam for 0.5 h at 126 degrees C.

During the treatment with all-trans retinoic acid (ATRA) for acute promyelocytic leukemia (APL), leukocytosis occured in 33%-75% of the treated cases. ELISA method was used in detecting levels of serum granulocyle colony-stimulating factor (G-CSF) in 47 cases of APL during treatment with ATRA. It was found that the peak of increased serum G-CSF level occurred on the 9th day, and WBC number was highest on the 11th day. After ATRA treatment, both serum G-CSF level and WBC number increased in 68.1% of the cases. In 19.2% of the cases treated, serum G-CSF level was increased but without obvious change in WBC number, and the reverse was true in 12.7% of the cases. Serum G-CSF level was statistically correlated to the number of WBC, promyelocytes and its late stage by Spearman rank correlation analysis.

MTT assay was evaluated on cytoxicity for suspension growing cell lines of SO-Rb50 and SO-Rb70, and the toxicity of TAH (the total alkaloid of peqanum harmala L) on the above cell lines was assessed.

In an in vitro culture system of human cancer cells MCF-7 and its adriamycin-resistant line MCF-7/Ad or KB and its vincristine-resistant line KBv200, tetrandrine was found to exhibit significantly selective anticancer activity against the drug-resistant cancer cell MCF-7/Ad. In addition, essentially complete reversal effects of tetrandrine on drug resistance were observed in MCF/Ad or KBv200.

The different processes for preparing gamboge could influence its bactericidal activity and cytotoxicity. The gamboge processed with high pressure steam has been proved the most powerful in killing Staphylococcus aureus and tumor cells. The most suitable condition for processing gamboge is to steam it at 126 degrees C for 30 minutes.

From March 1994 to March 1995, 14 cases of refractory advanced breast cancers were treated with Navelbine (NVB). NVB as a single agent was given weekly 40-60mg (24.9mg-33.3 mg/m2), every 2 weeks for one cycle. Six of fourteen cases (42.9%) achieved partial response (PR). The median remission duration of PR patients was 5 months (range 2-10 months). NVB was given 85 times, the main side effects were myalgia and arthralgia (80.0%), phlebitis (57.6%). Sixty-five of eighty five pretreatment WBC counts were below 4.0 x 10(9)/L, and the severity of leukopenia was related to pretreatment WBC level. No patient died of infection.

The expression and property of alkaline phosphatase (ALP) in Eca109 cells, a cell line derived from human esophageal carcinoma were studied with specific inhibition assay and poly-acrylamide gel electrophoresis. The results showed that ALP of Eca109 cells was heat stable and was strongly inhibited by L-phenyalanine, but slightly inhibited by urea. Prednisolone could cause dramatic increase in activity of ALP, but no change in ALP isozyme spectrum and concomitant increase in lactic dehydrogenase activity were found after prednisolone treatment. The results suggested that placental alkaline phosphatase as an oncofetal gene product could be expressed ectopically by Eca109 cells and prednisolone could specifically induce increase in its activity.

Elemene, isolated from the Chinese medicinal herb Rhizoma Zedoariae was shown to exhibit antitumor activity in vitro and in vivo to human and murine tumor cells. This novel antineoplastic agent has been demonstrated to have substantial clinical activity against various tumors. In this paper, the mechanisms of antitumor activity of elemene are reported. The in vitro effect of elemene on the growth of leukemia cells was evaluated by MTT assay. The IC50 values of elemene for promyelocytic leukemia HL-60 cells and erythroleukemia K562 cells were found to be 27.5 micrograms/ml and 81 micrograms/ml, respectively, while IC50 for peripheral blood leukocytes (PBL) was 254.3 micrograms/ml. The inhibitory effect of elemene on proliferation of HL-60 cells was associated with cell cycle arrest from, S to G2M phase transition and with induction of apoptosis. The apoptosis of tumor cells was confirmed by DNA ladder formation on gel electrophoresis and characteristic ultrastructural alternations. These results indicate that induction of apoptosis contributes to the mechanisms for antitumor activity of elemene.

From August 1993 to March 1994, 36 patients were enrolled for a phase I study of Boanmycin (Bleomycin A6) a new anticancer drug to determine it toxicity and maximal dose. Of the 36 cases, 16 were male and 20 female, age 20-62. Dose escalation was performed if a minimum of threed patients were fully evaluable for toxicity (2 weeks following drug administration) and if severe or life-threatening toxicity had not occurred. Dose of Boanmycin were escalated from 1 mg (0.5-0.7 mg/m2) to 12 mg(6.7-7.5 mg/m2) i. m. three times every week for two weeks. Surveillance of serum concentration of Boanmycin was conducted in six cases by microbiological analysis, and the pharmacokinetics parameters were obtained. Phase I study of Boanmycin showed that Boanmycin had no myelosuppression and cardiac toxicity, and its major adverse reactions were fever, gastrointestinal reactions and hardening at injection (by i. m. route). Rather than dose-related, fever was individual-related. There were mild myalgia, alopecia, skin rash, pigmentation in some patients. All adverse reactions resolved after discontinuation of therapy. There was no Boanmycin-related lethal complication, and the maximum tolerated dose was not obtainable. If patients have renal or lung disease, Boanmycin aggravate their renal and lung functions. Therefore we recommend that dose of Boanmycin for phase I clinical trial should be is 8-10 mg(5-6 mg/m2) i m or iv (iv can decrease local side effect) two-three times per week.

Experiments were conducted by using scrape-loading and dye transfer (SLDT) method to study the gap junction intercellular communication (GJIC) of Chinese hamster lung cells (V79), mouse fibrous cells (Balb/c-3T3), rat liver cells (WB) and human embryonal lung cells (2BS). We also observed the inhibition of the GJIC by TPA and the antagonistic effect of Curcumin derivatives on TPA. The results indicated that V79, WB, 3T3 and 2BS normal cells showed medium level of GJIC, and TPA could inhibit the GJIC to some extents. Curcumin derivatives (91022, 91022-S) could counteract the inhibition of TPA-induced GJIC. It was also found that human lung adenocarcinoma cell (A549) and GLC lacked GJIC, and 91022 could improve the GJIC of A549 cell. It may be related to its anticancer activity.