A prospective randomized trial in 64 esophageal cancer patients was conducted from 1986 to 1989. The patients were randomized into two groups-PPF (DDP 100 mg/m2 + pingyangmycin + 5-FU) regimen plus radiotherapy (combined group) or radiotherapy alone (control group). The overall response rate and CR rate in the combined group were 87.5% (28/32) and 40.6% (13/32). Those of the control group were 81.3% (26/32) and 21.9% (7/32), respectively. The overall response rates were similar in these two groups, but the CR rate in the combined groups was higher than that of the control group. The 1-year survival rates in the combined and control groups were 77.4% (24/31) and 45.2% (14/31) (p less than 0.01). The 2-year survival rates were 56.3% (9/16) and 34.6% (9/26), respectively (p greater than 0.05). Our preliminary results show that combined chemotherapy including high dose cisplatin and radiotherapy may improve the therapeutic result of esophageal cancer.

The effects of acupuncture and moxibustion on 376 cases of chemotherapy-induced leukocytopenia was observed in patients with malignant tumors in the intermediary and advanced stages. Findings revealed that the total effect in 121 cases (88.4%) occurred in the group treated with acupuncture and moxibustion with warming needle; while the total effect in 221 cases (90.9%) was in the group treated with moxibustion with ignited moxa cone. A comparison made between the 2 groups showed no significant difference (P greater than 0.05). The total effective rate was 38.2% when compared with the control group using batylalcohol and pentoxyl and so the difference was significant (P less than 0.01). Analysis found that with patients having higher basic WBC value, the effect would be higher. Conversely, those who had lower basic value in their WBCs, the expected effect would be lower. These findings suggest that acupuncture and moxibustion in raising the effect on the white cells were influenced by the extent to which the bone marrow was inhibited, having no relevance to the kind of disease, the chemotherapy regime, and the treatment course which the patient was in.

Our experiments have proved that human promyelocytic leukemia cells (HL-60) could be induced to differentiate in vitro by notoginsenoside R1 into mature neutrophils. The morphological results showed that 68% of HL-60 cells were differentiated in 80 microgram/ml inducer for 5 days, in which metamyelocytes were 32%, banded neutrophils 30% and segmented neutrophils 6% 3H-TdR and 3H-UR incorporate assay showed that notoginsenoside R1 effected synthesis of DNA and RNA while it induced differentiation of HL-60 cell. At 48 h, percent of incorporate inhibition was 26.32% with 3H-TdR and 18.57% with 3H-UR; at 72 h, 17.46% and 21.76%, respectively.

210 children with hemangiomas were treated by local injection of Bleomycin A5. Bleomycin A5 was effective in all patients with strawberry and mixed hemangiomas, 91.2% of patients with cavernous hemangiomas, 44.4% of patients with port-wine stain. There was no response in pampiniform hemangioma. The therapeutic mechanism, indications and complications of the new method for treatment of hemangioma are discussed.

Our studies show that the growth of transplantable chondrosarcoma in rats is inhibited significantly by N-4-(hydroxycarbophenyl) retinamide (RII) at a dosage of 50 mg/kg. RII show a weak ability to induce the differentiation of HL-60 cells at a concentration of 1 umol/L. However, most of the HL-60 cells were induced to differentiate along granulocyte lineage after exposure to RII (1 mumol/L) and S86019 (10 micrograms/ml). Flow cytometry studies indicated that the majority of HL-60 cells were arrested in G1 phase by RII plus S86019. Northern blot analysis clearly demonstrated that c-myc expression was inhibited after treating HL-60 cells with RII plus S86019 for 12 hours. Moreover, thymidylate synthetase mRNA transcription was inhibited in those differentiated cells.

We designed a new gelatin microsphere (GM, 65 micron in diameter), which could combine with mitomycin C and 131I. The test in vitro showed that the GM had excellent drug release effect. Hepatic arterial embolization was carried out in 6 dogs with 131I-MMC-GM. The dogs survived from 4 to 28 days before being killed. Scintigraphy indicated that high radioactivity was concentrated in the liver, but was very low in the blood and thyroid. Pathologic study found that the GM was trapped in hepatic arterioles. The GM was eliminated by foreign body giant cells and the lumen of arterioles was occupied by granulations 14-28 days after operation. 131I-MMC-GM is a multiple anticancer agent which can exert triple action of targeting chemotherapy, internal radiotherapy and arterial embolization.

We reported the results of hepatic artery ligation (HAL) and infusion (HAI) with chemotherapy in the treatment of 356 patients with nonresectable primary liver cancer (PLC). A comparison of data between the periods 1958-1977 (81 cases) and 1978-1989 (275 cases) revealed that remarkable improvement in survival in the latter period might be attributed to the accurate site of hepatic artery cannulation, long-term infusion with chemotherapy, and combined treatment with subsequent tumor resection. During 1978-1989, the 5-year survival rates of different treatment modalities were 0% in HAL (n = 36) alone, 7.9% in HAI (n = 67) alone, 24.4% in HAL + HAI (n = 112, with subsequent resection in 10 cases), 36.5% in HAL + HAI + radiation (internal and/or external) (n = 60, with subsequent resection in 19 cases). The results indicate that HAL + HAI + combined treatment might provide a hope for the prolongation of survival or even resection in some patients with nonresectable PLC.

A novel sesquiterpene lactone, versicolactone A, with 12-carbon ring skeleton, was isolated from the roots of Aristolochia versicolar S. M. Hwang. Versicolactone A, C15H20O2, colorless prisms, mp 130-132 degrees C, [alpha]6D +486 degrees (c 0.1276, CHCl3). Its structure was established by spectroscopic methods, mainly 2D-NMR (1H-1H COSY, 1H-13C COSY, COLOC), HRMS and metastable ion measurement.

Title compounds were synthesized by condensation of 5-chloro-2,4,6-triaminoquinazoline (8) with various substituted benzaldehydes to produce the corresponding Schiff bases, followed by reduction with NaBH4, II and III were obtained by formylation or nitrosation of I respectively. Primary screening for suppressive therapeutic effects against P. berghei in mice showed that eight of the twelve compounds produced 100% suppression when administered orally at dose of 20 mg/kg. The results against L1210 Leukemia cell and B16 melanoma cell in vitro exhibited potent inhibition. Among them four compounds were more active than MTX and SIPI 759. Further work is in process. Antibacterial tests in vitro showed that a number of compounds possessed moderate activities against Diplococcus pneumoniae.

Four bisbenzylisoquinoline alkaloids (I-IV) have been isolated from the roots of Cocculus trilobus DC. (Menispermaceae) growing wild in the mountainous areas of Zhejiang province. Their structures were established as isotrilobine (I), trilobine (II), isotrilobine-N-2-oxide (III) and nortrilobine (IV) on the basis of spectral analysis (UV, IR, HNMR,MS), physico-chemical constants and properties of the derivatives. III is a new alkaloid and IV was found from this plant for the first time.

The mechanism of enhancement of Bleomycin A5 antitumor activity by verapamil was explored by flow cytometry and tracing the radiolabelled bleomycin A5 in vivo. Verapamil was found to increase the G2 blocking effect of bleomycin A5 prominently in mouse S-180 and human HEP-2 cell lines. The distribution of 57Co-bleomycin A5 in mice bearing S-180 sarcoma was changed by verapamil and accumulation of the drug in tumor was increased. In contrast, the labelled drug in the lung was decreased. It seems that the effects of verapamil in enhancing the antitumor activity of bleomycin A5 are to increase the accumulation of the drug in tumor cells and enhance the G2 blocking effect of the drug in cell cycle.

From 1965 through 1989, a total of 1,382 cases of malignant trophoblastic neoplasms, were treated in our hospital. Colitis related to chemotherapy was observed in 110 cases. This toxic reaction was specific to 5-Fluorouracil treatment and may result in pseudomembranous colitis if improperly treated. Staphylococcus aureus or Clostridium difficile was the causative agent. For the early detection of this disease, it is necessary to monitor the bacteria flora in the smear of fecal substance. Vancomycin and Metronidazole together with lactobacillus preparation were given and proved to be effective in most cases. The mechanism of formation of pseudomembranous colitis, the causative agents and method of diagnosis and treatment were discussed.

The effect of bleomycin A5 (BLM) alone and along with calmodulin inhibitor N-(4-aminobutyl)-5-chloro-2-naphthalene sulfonamide (W-13) on the proliferation of S-180 cells in vitro were studied. IC50 of BLM alone to the cells was about 2.63 micrograms/ml, which was decreased to 1/3.8 and 1/9.5 of 2.63 micrograms/ml when plus W-13 1, 5 micrograms/ml respectively. The results indicated that nontoxic doses of W-13 enhanced the inhibition of cell proliferation under the condition of BLM 0.5-2.5 micrograms/ml. In colony forming test, the survival fraction of S-180 cells treated with BLM plus W-13 was decreased to 1/87-240 of the cells treated with BLM alone. The results suggest that W-13 can enhance antitumor activity of BLM in vitro and may be used as an enhancer of BLM in vivo.

Naphthoquinone pigment-LIII, an extract from Arnebia euchroma, could apparently inhibit the proliferation of stomach cancer cell line and esophagus cancer cell line. At the effective concentration of 5 micrograms/ml, the mitotic index and growth curve declined without showing any damage to human normal cells. At 5-10 micrograms/ml, the colony efficiency of cancer cells became significantly low. The anti-cancer effect of Naphthoquinone pigment-LIII might be related to its role of influencing the amount of RNA and ultrastructure of cancer cells which was discussed in this paper.

Verapamil (Ver), a calcium influx blocker, enhanced the cytotoxicity of bleomycin A5 (BLM) in cultured S-180 cells. IC50 of BLM to the cells was about 2.6 micrograms/ml when the cells were treated with BLM alone, but when the cells were treated with BLM plus Ver 1, 5, 10 micrograms/ml, the IC50 were 1/1.2, 1/5.2, 1/7.4 of the cells treated with BLM alone, respectively. In colony test, the survival fractions of the cells treated with BLM 20, 60, 100 micrograms/ml plus Ver 60 micrograms/ml were 1/7, 1/8, 1/11 of the cells treated with BLM alone, respectively. Ver enhanced the growth inhibitory actions of BLM in mice bearing S-180 sarcoma by 60% or over. The mean survival the growth inhibitory actions of BLM in mice bearing S-180 sarcoma by 60% or over. The mean survival time of the mice bearing S-180 ascites sarcoma treated with BLM plus Ver was prolonged 21% from that of the mice treated with BLM alone. The results suggest that Ver may be used clinically as an antitumor enhancer of BLM.

Effects of six derivatives of 5,6-diphenyl-pyridazin-3-one (DPP) on CMTC of Vero cells were studied by means of the tubulin indirect immunofluorescence technique. Results showed that the effects were different with different derivatives and dose-dependent. Although PD033 had been know to be potent in inhibiting microtubule assembly in vitro, it showed little effect on disturbing CMTC in vivo. Besides having the effects mentioned above, PD032 also induced the formation of free microtubules similar to those induced by taxol.

Pingyangmycin (PYM), produced by Streptomyces pingyangensis n. sp., was found to be identical to bleomycin A5. In the present study, a comparative observation was carried out in 10 human cancer cell lines. As determined by a colony-forming assay, the dose-response curves obtained from cells exposed to PYM for 1 h were of one type only: biphasic exponential. The sensitivities of these cells derived from different types of tumors, however, varied with a broad range of ID50 values (0.03-0.82 microgram/ml). A hepatoma cell line (BEL-7402) and three lines derived from squamous carcinomas of the esophagus (Eca109 and CaEs17) or the nasopharynx (CNE) were relatively sensitive (ID50 less than 0.20 microgram/ml) to PYM which is known to have clinical activity against these diseases. Two gastric adenocarcinoma cell lines (MGc80-3 and BGC-823) and a pulmonary adenocarcinoma cell line (SPC-A-1) appeared to be less sensitive to the drug, with ID50 values of 0.21-0.47 microgram/ml. PYM was 7-fold more effective against LTEP-78 cells derived from pulmonary squamous carcinoma as opposed to SPC-A-1 cells, resulting in a low ID50 value of 0.04 microgram/ml. However, PYM as a single agent has not yet received full evaluation in relation to this type of lung cancer. In contrast with other cell lines of squamous cancer origin, HeLa and CC-801 cells derived from uterine cervix carcinomas which have been evaluated as highly responsive to PYM had the highest ID50 values (greater than 0.70 microgram/ml).

In order to study the diagnostic and the therapeutic value of digital subtraction angiography (DSA) in portal hypertension, we performed arterioportography 68 times and hepatic venography 11 times on 52 cases with clinically suspected portal hypertension. Seven portal hypertension cases caused by hepatic cancer were treated with transcatheter hepatic artery infusion of anticancerous agent, and one with the stricture of inferior vena cava on hepatic segment was treated by balloon catheter dilatation. Our results showed that, DSA is a safe, reliable and advanced diagnostic technique for portal hypertension, it can also be used as a therapeutic measure in some cases.

Thirty cancer patients scheduled for intra-arterial catheterization for chemotherapy were premedicated with pethidine 1 mg/kg atropine 0.807 mg/kg and prochlorperazine 5 mg intramuscularly. Anesthesia was induced with 2 mg/kg propofol and maintained with continuous infusion of propofol at a rate of 12 mg/kg/h. Patients breathed room-air spontaneously through the whole course of anesthesia. Anesthesia was induced with 2 mg/kg propofol in all patients, then maintained successfully by using a mean infusion rate of 12.13 +/- 0.43 mg/kg/h propofol. They lost consciousness within 29.60 +/- 5.50 second. Two minutes after induction, there were significantly decreased in systolic pressure, diastolic pressure, stroke volume and cardiac output but heart rate did not change significantly. Blood pressure and cardiac output remained stable but lower than pre-anesthetic values during the rest of the anesthetic course. Arterial blood gas analysis confirmed the respiratory depression. Two minutes after induction, there were significantly decreased in PaO2, SaO2 and pH were noted. PaCO2 was increased significantly. Recovery from the anesthesia was rapid and uneventful. The average time required for the patients to sustain eye-opening and to answer questions were 9.20 +/- 1.79 min and 10.73 +/- 1.87 min respectively after discontinuing propofol injection. Transient restlessness occurred in one patient. No other post-operative complications were noted.

The effects of a novel antitumor antibiotic polyactin A (PA) on in vitro IL-2 production and IL-2 responsiveness of human lymphocytes were investigated. The results show that PA in a concentration range from 0.01 to 100 micrograms/ml obviously augmented in vitro IL-2 production, IL-2 receptor expression and responsiveness to IL-2 of human lymphocytes in the presence of PHA, and that these enhancing effects of PA were dose-dependent. The results demonstrated the potentiating effect of PA on cellular immunity and suggested the suitable use of PA in clinical treatment of tumors. The possible application of PA to the treatment of immune disorders involving deficiency of IL-2 production and/or IL-2 responsiveness of lymphocytes is also considered.