Chemical constituents of Lonicera japonica roots and anti-inflammatory activity / 中草药

Objective: To research the chemical composition from the roots of Lonicera japonica and their anti-inflammatory activities. Methods: The compounds were isolated and purified by chromatography on silica gel column, Sephadex LH-20 column, preparative thin-layer, and semi-preparative HPLC, etc. Their structures were identified on the basis of spectroscopic data, and parts of the isolated compounds were tested for their anti-inflammatory activities against zebrafish. Results: Fourteen compounds were isolated and elucidated as 3,13-dihydroxystemodan-2-one (1), chrysophanol (2), palmarumycin CP2 (3), β-sitosterol (4), stigmasterol (5), stigmast-4,6,8(14), 22-tetraen-3-one (6), erythrinassinate D (7), lanosterin (8), 3-O-acetyloleanolic acid (9), protocatechuin aldehyde (10), daucosterol (11), (E)-3-(3,4-dihydroxybenzylidene)-5-(3,4-dihydroxyphenyl)-2(3H)-furanone (12), lomacarinoside B (13), and (2E,6S)-8-(α-L-arabinopyranosyl-(1″→6')-β-D-glucopyranosyloxy)-2,6-dimethyloct-2-eno-1,2″-lactone (14). Conclusion: Compound 1 is a new compound, and compounds 2, 3, 6, 7-9, and 13 are isolated from L. japonica for the first time. Compounds 9 and 10 show the significant anti-inflammatory activities at 100 μg/mL.

Effects of BCG or CP-2 on the DNA Synthesis in the Epithelial Cells of the Mouse Appendix / 대한해부학회지

This experiment was performed to evaluate the morphological responses of the appendicular mucosa of the mouse, inoculated with Ehrlich carcinoma cells in the inguinal area, following administration of BCG or CP-2 (Coptis chinensis-Croton tiglium extracts). Healthy adult ICR mice weighing 25 gm each were divided into normal and experimental groups (experimental control, BCG or CP-2 treated group). Each experimental group mouse was inoculated with 1 x 10(7) Ehrlich carcinoma cells subcutaneously in the inguinal area. From the next day after inoculations, 0.2 mL of saline, BCG (0.5 mL/25 g B.W.: 0.03 x 10(8) ~ 0.32 x 10(8) CFU) or CP-2 (30 mg/kg) were injected subcutaneously to the animals every other day, respectively. The day following the 7 th injection of BCG or CP-2, each mouse was injected with a single dose of 0.7 microCi/gm of methyl-3H-thymidine (25 Ci/mmol, Amersham Lab., England) through tail vein. Seventy minutes after the tritiated thymidine injection, animals were sacrificed. The number of the labeled epithelial cells of the appendicular mucosae were observed and evaluated. On histological studies of the experimental control, BCG or CP-2 treated mice, general morphologies of the appendicular mucosae were similar. On autoradiographic study, number of the labeled cells of normal control, experimental control, BCG treated or CP-2 treated groups were 362.2+/-56.12, 350.7+/-42.65, 265.8+/-27.08 and 241.3+/-53.29, respectively. Above results show that BCG and CP-2 suppress the DNA synthetic activity of the epithelial cells of the appendix, but did not show any remarkable morphological alterations on the mucosae. These results suggest that BCG and CP-2 are ones of effective anticancer drugs for the cytostatic therapy.

Effects of Adriamycin or CP-2 to the Rectal Mucosae of Mouse Implanted with Ehrlich Carcinoma Cells: An Autoradiographic Study / 대한해부학회지

This experiment was performed to evaluate the morphological responses of the rectal intestinal glands of the mouse, inoculated with Ehrlich carcinoma cells, following administration of adriamycin or composition of the extracts of the Croton tiglium and Coptis chinensis rhizome (CP-2, Institute of Experimental Tumor Research, Seoul, Korea). Healthy adult ICR mice weighing 25 gm each were divided into normal and experimental groups (tumor control group, adriamycin treated group, and CP-2 treated group). In the experimental groups, each mouse was inoculated with 1 x 10(7) Ehrlich carcinoma cells subcutaneously in the inguinal area. From next day, 0.2 mL of saline, adriamycin (2 mg/kg) or CP-2 (30 mg/kg) were injected subcutaneously to the animals every other day, respectively. The day following the 7th injection of anticancer drugs, each mouse was injected with a single dose of 0.7 microCi/gm of methyl- 3H-thymidine through tail vein. Seventy minutes after the thymidine injection, animals were sacrificed. and rectal tissues were collected and fixed in 10% neutral formalin. Deparaffinized sections were coated with autoradiographic emulsion EM-1 (Amersham Lab., England) in the dark room and dried. The number of the labeled epithelial cells of the rectal crypts (mean number of labeled epithelial cells per 3.5 mm length of mucosa) were observed and calculated. On histological study, in the rectum of adriamycin treated groups, length of the intestinal crypts is shorter than those of the normal control ones. Disrupted intestinal crypts and epithelial cells were observed. But in the CP-2 treated group, morphological changes of the rectum were not observed. On autoradiographic study, number of the labeled cells of normal control, rumor control, adriamycin-treated, CP-2-treated groups were 263.1 (+/-38.65), 395.7 (+/-52.52), 73.3 (+/-22.54), 96.3 (+/-28.36), respectively. In the adriamycin and CP-2 treated groups., poorly-labeled cells containing only a few silver grains of 3H-thymidine were observed more frequently than in those of the normal and tumor control groups. But in the tumor control group, number of the heavy labeled cells were observed more frequently than in those of the normal control group. From the above results, adriamycin and CP-2 may suppress the DNA synthesis of the cells of the rectal crypts. But CP-2 does not result any histological defect on the rectal mucosa. These results suggest that CP-2 is expected as one of most effective anticancer drugs.

Effects of Antitumor Agents on the Duodenum of Mouse Implanted with Ehrlich Carcinoma Cells: An Autoradiographic Study / 대한해부학회지

This experiment was performed to evaluate the morphological responses of the intestinal gland of the mouse duodenum inoculated with Ehrlich carcinoma cells, following administration of 5-fluorouracil, mitomycin C or CP -2. Healthy adult ICR mice weighing 25 gm each were divided into normal and experimental groups. In the experimental groups, each mouse was inoculated with 1 x10(7) Ehrlich carcinoma cells subcutaneously in the inguinal area. From the next day of inoculation, 0.2 mL of saline (experimental control group), 5-fluorouracil (30 mg/kg), mitomycin C (400 microgram/ kg) or CP -2 (30 mg/kg) were injected subcutaneously to the animals every other day, respectively. The day following the 7th injection of anticancer drugs, each mouse was injected with a single dose of 0.7 microCi/g of methyl -(3)H-thymidine (25 Ci/mmol) through tail vein. Seventy minutes after the thymidine injection, animals were sacrificed. The number of the labeled epithelial cells of the duodenal crypts (mean number of labeled epithelial cells per 3.5 mm length of mucosa) were observed and calculated. On histological study, in the duodenum of mitomycin C treated groups, narrowed intestinal gland, a number of the nectotic epithelial nuclei and loosely arranged lamina propria were observed. However, in the CP-2 treated group, morphological changes of the duodenum were not observed. On autoradiographic study, number of the labeled cells of normal control, experimental control, CP-2 treated, 5-fluorouracil treated and mitomycin C treated groups were 625.5 +/-58.85, 691.3 +/-82.32, 428.3 +/-83.16, 527.5 +/-79.84 and 297.33 +/-45.72, respectively. In the CP-2 and mitomycin C treated group, poorly-labeled cells containing only a few silver grains of (3)H-thymidine were observed more frequently than in those of the normal control group. From the above results, CP-2 and mitomycin C are more suppressed the DNA synthesis of the cells of the duodenal crypts as compare with 5-fluorouracil. But CP-2 does not result any histological defect on the duodenal mucosa. These results suggest that CP-2 is expected as one of most effective anticancer drugs.

Effects of Adriamycin or CP -2 on the Spleen of Mouse Implanted with Ehrlich Carcinoma Cells: An Autoradiographic Study / 체질인류학회지

In this experiment, side effects of two anticancer drugs (adriamycin and CP -2) on the structure of spleen were histologically studied. Each of ICR mice was inoculated with 1 x10 7 Ehrlich carcinoma cells subcutaneously in the inguinal area. From next day, 0.2 ml of saline solution, adriamycin (2 mg/kg) or CP -2 (30 mg/kg) were injected subcutaneously every other day. The day following the 7th injection of adriamycin or CP -2, each mouse was injected with a single dose of 0.7 micro Ci/gm of methyl -3 H -thymidine (25 Ci/mmol, Amersham Lab., England) through tail vein. Seventy minutes after the thymidine injection, animals were sacrificed, and splenic tissues were collected and fixed in 10% neutral formalin. Deparaffinized sections were coated with autoradiographic emulsion EM -1 (Amersham Lab., England) in the dark room and dried, and were kept in a light -tight box. The sections were exposured for 5 weeks in the dark room, and were developed in D -19 developer. The number of the labeled cells in the areas of the white pulp, the red pulp and the marginal zone (mean number of labeled cells per 0.21 mm 2 ) were observed and calculated. In the spleen of adriamycin treated group, vacuoles containing pyknotic nuclei were observed frequently. Whereas in the CP -2 treated group, morphological changes of the spleen were not observed. The number of the labeled cells of normal control, experimental control, CP -2 treated and adriamycin treated groups were 240.3 +/-53.28, 252.3+/- 58.24, 216.7 +/-55.17 and 45.4 +/-15.46, respectively, and most of the labeled cells were located near the marginal zone of the spleen. In the adriamycin treated group, labeled cells containing a few silver grains of 3 H -thymidine were observed more frequently than in those of the normal and experimental control groups. From the above results, adriamycin and CP -2 may suppress the DNA synthesis of the splenic tissues. Especially, CP -2 does not results any histological defect on the splenic tissues. These result suggest that CP -2 is expected as one of effective anticancer drugs.