• Tuberculosis and Respiratory Diseases
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• 제73권5호
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• pp.288-291
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• 2012

Typhlitis is a necrotizing colitis that usually occurs in neutropenic patients and develops most often in patients with hematologic malignancies such as leukemia and lymphoma. Typhlitis may proceed to bowel perforation, peritonitis and sepsis, which requires immediate treatment. Irinotecan is a semisynthetic analogue of the natural alkaloid camptothecin which prevents DNA from unwinding by inhibition of topoisomerase I. It is mainly used in colon cancer and small cell lung carcinoma (SCLC), of which the most common adverse effects are gastrointestinal toxicities. To the best of our knowledge, no case of typhlitis after chemotherapy with a standard dose of irinotecan in a solid tumor has been reported in the literature. We, herein, report the first case of typhlitis developed after chemotherapy combining irinotecan and cisplatin in a patient with SCLC.

• 생약학회지
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• 제35권2호통권137호
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• pp.110-115
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• 2004

For the evaluation of anti-tumor activity of Korean Oldenlandia Herb (KOH) and Radix (KOR), our experiment was performed with methanol extracts of KOH and KOR. They did not shown any cytotoxicity against HT1080 cell lines. However, they effectively showed anti-metastatic activity through inhibition of the adhesion of HT1080 cells to gelatin, downregulated the expression of MMP2 and uPA and upregulated the expression of TIMP2. They also inhibited tube formation of HUVECs induced by bFGF. However, they did not affect DNA topoisomerase I activity. Simiarly, the T/Cs % in KOH and KOR treated mice were increased 134.9% and 171 %, respectively at 2500 mg/kg. These results suggest that KOH and KOR exert anti-tumor activity via anti-metastatic and anti-angiogenic activities. The further study for isolation of effective compounds and its exact mechanism and comparative study with Chinese Oldenlandia Herba will be required.

• Journal of Genetic Medicine
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• 제1권1호
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• pp.45-50
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• 1997

Neuroblastoma, a pediatric malignant neoplasm of neural crest origin, has a wide range of clinical virulence. The mechanisms contributing to the development of neuroblastomas are largely unclear, but non-random chromosomal changes identified over the past years suggest the involvement of genetic alterations. Amplification of the human N-myc proto-oncogene is frequently seen either in extrachromosomal double minutes or in homogeneously staining regions (HSRs) of aggressively growing neuroblastomas. N-myc maps to chromosome 2 band 24, but HSR have never been observed at this band, suggesting transposition of N-myc during amplification. We have constructed and analyzed the region-specific painting probe for HSR in neuroblastoma IMR-32 to determine the derivative chromosomes. Microdissection was performed on HSR using an inverted microscope with the help of microglass needles and an micromanipulator. We pretreated the microdissected fragments with Topoisomerase I which catalyzes the relaxation of supercolled DNA, and performed two initial rounds of DNA synthesis with T7 DNA polymerase followed by conventional PCR to enable the reliable preparation of Fluorescent in situ hybridization probe from a single microdissected chromosome. With this method, it was possible to construct the region-specific painting probe for HSR. The probe hybridized specifically to the HSRs of IMR-32, and to 2p24, 2p13 of normal chromosome. Our results suggest there was coamplification of N-myc together with DNA of the chromosome 2p24 and 2p13. Moreover, the fluorescent signals for the amplified chromosomal regions in IMR-32 cells were also easily recognized at a Thus this painting probe can be applied to detect the similar amplification of N-myc in neuroblastoma tissue, and the probe pool for HSR may be used to identify the cancer-relevant genes.

• Biomolecules & Therapeutics
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• 제14권2호
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• pp.90-95
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• 2006

CKD-602 exerts its antitumor effect via inhibition of topoisomerase I in cancer cells. Multicellular spheroid (MCS) and Multicellular layers (MCLs) are known as in vitro 3-dimensional models which closely represent tumor conditions in vivo. In order to investigate the potential of CKD-602 against human colorectal tumors, we evaluated the anti-proliferative activity and penetration ability of CKD-602 in MCS and MCL cultures of DLD-l human colorectal cancer cells, respectively. The maximum effects($E_{max}$) induced by CKD-602 were significantly lower in MCS compared to monolayers (48% vs 92%). With prolonged drug exposure, the $IC_{50's}$ of CKD-602 decreased to $23.5{\pm}1.0nM$ in monolayers after 24 h exposure and $42.3{\pm}1.7nM$ in MCS after 6 days, respectively. However, no further increase in effect was observed for exposure time longer than growth doubling time (Td) in both cultures. Activity of CKD-602 was significantly reduced after penetration through MCL and also with cell-free insert membrane. In conclusion, CKD-602 showed significantly decreased anti-proliferative activity in 3D cultures (MCS) of human colorectal cancer cells. Tumor penetration of CKD-602 could not be determined due to loss of activity after penetration through cell free insert membrane, which warrants further evaluation using a modified model.

• 혜화의학회지
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• 제10권2호
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• pp.11-19
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• 2002

To evaluate the antitumor activity and antimetastatic effects of Bruceae FructusCBF), studies were done experimentally. The results were obtained as follows : 1. In cytotoxicity against A549, SK-MEL-2, MCF-7 and XF498 cell concentration inhibiting cell growth up to below 50% of control was recognized at $25{\mu}g/m{\ell}$ of BF. Also BF inhibited cell growth up to below 50% of control against HCT15 cell at $12.5{\mu}g/m{\ell}$, so it showed stronger cytotoxicity against HCT15 cell than another cancer cell. 2. In Inhibitory effect on activity of DNA topoisomerase- I, the $IC_{50}$ was shown $10-50{\mu}g/m{\ell}$ of BF. 3. The T/C% was 143.4 in BF treated group in S-180 bearing ICR mice. 4. The concentration inhibiting adhesion of A549 and SK-OV-3 to complex extracellular matrix up to below 30% of control was recognized at $1{\mu}g/m{\ell}$ of BF. 5. In pumonary colonization assay, a number of colonies in the lungs were decreased significantly in BF treated group as compared with control group. These results suggested that BF extracts might be usefully applied for prevention and treatment of cancer.

• 혜화의학회지
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• 제9권2호
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• pp.97-109
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• 2001

To evaluate the antitumor activity and antimetastatic effects of HDBT, studies were done experimentally. The results were obtained as follows: 1. HDBT extracts didn't show cytotoxicity against BALB/C mouse lung fibroblast cell. 2. In cytotoxicity against A549, SK-OV-3, B16-BL6 and HT1080 concen- tration inhibiting cell growth up to below 30% of control was recognized at $10^{-3}g/ml$ of HDBT. 3. The concentration inhibiting adhesion of A549 and B16-BL6 to complex extracellular matrix up to below 30% of control was recognized at $10^{-3}g/ml$ of HDBT. 4. In Inhibitory effect on activity of DNA topoisomerase I, the $IC_{50}$ was shown $200-300{\mu}g/m{\ell}$ of HDBT. 5. The T/C% was 137.9% in HDBT-treated group in S-180 bearing ICR mice. 6. In CAM assay, HDBT extracts inhibited angiogenesis significantly at $15{\mu}g/egg$ concentration as compared with control. 7. In pumonary colonization assay, a number of colonies in the lungs were decreased but insignificantly in HDBT-treated group as compared with control group. 8. In hematological changes in B16-BL6 injected C57BL/6, numbers of WBC were decreased significantly in HDBT-treated group but numbers PLT were increased insignificantly as compared with control. From above results it was concluded that HDBT could be usefully applied for the prevention and treatment of cancer.

• 혜화의학회지
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• 제8권1호
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• pp.403-424
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• 1999

To evaluate the antitumor activity, antimetastatic and radioprotective effects of Kamisasammaekmundongtang(KSMT), studies were done experimentally. The results were obtained as follows: 1. In cytotoxicity against P388, A549 and B16-F10, KSMT was not showed satisfiable cytotoxicity as compared with control. 2. In Inhibitory effect on activity of DNA topoisomerase I, KSMT has strong inhibitory effect. 3. The inhibitory effect on adhesion of A549 to complex extracellular matrix was significantly increased at 0.5mg/ml, 1mg/ml of KSMT. 4. The T/C% was 122 in KSMT treated group in S-180 bearing ICR mice. 5. In antiangiogenetic effect on CAM assay, inhibitory rate was 33% in KSMT treated group. 6. In pulmonary colonization assay, a number of colonies in the lungs were decreased significantly in KSMT treated group as compared with control group. 7. By FACS analysis of splenic leukocyte after exposure to radiation by linear accelerator, T-helper cell, B cell and macrophage in KSMT treated group were significantly increased while splenocytes were decreased in control group. 8. In histological changes of jejunum of $Bald{\setminus}C$ mice after exposure to radiation by linear accelerator, exclusion and fusion of villi were decreased as compared with control group. But in duodenum and ileum, exclusion and fusion of villi were not decreased as compared with control group. 9. WBC, PLT were increased in KSMT treated group as compared with control group after exposure to radiation by linear accelerator, but the increasing effect was not significant. Above results suggest that KSMT may be useful in prevention of cancer metastasis and protection from damage by radiotherapy. But the further study of KSMT would be demanded.

• 혜화의학회지
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• 제9권1호
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• pp.143-153
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• 2000

To evaluate the antitumor activity and antimetastatic effects of Hongsam -daibotang(HDT-C), studies were done experimentally. The results were obtained as follows: 1. In cytotoxicity against A549, SK-OV-3 and B16-BL6 concentration inhibi ting cell growth up to below 30% of control was recognized at $10^{-3}g/ml$ of HDT-C. 2. The T/C% was 145.4% in HDT-C treated group in S-180 bearing ICR mice. 3. In Inhibitory effect on activity of DNA topoisomerase I, the $IC_{50}$ was shown $100-200{\mu}g/ml$ of HDT-C. 4. The expressing $TNF-{\alpha}$ was increased in HDT-C treated group as compared with control. 5. The expressing MMP-9 was decreased in HDT-C treated group as compared with control. 6. HDT-C extracts exhibited efficient adhesive effect of A549, B16-BL6 cell to complex extracellular matrix. 7. In CAM assays, angiogenesis was significantly inhibited in HDT-C treated group than control group. 8. In pumonary colonization assay, a number of colonies in the lungs were decreased significantly in HDT-C treated group as compared with control group. 9. In hematological changes in B16-BL6 injected C57BL/6, numbers of WBC and were decreased insignificantly and also those of platelet were increased insignificantly in HDT-C treated group as compared with control. 10. In the histological changes of lung in B16-BL6 injected mice, infiltration of cancer cells were inhibited effectively in HDT-C treated groups whereas many cancer cells were infiltrated into erivascular and peribronchiol of control group. These results suggested that HDT-C extracts might be usefully applied for prevention and treatment of cancer.

• Journal of Microbiology and Biotechnology
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• 제33권6호
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• pp.806-822
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• 2023

In the current study we assessed a new crystallized compound, 5-(1-hydroxybutyl)-4-methoxy-3-methyl-2H-pyran-2-one (C-HMMP), from the endophytic fungus Colletotrichum acutatum residing in the medicinal plant Angelica sinensis for its in vitro antimicrobial, antibiofilm, antioxidant, antimalarial, and anti-proliferative properties. The promising compound was identified as C-HMMP through antimicrobial-guided fraction. The structure of C-HMMP was unambiguously confirmed by 2D NMR and HIRS spectroscopic analysis. Antimicrobial property testing of C-HMMP showed it to be effective against a variety of pathogenic bacteria and fungi with MICs ranging from 3.9 to 31.25 ㎍/ml. The compound displayed excellent antibiofilm activity against C. albicans, S. aureus, and K. pneumonia. Furthermore, the antimalarial and radical scavenging activities of C-HMMP were clearly dosedependent, with IC50 values of 0.15 and 131.2 ㎍/ml. The anti-proliferative activity of C-HMMP against the HepG-2, HeLa, and MCF-7 cell lines in vitro was investigated by MTT assay, revealing notable anti-proliferative activity with IC50 values of 114.1, 90, and 133.6 ㎍/ml, respectively. Moreover, CHMMP successfully targets topoisomerase I and demonstrated beneficial anti-mutagenicity in the Ames test against the reactive carcinogenic mutagen, 2-aminofluorene (2-AF). Finally, the compound inhibited the activity of α-glucosidase and α-amylase with IC50 values of 144.7 and 118.6 ㎍/ml, respectively. To the best of our knowledge, the identified compound C-HMMP was obtained for the first time from C. acutatum of A. sinensis, and this study demonstrated that C-HMMP has relevant biological significance and could provide better therapeutic targets against disease.

• Tuberculosis and Respiratory Diseases
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• 제66권2호
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• pp.93-97
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• 2009

연구배경: Belotecan (Camtobell, CKD-602, Chongkundang Pharm., Korea)은 camptothecin의 치환체로 topoisomerase I 효소를 억제하여 항암효과를 나타내는 것으로 알려져 있다. 이에 2차 항암화학요법에 치료제로써 Belotecan 의 효과, 생존율 및 부작용에 대해 연구하였다. 방 법: 이에 소세포폐암에서 etoposide와 platinum을 사용한 1차 항암화학요법에서 실패한 49명의 환자들을 대상으로 2차 항암화학요법에 Belotecan을 투약하였다. 결 과: 전체 반응률은 25%였으며, 11명의 환자에서 partial response를 보였다. 또한 1차 항암화학요법 이후 90일 이내에 재발한 군과 90일 이상 경과한 군간에 유의한 차이는 보이지 않았다. 전체 환자의 중심생존기간은 10.3개월(290일)이었고, 비반응군에서는 186일(95% CI; 67-305)로 반응군의 471일(95% CI; 234-568)에 비해 생존기간의 감소 유의하게 있음을 확인하였다(p=0.07). 결 론: 2차 항암화학요법의 치료제로써 Belotecan의 효능과 부작용에 대해서는 향후 무작위 비교 연구가 필요할 것으로 사료된다.