• Journal of Life Science
• /
• 제20권4호
• /
• pp.623-631
• /
• 2010

Hericium erinaceus, an edible and medicinal mushroom belonging to the Basidiomycota family, has been used for curing gastric ulcers and stomach cancers in human beings and is also known to have good inhibitory effects on sarcoma 180 and Ehrlich carcinoma in mice. Neutral saline soluble (0.9% NaCl), hot water soluble and methanol soluble substances (hereinafter referred to as Fr. NaCl, Fr. HW and Fr. MeOH, respectively) were extracted from the fruiting body of the mushroom. In in vitro cytotoxicity tests, crude polysaccharides were not cytotoxic against cell lines such as Sarcoma 180, HepG2, HT-29 and NIH3T3 at concentrations of $10{\sim}2,000\;{\mu}g/ml$. Intraperitoneal injection with crude polysaccharides exhibited a life prolongation effect of 29.1~54.1% in mice previously inoculated with Sarcoma 180. Fr. Na increased the numbers of spleen cells by 2.9 fold at a concentration of $50\;{\mu}g/ml$ compared with the control. Fr. Na improved the immuno-potentiating activity of B lymphocytes by increasing alkaline phosphatase activity by 5.5 fold compared with the control at a concentration of $200\;{\mu}g/ml$. Fr. NaCl increased the numbers of peritoneal exudate cells and circulating leukocytes by 4 and 2.3 folds at a concentration of 50 mg/kg, respectively. Therefore, the crude polysaccharides extracted from the fruiting body of H. erinaceus could improve antitumor activities in mice.

• YAKHAK HOEJI
• /
• 제42권3호
• /
• pp.275-283
• /
• 1998

Aclarubicin(ACL)-entrapped freeze dried liposomes were prepared using Microfludizer to attain a sustained release at targeted organs in a prolonged time so that it can reduce th e side effect and maximize the therapeutic effect. The freeze-dried liposomes were evaluated for pharmacokinetics, antitumor activity against Sarcoma 180, cytotoxicity against L1210 and A549 tumor cells, spleen toxicity and myelosuppressive action. The $AUC_{0{\rightarrow}8hr}$ values were $122{\pm}42,\;382{\pm}140,\;419{\pm}171,\;835{\pm}206\;and\;443{\pm}309{\mu}g{\cdot}min/ml$ for free ACL. ACL-liposome formulation I, II, III and IV, respectively. Cytotoidcity of ACL-entrapped liposomes against L1210 and A549 tumor cells was 2-4 times higher than that of free aclarubicin. ACL-liposome formulation I(PC/CHOL/TA) showed the most potent antitumor activity against Sarcoma 180 in mice. The loss of body weight was much smaller with ACL-entrapped liposomes than free ACL after I.p. injection at a dose of 2 mg/kg/day. Compared to free ACL, ACL-entrapped liposomes expressed a lower and delayed spleen toxicity up to 5th day after I.v. administration. Myelosupperssion seemed to be lower with ACL-entrapped liposome of PC/PC-hydrate/CHOL/TA (formulation III) than free aclarubicin.

• Journal of Mushroom
• /
• 제2권4호
• /
• pp.169-174
• /
• 2004

A hot water extract(HWE-P4) was separated from the fruit bodies of PMO-P4, and its antitumor and immunomodulatory activities against sarcoma-180 in ICR mice were investigated. The internal transcribed spacer(ITS) regions from PMO-P4 were amplified using polymerase chain reaction(PCR) and sequenced. The results revealed that PMO-P4 was belong to the Phellinus baumii. When oral administration at the dose of 160mg/kg/day in the mice until the end of the experiment with 2 week's pre-feeding of the HWE-P4, the survival rate of the mice was 152% for 50days after the inoculation of sarcoma-180 and the suppression rate of the tumor growth was 35.3%(p<0.05) for 28 days after inoculation of sarcoma-180. The HWE-P4 increased 71.4% of the CD4/CD8 ratio and 5-fold of the expression of CD25(IL-2 receptor chain) compared with the control. From these results, the antitumor activity of HWE-P4 is exerted through its immunomodulating activity on the host's immune system.

• YAKHAK HOEJI
• /
• 제42권4호
• /
• pp.345-352
• /
• 1998

Praecoxin A, an ellagitannin, purified from Alnus hirsuta var.microphlla was evaluated on the antitumor activity. Praecoxin A had the significant cytotoxicity to s ix tumor cell lines: human chronic myelogenous leukemia K-562, human promyelocytic leukemia HL-60, mouse leukemia P388, mouse lymphocytic leukemia L-1210, sarcoma-l8O, mouse lymphoma L5178Y except L-1210. And the most sensitive cell line was K-562 ($ED_{50}=2.43{\mu}g/ml$). The $ED_{50} of praecoxin A against HL-60, P388, L-1210, sarcoma7l8O and L5178Y were 6.28, 8.66, 10.00, 7.01, $9.32{\mu}g/ml$, respectively. Praecoxin A showed the increasing effect in life span by 36.8% on the 1st day after treatment of 10mg/kg in mice bearing sarcoma-180 tumor cells (ascitic form) via NCI (National Cancer Institute, U.S.A.) protocol in vivo assay. As a result, praecoxin A is considered to show the antitumor activity.

• Archives of Pharmacal Research
• /
• 제6권2호
• /
• pp.123-131
• /
• 1983

Polysaccharide fractions were prepared from Ginseng root, Mori Radicis Cortex (M. R. C. ), Phellodendri Cortex (Ph. C. ), Sappan Wood (S. W. ) and Tigli Semen (T. S.). Water extract was also prepared from the mixture of ph. C., S. W. and T. S. Ginseng polysaccharide and water extract of the mixture showed marked antitumor activity against sarcoma 180. Ginseng polysaccharide showed a mild increasing effect on the number of circulating leucocytes and a marked increasing effect on the number leucocytes and a marked increasing effect on the number of plaque forming cells (PEC). Polysaccharides from ginsing root, S. W., Ph. C. + T. S. and water extract of the mixture showed dramatic inducing activities of periotoneal exudate cells (PEC), polymorphonuclear leucocytes (PMN) and macrophages. These results suggest the possibility that water extract of the mixture may have the lentinan like effect and ginseng polysaccharide may have stimulating effects on the general immune system.

• Archives of Pharmacal Research
• /
• 제18권6호
• /
• pp.396-401
• /
• 1995

As a part of trials to develop the antitumor agent from tannins isolated from plants, the antitumor activity of peduculagin, an ellagitannin, isolated from Alnus hirsuta var. microphylla was examined in vitro and in vivo. In vitro, the cytotoxicity was determined by 0.4% typanblue dye exclusion method. peduculagin showed the dose-dependent cytotoxicity against human chronic myelogenous leukemia (K-562), human promyelocytic leukemia (HL-60), mouse lymphoid neoplasm (P388), mouse lymphocytic leukemia (L1210) and mouse sarcoma 180(S180) cell lines. $ED_{50}\; values\; (ED_{50})$ of each cell line were 5.30, 0.92, 2.78, 9.35 and $1.38 \mug/ml$ respectively. The most sensitive cell line was HL-60. In vivo, pedunculagin was administered to ICR mouse with the doses of 50 and $100{\;}{\mu}g/ml$intraperitoneally once at 20 days before S180 inoculation. peduculagin showed the antitumor activity and its T/C ratio (%) was 120.82% in the group of both concentrations.

• Archives of Pharmacal Research
• /
• 제23권5호
• /
• pp.482-487
• /
• 2000

The antitumor activity of Bifidobacterium breve K-110, and K-I11, and B. infantis K-525 was investigated. These Bifidobacterial cells and their cell wail preparations (WPG) significantly increased the survival rate of mice who had been intraperitoneally implanted with sarcoma 180 cells. Solid tumor growth was inhibited even when the sarcoma 180 cells were implanted into the groins of the mice. However, the Bifidobacterial cells did not show in vitro cytotoxicity against tumor cell lines. Cell kinetic studies revealed that these WPGs induced neutrophils, which were followed by macrophages, at the site of peritoneal injection. The WPGs directly activated these cells to inhibit the growth of tumor cells in vitro assays. Our results suggest that Bifidobacterial WPGs induce and activate nonspecific phagocytes in situ to reject growing tumor cells in the mouse peritoneal cavity.

• YAKHAK HOEJI
• /
• 제37권1호
• /
• pp.89-94
• /
• 1993

In order to find out a proper connecting bridge between 5-fluorouracil(5-FU) and a macromolecule such as a polypeptide, potentially hydrolytic N$^{1}$-derivartives of 5-FU have been systhesized and evaluated for their biological activity. When tested with in vitro leukemic L$_{1210}$ cells all the obtained derivartives exhibited slightly higher antitumor activity than the parent 5FU. Among them the N$^{1}$ -carbamoyl analogue 2 and N$^{1}$-acetamido analogue 6b showed 50% inhibition of the L$_{1210}$ cell growth at the concentrations of 5.01$\times$10$^{-8}$M and 1.03$\times$10$^{-7}$M, respectively. When tested against sarcoma 180 tumor cells inoculated into mice, the compounds 2 and 6b exhibited, respectively, 62% and 54% inhibition of the solid tumor growth at the 5-time doses of 100 mg/kg/day. Both compounds, N$^{1}$-carbamoyl analogue 2 and N$^{1}$-acetamido analogue 6b, realeased the parent 5-FU when incubated in the L$_{1210}$ cell cultural media for 5 hrs.

• The Korean Journal of Mycology
• /
• 제36권1호
• /
• pp.75-83
• /
• 2008

Lentinus giganteus, one of edible and medicinal mushroom belongs to Pleurotaceae of Agaricales, has been known to contain some inhibitive substances on Sarcoma 180 and curative effect on high blood pressure. Neutral saline soluble (0.9% NaCl), hot water soluble and methanol soluble substances (hereinafter referred to Fr. NaCl, Fr. HW and Fr. MeOH, respectively) were extracted from fruiting body of the mushroom. In vitro cytotoxicity tests, crude polysaccharides were not cytotoxic against cancer cell lines such as Sarcoma 180 and HepG2 at the concentration of $10{\sim}2,000\;{\mu}g/ml$, but crude polysaccharides from Fr. NaCl was toxic to NIH3T3 at the concentration of $10{\sim}2,000\;{\mu}g/ml$. Intraperitoneal injection with crude polysaccharides showed life prolongation effect of $14.3{\sim}67.5%$ in mice previously inoculated with Sarcoma 180, respectively. Fr. NaCl exhibited the immuno-potentiating activity of B lymphocyte by increasing the alkaline phosphatase activity by $1.53{\sim}1.68$ folds compared with control at the concentration of $50{\sim}200\;{\mu}g/ml$, respectively. The numbers of peritoneal exudate cells and circulating leukocytes were increased by 7.7 and 1.6 folds by injecting Fr. NaCl and Fr. MeOH into the mice at the concentration of 50 mg/ml body weight, respectively.

• Journal of Life Science
• /
• 제7권2호
• /
• pp.149-159
• /
• 1997

Chitin, a linked polysaccharide composed of 2-acetamido-2-deoxy-$\beta$-D-glucopytanose residues, is distributed widely in nature. It has been utilized on various application field due to the development of chitin derivatives such as chitosan, partial deacetylated chitin, carboxylmethyl chitin, sulfated chitin, and so on. Chitin and chitosan have been recently interested in antitumor and antimicrobial activities, because of a powerful tumor inhibitory effect against experimental mouse tumors. Especially, the oligosaccharides obtained by partial degradation of them exhibited a remarkable antitumor effect against sarcoma 180, MM 48 and Meth Asolid tumors and antimetastatic effect against Lewis lung carcinoma in mice. This review describes on antitumor effects of chitin, chitosan and their oligosaccharides by their mechanism of action involving enhancement of immunological system.