1. Treatment of intestinal metaplasia and atypical hyperplasia of gastric mucosa with xiao wei yan powder
138 cases of intestinal metaplasia (IM) and 104 cases of atypical hyperplasia (AH) of the gastric mucosa of chronic gastritis treated with Xiao Wei Yan Powder (XWYP) were reported. The diagnoses were based on the pathological examination of gastric antrum biopsy specimens. The cases were randomly divided into treated group and control group. The XWYP contained Smilax glabrae, Hedyotis diffusae, Taraxacum mongolicum, Caesalpinia sappan, Paeonia alba, Cyperus rotundus, Bletilla striata, Glycyrrhiza uralensis etc., and was prepared in powder form, taken orally 5-7g tid. After 2-4 months of administration, gastroscopic and pathological examinations were repeated. Results: In treated group, the total effective rate of IM was 91.3% and that of the AH was 92.16%, while in control group, they were 21.3% and 14.46% respectively (P < 0.01). It denoated that XWYP had marked therapeutic effects for IM and AH. The animal experiments revealed no toxic effect, so safety guarantee was provided for its clinical application.
Liu XR, Han WQ, Sun DR. Zhongguo Zhong Xi Yi Jie He Za Zhi. 1992 Oct;12(10):602-3, 580.
2. Anti-carcinogenic activity of Taraxacum plant. II.
Eleven triterpenoids (1-11) from the roots of Taraxacum japonicum (Compositae) were examined for their inhibitory effects on Epstein-Barr virus early antigen (EBV-EA) induced by the tumor promoter, 12-O-tetrade-canoylphorbol-13-acetate (TPA), in Raji cells as a primary screening test for anti-tumor-promoters (cancer chemopreventive agents). Of these triterpenoids, taraxasterol (1) and taraxerol (7) exhibited significant inhibitory effects on EBV-EA induction, but the inhibitory effects of their acetates 2 and 8 were weaker than those of 1 and 7. Furthermore, 1 and 7 exhibited potent anti-tumor-promoting activity in the two-stage carcinogenesis tests of mouse skin using 7,12-dimethylbenz[a]anthracene (DMBA) as an initiator and TPA as a promoter, and 1 showed a remarkable inhibitory effect on mouse spontaneous mammary tumors using C3H/OuJ mouse. These results strongly suggested that taraxasterol (1) could be a valuable chemopreventive agent.
––Takasaki M, Konoshima T, Tokuda H, Masuda K, Arai Y, Shiojima K, Ageta H. Biol Pharm Bull. 1999 Jun;22(6):606-10.
3. Studies on immunopotentiating activities of antitumor polysaccharide from aerial parts of Taraxacum platycarpum.
The polysaccharide fraction from Taraxii Herba showed potent immunopotentiating activities with antitumor activities. The fraction having small amount of protein inhibited the growth of solid tumor and increased peritoneal exudate cells and immunoorgan weights in normal mice, and also increased hypersensitivities in tumor bearing mice.
––Jeong JY, Chung YB, Lee CC, Park SW, Lee CK. Arch Pharm Res. 1991 Mar;14(1):68-72.
1. Protease inhibitors and carcinoma of the esophagus.
Squamous cell carcinoma of the esophagus is endemic in parts of South Africa. Previous case-control studies have shown many associations but no clear etiologic pathway has been established. A case-control study of dietary and social factors was performed for 130 patient/control pairs matched for age, gender, and educational level. Staple diet, consumption of wild vegetables, use of tobacco, and traditional beer consumption were compared between the two groups. The results showed that new significant associations were found with the consumption of beans (P = 0.016) and consumption of the full traditional diet of maize, pumpkin, and beans (P = 0.027). Known associations with the consumption of Solanum nigrum (P = 0.018) and with smoking (P = 0.002) were confirmed by multiple regression analysis. It’s concluded that Solanum nigrum, beans, and pumpkin all contain protease inhibitors. Suppression of protease inhibitors can lead to overexpression of growth factors in the esophagus, resulting in a proliferative and oncogenic drive.
––Sammon AM. Cancer 1998 Aug 1;83(3):405-8
2. Sultana S, Perwaiz S, Iqbal M, Athar M. Crude extracts of hepatoprotective plants, Solanum nigrum and Cichorium intybus inhibit free radical-mediated DNA damage. J Ethnopharmacol 1995 Mar;45(3):189-92.
The presence of plant extracts of Solanum nigrum and Cichorium intybus in the reaction mixture containing calf thymus DNA and free radical generating system protect DNA against oxidative damage to its deoxyribose sugar moiety. The effect was dependent on the concentration of plant extracts. However, the effect of Cichorium intybus was much pronounced as compared to the effect of Solanum nigrum. These studies suggest that the observed hepatoprotective effect of these
crude plant extracts may be due to their ability to suppress the oxidative degradation of DNA in the tissue debris.
1. Antimicrobial activities of naphthazarins from Arnebia euchroma.
Bioassay-directed fractionation of extract of Arnebia euchroma led to the isolation of alkannin (1), shikonin (2), and their derivatives (3-8) as the active principles against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE). The stereochemistry of alpha-methylbutyryl alkannin (8) is revealed for the first time, and the antimicrobial activity of 8 was compared with its corresponding diastereomer (9). The derivatives 3-9 showed stronger anti-MRSA activity [minimum inhibitory concentrations (MICs) ranged from 1.56 to 3.13 microg/mL] than alkannin or shikonin (MIC = 6.25 microg/mL). Anti-MRSA activity of derivatives was bactericidal with minimum bactericidal concentration (MBC)/MIC < or = 2. In a time-kill assay, the bactericidal activity against MRSA was achieved as rapidly as 2 h. The derivatives 3-9 were also active against vancomycin-resistant Enterococcus faecium (F935) and vancomycin-resistant Enterococcus faecalis (CKU-17) with MICs similar to those with MRSA. Aromatic ester derivatives were also synthesized for antimicrobial activity comparison. None of these compounds were active against Gram-negative bacteria tested. Their cytotoxicity was also evaluated on selected cancer cell lines, and they expressed their activity in the range 0.6-5.4 microg/mL (CD(50)). Our results indicate that the ester derivatives of alkannin are potential candidates of anti-MRSA and anti-VRE agents with antitumor activity.
––Shen CC, Syu WJ, Li SY, Lin CH, Lee GH, Sun CM. J Nat Prod. 2002 Dec;65(12):1857-62.
2. Beta-hydroxyisovalerylshikonin induces apoptosis in human leukemia cells by inhibiting the activity of a polo-like kinase 1 (PLK1).
beta-Hydroxyisovalerylshikonin (beta-HIVS), which was isolated from the plant, Lithospermum radix, induces apoptosis in various lines of human tumor cells. To identify genes involved in beta-HIVS-induced apoptotic process, we performed cDNA array analysis and found that beta-HIVS suppresses the expression of the gene for a polo-like kinase 1 (PLK1) that is involved in control of the cell cycle. When U937 and HL60 cells were treated with 10(-6) M beta-HIVS for 0.5 h, both the amount of PLK1 itself and the kinase activity of this enzyme were decreased. By contrast, Bcr-Abl-positive K562 cells were resistant to the induction of apoptosis by beta-HIVS and this compound did not suppress the kinase activity of PLK1 in these cells. However, simultaneous treatment of K562 cells with both beta-HIVS and STI571, which selectively inhibits the protein tyrosine kinase (PTK) activity of Bcr-Abl, strongly induced apoptosis. Moreover, beta-HIVS increased the inhibitory effect of STI571 on PTK activity. Treatment of K562 cells with antisense oligodeoxynucleotides (ODNs) specific for PLK1 sensitized these cells to the beta-HIVS-induced fragmentation of DNA. These results suggest that suppression of the activity of PLK1 via inhibition of tyrosine kinase activity by beta-HIVS might play a critical role in the induction of apoptosis.
––Masuda Y, Nishida A, Hori K, Hirabayashi T, Kajimoto S, Nakajo S, Kondo T, Asaka M, Nakaya K. Oncogene. 2003 Feb 20;22(7):1012-23.
1. Clinical study
xia ku cao was used as the main herb, and combined with yin chen, bai hua she she cao, hai zao, kun bu, lou lu. The formula was used to treat primary liver cancer and had certain therapeutic effect.
1. Cucurbitacins from Trichosanthes kirilowii as the inhibitory components on tyrosinase activity and melanin synthesis of B16/F10 melanoma cells.
Cucurbitacins 1 and 2 were isolated from the root of Trichosanthes kirilowii by tyrosinase inhibitory activity-guided fractionation. Spectroscopic analysis revealed that compounds 1 and 2 were cucurbitacin D and 23,24-dihydro-cucurbitacin D, respectively. Compounds 1 and 2 effectively inhibited the activity of tyrosinase (IC(50) = 0.18 microM and 6.7 microM, respectively), and the synthesis of melanin (IC(50) = 0.16 microM and 7.5 microM, respectively) in B16/F10 melanoma cells.
––Oh H, Mun YJ, Im SJ, Lee SY, Song HJ, Lee HS, Woo WH. Planta Med. 2002 Sep;68(9):832-3.
2. Effect of trichosanthin an anti-leukemia protein on normal mouse spleen cells.
Trichosanthin, from Trichosanthes kirilowii is a member of the Cucurbitaceae family. It has been reported to have anti-cancer activity. The effects of Trichosanthin peptides (15 amino acids in length) on ConA stimulated incorporation of 3[H] thymidine into cultured, primary mouse spleen cells and L1210 cells were determined. Both spleen cells and L1210 cells were plated at 7.5 x 10(5) cells/ml in a microtiter plate. Different concentrations of the peptide (0.5, 5, 25, and 50 micrograms/ml) and ConA (1 microgram/ml) were added with serum free media, and half of the samples were labeled with 1 microCi/well of 3[H] thymidine. The additional half of the cell samples were used to determine cell number and % viability. After 24 hours incubation, the N-terminal peptides (amino acid residues #1-15 and 16-30) caused increases in ConA stimulated incorporation of 3[H] thymidine into normal spleen cells at low concentrations of the peptides (5 micrograms/ml). The viability of spleen cells and L1210 cells were not affected by these peptides at 5 micrograms/ml. These N-terminal peptides (#1-15 and 16-30) were tested for in vivo anti-tumor activity. There was a delay of tumor formation in the treated vs control group. The results suggest that N-terminal sequences of trichosanthin have anti-tumor activity.
––Takemoto DJ. Anticancer Res. 1998 Jan-Feb;18(1A):357-61.
3. Cytotoxic activity of bryonolic acid isolated from transformed hairy roots of Trichosanthes kirilowii var. japonica.
Bryonolic acid was isolated in high yield from transformed hairy root cultures of Trichosanthes kirilowii var. Japonica. Bryonolic acid exhibited cytotoxic activity to various tumor cells in vitro, independent of cell type. Normal cells such as rat hepatocytes are less sensitive to bryonolic acid. The appearance of a DNA ladder was detected in the bryonolic acid-treated HL-60RG cells, indicating that cell death triggered by bryonolic acid is due to apoptosis.
––Kondo T, Inoue M, Mizukami H, Ogihara Y. Biol Pharm Bull. 1995 May;18(5):726-9.
1. Anti-tumor effect
Water extract and aether extract had same anti-tumor activity when given through intraperitoneal injection.
No related research.
No related research.
1. Cytokine production by human lymphocytes stimulated by a herbal compound containing Bupleurum (KY88 LIVER LIVO).
AIM: Compounds containing Bupleurum possess immunomodulating effects. KY88 LIVER LIVO (KY88) is a blend of such compound. The aim of this study is to investigate the effects of KY88 on the production of cytokines by lymphocytes in vitro. METHODS: Seventy Sprague Dawley rats were used of which 40 were orally fed with 4 mg purified KY88 for 35 d. Normal human lymphocytes were isolated and cultured in standard conditions. The culture medium was collected at zero and 72 h after the KY88 treatment. The cytokines, including interleukin-1beta (IL-1beta), IL-2, IL-4, IL-6, tumor necrosis factor-alpha (TNF-alpha), and interferon-gamma, were measured by ELISA kits. RESULTS: TNF-alpha levels in the supernatant of cultured human lymphocytes significantly increased after the treatment of PHA and KY88. The mean levels were (855+/-251), (399+/-145), and (176+/-49) ng/L after the treatment with KY88 at the concentrations of 10, 1 and 0.1 g/mL respectively. However, the level in the control group without specific treatment was only (68+/-4) ng/L. The difference between KY88 10 g/mL and control groups was significant (P<0.05). KY88 may regulate the immune function through the induction of TNF-alpha expression.
––Chow WC, Loo TY, Sham ST. Acta Pharmacol Sin. 2003 Feb;24(2):140-4.
2. Inhibitory effect of bupleuri radix saponins on adhesion of some solid tumor cells and relation to hemolytic action: screening of 232 herbal drugs for anti-cell adhesion.
Among 232 herbal drugs tested, six showed a remarkable anti-cell adhesive activity, and the extract from the roots of Bupleurum falcatum (Umbelliferae), the semen of Psorala corylifolia (Leguminosae), and the semen of Areca catechu (Palmae) showed an anti-cell adhesive action at non-cytotoxic concentrations. Saikosaponins-a, d and e, isolated from the roots of Bupleurum falcatum, exhibited a potent anti-cell adhesive activity and a strong hemolytic action. In a structure-activity relationship for both activities, it seems that a sugar moiety and an ether linkage between C-13 and C-28 are required for good bioactivities. In addition, saikosaponin d with a beta-hydroxy group at C-16 was more potent than saikosaponin a possessing an alpha-hydroxy group. Taken together, it is suggested that the mechanism for anti-cell adhesive activity of saikosaponin may resemble that for their hemolytic action.
––Ahn BZ, Yoon YD, Lee YH, Kim BH, Sok DE. Planta Med. 1998 Apr;64(3):220-4.
3. Induction of differentiation in rat C6 glioma cells with Saikosaponins.
The effects of saikosaponins (a, b(1), b(2), c, d), isolated from Bupleurum Radix, on the induction of differentiation in rat C6 glioma cells were studied. Saikosaponins a and d were shown to inhibit cell proliferation and alter cell morphology. In addition to cytostasis, the enzymatic activities of glutamine synthetase (GS) and 2',3'-cyclic nucleotide 3'-phosphohydrolase (CNP) were also noticeably increased after treatment with saikosaponin a. Nevertheless, saikosaponin d only showed an increase of GS activity, no significant changes in CNP activity were found. These results suggest that saikosaponin a can induce the differentiation of C6 glioma cells into astrocytes and/or oligodendrocytes, but saikosaponin d can only induce the differentiation of C6 glioma cells into astrocytes.
––Tsai YJ, Chen IL, Horng LY, Wu RT. Phytother Res. 2002 Mar;16(2):117-21.
1. Biological activities of crude plant extracts from Vitex trifolia L. (Verbenaceae).
Biological assays of Vitex trifolia L. organic extracts have shown relevant activities. Hexanic and dichloromethanic (DCM) extracts, when prepared from stems and foliage, have proved to be very toxic against several cancer cell lines in culture (SQC-1 UISO, OVCAR-5, HCT-15 COLADCAR, and KB). Also, an important antifeeding activity against the insect pest Spodoptera frugiperda (Lepidoptera: Noctuidae) was recorded. The hexanic extract from leaves completely inhibited the growth of the fungal plant pathogen Fusarium sp. within the first 2 days of the experiment, but dropped significantly at day 6 (15% inhibition). The potential of V. trifolia for several uses is discussed.
––Hernandez MM, Heraso C, Villarreal ML, Vargas-Arispuro I, Aranda E. J Ethnopharmacol. 1999 Oct;67(1):37-44.