No related research.
1. Furanosesquiterpenoids of Commiphora myrrha.
An investigation on the gum exudates of Commiphora myrrha has led to the isolation of six sesquiterpenoids. On the basis of spectroscopic data interpretation, they were determined as two new furanosesquiterpenoids, rel-1S,2S-epoxy-4R-furanogermacr-10(15)-en-6-one (1) and rel-2R-methyl-5S-acetoxy-4R-furanogermacr-1(10)Z-en-6-one (2), and four known furanosesquiterpenoids, rel-3R-methoxy-4S-furanogermacra-1E,10(15)-dien-6-one (3), rel-2R-methoxy-4R-furanogermacr-1(10)E-en-6-one (4), furanogermacra-1(10)Z,4Z-dien-6-one, and curzerenone [6,7-dihydro-5beta-isopropenyl-3,6beta-dimethyl-6-vinylbenzofuran-4(5H)-one]. This is the first report of the relative stereochemistry for the known compounds 3 and 4. Compound 1 exhibited weak cytotoxic activity against a MCF-7 breast tumor cell line in a clonogenic assay, while the other five compounds were inactive in this assay.
––Zhu N, Kikuzaki H, Sheng S, Sang S, Rafi MM, Wang M, Nakatani N, DiPaola RS, Rosen RT, Ho CT. J Nat Prod. 2001 Nov;64(11):1460-2.
1. Further study on the effects of motherwort (Leonurus sibiricus L) on preneoplastic and neoplastic mammary gland growth in multiparous GR/A mice.
To evaluate further the chemopreventive role of motherwort (Leonurus sibiricus L; MW) in lesions of the mammary gland and uterus of GR/A mice, the effects on these lesions of the adsorbed (MW1) and unadsorbed (MW2) fractions of MW separated by ion-exchange resins were studied. The incidence of palpable mammary tumours was suppressed and their growth was retarded by both MW1 and MW2, between whose effects no apparent difference was seen. However, neither of them showed effects on pregnancy-dependent mammary tumours (PDMT), mammary hyperplastic alveolar nodules (HAN) or uterine adenomyosis, whereas MW promoted PDMT and inhibited HAN and adenomyosis. All these findings indicate the importance of the synergistic action of several components, specified and unspecified, for the full manifestation of the effects of Chinese medicine.
––Nagasawa H, Inatomi H, Suzuki M, Mori T. Anticancer Res. 1992 Jan-Feb;12(1):141-3.
1. Inhibition of tumor growth by S-3-1, a synthetic intermediate of salvianolic acid A.
Salvianolic acid A (1) is one of the active components from Salvia miltiorrhiza, which was found to suppress the growth of mouse tumors. S-3-1 (a 2-allyl-3,4-dihydroxybenzaldehyde, 2) is a synthetic intermediate of a salvianolic acid A derivative with strong inhibitory effects on the growth of cancer cells in vitro. The inhibitory effects of 2 on tumor growth and its molecular targets were studied. 2 significantly suppressed the growth of mouse Lewis lung carcinoma, S180 sarcoma and H22 hepatic carcinoma in a dose-dependent manner. With a simple scrape-loading dye transfer method, 20 microg/ml of 2 was found to significantly enhance gap junction intercellular communication (GJIC) in human pancreatic adenocarcinoma PaCa Cells, human lung epithelial carcinoma W1-38 cells and human lung adenocarcinoma A549 cells, but 2 had no marked effect on GJIC in human colon cancer CACO2 cells. With Northern blot analysis, 2 was found to inhibit the expression of c-myc gene in A549 cells and have no marked effect on H-ras oncogene expression, and increase the cellular P53 mRNA contents, though it did not affect the expression of RB tumor suppressor gene. 2 also suppressed the P46 (JNK/SAPK) expression in A549 cells. Western blot analysis was applied to visualize the P21ras protein. Results shows that 2 at concentrations ranging from 10 to 20 microg/ml decreases the contents of the membranous P21ras and total P21ras and increases the contents of cytosolic P21ras protein in a time-dependent manner. However, 2 had no significant effects on farnesyl protein transferase activities at the concentrations that could efficiently decrease the membranous P21ras content. This suggested that 2 might suppress tumor growth partly through enhancement of GJIC and reversion of the transformed phenotypes. The other mechanisms may be that 2 can suppress the overexpression of c-myconcogene, inhibit the function of Ras oncoprotein, increase the expression of P53 tumor suppressor gene and interrupt P46-associated mitogen-activated pathway other than farnesylation of Ras protein.
––Li HY, Li Y, Yan CH, Li LN, Chen XG. J Asian Nat Prod Res. 2002 Dec;4(4):271-80.
2. Salvia miltiorrhiza inhibits cell growth and induces apoptosis in human hepatoma HepG(2) cells.
Salvia miltiorrhiza (SM) is a traditional Chinese herbal medicine, commonly used to treat liver diseases in China for centuries. Several earlier studies have indicated that SM exhibits anti-tumor properties, but its mechanism remains to be elucidated. In this study, we evaluated the molecular mechanism of SM in a human hepatoma cell line, HepG(2). Our results show that SM exerted clear cytotoxic effects, and strongly inhibited the proliferation of HepG(2) cells. It was also observed that SM treatment caused apoptotic cell death as evaluated by: (a), morphological changes by using acridine orange/ethidium bromide staining; (b), DNA fragmentation by TdT-mediated dUTP nick end labeling (TUNEL); and (c), sub-G(1) cell analysis. Furthermore, depletion of intracellular glutathione (GSH) and reduction of mitochondrial membrane potential were found to be involved in the initiation of apoptosis by SM.
––Liu J, Shen HM, Ong CN. Cancer Lett. 2000 May 29;153(1-2):85-93.
1. Cytostatic and apoptosis-inducing activity of boswellic acids toward malignant cell lines in vitro.
Boswellic acids from frankincense were indentified as the active compounds which inhibit leukotriene biosynthesis, 5-lipoxygenase and exert antiproliferative activity toward a variety of malignant cells. Because of the relevance for the clinical application, we tested the ethanolic extract of Boswellia serrata gum resin containing a defined amount of boswellic acids for its cytotoxic, cytostatic and apoptotic activity on five leukemia (HL-60, K 562, U937, MOLT-4, THP-1) and two brain tumor (LN-18, LN-229) cell lines by WST-1 assay and flow cytometry. The Boswellia serrata extract induced dose-dependent antiproliferative effects on all human malignant cells tested with GI50 values (extract concentration producing 50% cell growth inhibition) between 57.0 and 124.1 micrograms/ml. In three haematological cell lines (K562, U937, MOLT-4) the effect of total extract expressed in GI50 was 2.8-, 3.3- and 2.3-times more potent (p < 0.05) than pure 3-O-acetyl-11-keto-beta-boswellic acid (AKBA). Morphological changes after 24-27 hours and the detection of apoptotic cells by AnnexinV-binding and/or by the detection of propidium iodide-labelled DNA with flow cytometry, confirmed the apoptotic cell death. The results of this study suggest the effectiveness of Boswellia serrata extract with defined content of boswellic acids.
––Hostanska K, Daum G, Saller R. Anticancer Res. 2002 Sep-Oct;22(5):2853-62.
2. Experimental study on Jurkat cell apoptosis induced by Boswellia carterii Birdw extractive
OBJECTIVE: To study the influence of Boswellia carterii Birdw(BCB) extractive of different concentrations on human Jurkat cell apoptosis at different time points. METHODS: Agarose gel electrophoresis, transmission electron microscope(TEM) and flow cytometry(FCM) were used for observing DNA ladders, morphology of Jurkat cells and cell cycle, respectively. RESULTS: BCB induced apoptosis of Jurkat cells and typical DNA ladders; TEM demonstrated the presence of apoptosis Jurkat cells, condensation of cytoplasm, numerous vaculoes in cytoplasm, compaction of the nuclear chromatin and formation of apoptosis dody. The sub-G1 peak was detected by cell cycle analysis. It revealed that G1 phage cells increased and S phage cells decreased. CONCLUSION: The data indicate that BCB extractive induces time- and concentration-dependent apoptosis in Jurkat cell line.
––Liu X, Qi ZH. Hunan Yi Ke Da Xue Xue Bao. 2000 Jun 28;25(3):241-4.
1. Inhibitory effect of alkane-6,8-diols, the components of safflower, on tumor promotion by 12-O-tetradecanoylphorbol-13-acetate in two-stage carcinogenesis in mouse skin.
Erythro-alkane-6,8-diols were isolated from the flowers of Carthamus tinctorius. 12-0-Tetradecanoylphorbol-13-acetate (TPA, 1 microgram/ear), a tumor-promoting agent, was applied to the ears of mice to induce inflammation. Of 8 alkane-6,8-diols assayed, the C27, C31, C32, C33 and C35 alkane diols inhibited the inflammation. The 50% inhibitory dose of these compounds for TPA-induced inflammation was 0.5-0.7 mg/ear. However, C21, C23 and C25 alkane-6,8-diols were found to have no effect. Furthermore, the mixture of erythro-alkane-6,8-diols from the flowers of C. tinctorius markedly suppressed the promoting effect of TPA on skin tumor formation in mice following initiation with 7,12-dimethylbenz[a]anthracene.
––Yasukawa K, Akihisa T, Kasahara Y, Kaminaga T, Kanno H, Kumaki K, Tamura T, Takido M. Oncology. 1996 Mar-Apr;53(2):133-6.
1. Effects of processing on specific toxicity and pharmacodynamics of radix Kansui, radix Achyranthis bidentatae and semen Armeniacae amarum
The comparative toxicological researches on crude and processed drugs show that the activating action of Radix Kansui, Radix Achyranthis Bidentatae and Semen Armeniacae Amarum on EBV-EA can be decreased by processing. Processing can also decrease stimulating activity on mouse skin, inhibit tumor-promoting activity in two stage skin tumor promoting test and lapactic effect by Radix Kansui. Meanwhile the pharmacological effects of these drugs can be retained or increased by processing.
––Nie S, Li Z, Liang A, Xue B, Li G, Wang X. Zhongguo Zhong Yao Za Zhi. 1996 Mar;21(3):153-6, 190.
No related research.
No related research.
1. Studies on the anticoagulant, antimetastatic and heparin-binding properties of ghilanten-related inhibitors.
The purpose of this study was to investigate the structure-activity relationships of ghilanten, an anticoagulant-antimetastatic protein of the South American leech Haementeria ghilianii. Five sequence-related variants of ghilanten, termed P1-P5, were purified and were shown to potently block the active-site hydrolysis of methoxycarbonyl-D-cyclohexylglycyl-glycyl-arginine-p-nitroanilide acetate by the human blood coagulation enzyme factor Xa; inhibition was rapid and stoichiometric. The amino acid sequence of P5 revealed a consensus sequence for heparin-binding at the carboxy-terminus. A synthetic peptide homologous to this region (93P-N-G-L-K-R-D-K-L-G-C-E-Y-C-E-C-R-P-K-R-K-L-I-P-R-L-S119) bound 125I-labelled heparin maximally at physiological pH and salt concentration. When administered intravenously to mice, the peptide suppressed lung metastases although less potentially than whole ghilanten. These findings suggest that the carboxy-terminal heparin-binding region may play a role in the antimetastatic action of the inhibitor.
––Brankamp RG, Manley GG, Blankenship DT, Bowlin TL, Cardin AD. Blood Coagul Fibrinolysis. 1991 Feb;2(1):161-6.
2. Promotion of lung tumor colonization in mice by the synthetic thrombin inhibitor (no. 805) and its reversal by leech salivary gland extracts.
The role of anticoagulation per se in the reduction of experimental or spontaneous metastasis still remains to be determined, as shown by the conflicting results reported by the literature using different conventional anticoagulants. A new compound has been synthesized (compound no. 805) which prolongs or suppresses coagulation via specific inhibition of thrombin and its possible use in a model of experimental metastasis to clarify the role of anticoagulants in tumor spread was investigated. Contrary to our expectations, this compound increased rather than decreased the number of lung colonies induced by intravenous injections of a variety of murine neoplasias. Studies of the mechanism of this effect indicated that the compound increases retention of tumor cells by the lung without apparent impairment of the natural cell immune system, suggesting that the synthetic thrombin inhibitor may enhance vascular attachment of tumor cells. The promoting effect of compound no. 805 on metastasis was totally reversed by the administration of leech salivary gland extracts, which appear to protect capillaries from damage produced by cyclophosphamide, as revealed by other studies.
––Iwakawa A, Gasic TB, Viner ED, Gasic GJ. Clin Exp Metastasis. 1986 Jul-Sep;4(3):205-20.
3. Anti-tumor effect
Hirudin had inhibitory effect on tumor cells, and had certain inhibitory effect on the growth of mice liver cancer. The high anti-coagulant effect of leech could help anticancer drugs and immune competent cells enter the cancer tissues to kill cancer cells.
1. Antiproliferative activity of Vietnamese medicinal plants.
Methanol, methanol-water (1:1) and water extracts were prepared from seventy-seven Vietnamese medicinal plants and tested for their antiproliferative activities against human HT-1080 fibrosarcoma cells. Among them, fifteen extracts including seven methanol extracts of Caesalpinia sappan, Catharanthus roseus, Coscinium fenestratum, Eurycoma longifolia, Hydnophytum formicarum and Streptocaulon juventas (collected at two areas), six methanol-water (1:1) extracts of Cae. sappan, Cat. roseus, Co. fenestratum, H. formicarum and S. juventas (at two areas), and two water extracts of Cae. sappan and S. juventas exhibited antiproliferative activities in a concentration-dependent manner. Their antiproliferative activities against human cervix HeLa adenocarcinoma, human lung A549 adenocarcinoma, murine colon 26-L5 carcinoma, murine Lewis lung carcinoma (LLC) and murine B16-BL6 melanoma cells were then examined. Co. fenestratum showed selective activity against lung carcinoma and/or lung metastatic cell lines, A549, LLC and B16-BL6, while H. formicarum and S. juventas showed selective activity against human tumor cell lines, HeLa and A549. Characteristic morphological change and DNA fragmentation indicated the antiproliferative activity to be due to the induction of apoptosis.
––Ueda JY, Tezuka Y, Banskota AH, Le Tran Q, Tran QK, Harimaya Y, Saiki I, Kadota S. Biol Pharm Bull. 2002 Jun;25(6):753-60.
2. 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.
3. Anticancer effect
Water extract (1g/ml) 2.5μl had obvious killing effect on HL-60, K562, L929 and Yacl in vitro, and this effect was believed to be dose-dependent.
No related research.