Inhibition of tumor growth by S-3-1, a synthetic intermediate of salvianolic acid A

Hong Yan Li, Yan Li, Chunhong Yan, Lian Niang Li, Xiao Guang Chen

Research output: Contribution to journalArticle

22 Citations (Scopus)

Abstract

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 μg/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 μg/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-myc oncogene, 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.

Original languageEnglish (US)
Pages (from-to)271-280
Number of pages10
JournalJournal of Asian Natural Products Research
Volume4
Issue number4
DOIs
StatePublished - Dec 1 2002
Externally publishedYes

Fingerprint

Tumors
Gap Junctions
Growth
myc Genes
Genes
Neoplasms
Tumor Suppressor Genes
Communication
Salvia miltiorrhiza
Prenylation
Lewis Lung Carcinoma
Carcinoma
ras Proteins
Proteins
ras Genes
Oncogene Proteins
Transferases
Mitogens
Sarcoma
Northern Blotting

Keywords

  • Inhibition
  • Oncogene
  • P21 protein
  • Salvianolic acid intermediate
  • Tumor growth

ASJC Scopus subject areas

  • Analytical Chemistry
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Complementary and alternative medicine
  • Organic Chemistry

Cite this

Inhibition of tumor growth by S-3-1, a synthetic intermediate of salvianolic acid A. / Li, Hong Yan; Li, Yan; Yan, Chunhong; Li, Lian Niang; Chen, Xiao Guang.

In: Journal of Asian Natural Products Research, Vol. 4, No. 4, 01.12.2002, p. 271-280.

Research output: Contribution to journalArticle

Li, Hong Yan ; Li, Yan ; Yan, Chunhong ; Li, Lian Niang ; Chen, Xiao Guang. / Inhibition of tumor growth by S-3-1, a synthetic intermediate of salvianolic acid A. In: Journal of Asian Natural Products Research. 2002 ; Vol. 4, No. 4. pp. 271-280.
@article{b1acf5f008ef44a885d9782148f2dca1,
title = "Inhibition of tumor growth by S-3-1, a synthetic intermediate of salvianolic acid A",
abstract = "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 μg/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 μg/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-myc oncogene, 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.",
keywords = "Inhibition, Oncogene, P21 protein, Salvianolic acid intermediate, Tumor growth",
author = "Li, {Hong Yan} and Yan Li and Chunhong Yan and Li, {Lian Niang} and Chen, {Xiao Guang}",
year = "2002",
month = "12",
day = "1",
doi = "10.1080/1028602021000049069",
language = "English (US)",
volume = "4",
pages = "271--280",
journal = "Journal of Asian Natural Products Research",
issn = "1028-6020",
publisher = "Taylor and Francis Ltd.",
number = "4",

}

TY - JOUR

T1 - Inhibition of tumor growth by S-3-1, a synthetic intermediate of salvianolic acid A

AU - Li, Hong Yan

AU - Li, Yan

AU - Yan, Chunhong

AU - Li, Lian Niang

AU - Chen, Xiao Guang

PY - 2002/12/1

Y1 - 2002/12/1

N2 - 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 μg/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 μg/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-myc oncogene, 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.

AB - 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 μg/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 μg/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-myc oncogene, 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.

KW - Inhibition

KW - Oncogene

KW - P21 protein

KW - Salvianolic acid intermediate

KW - Tumor growth

UR - http://www.scopus.com/inward/record.url?scp=0036888755&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0036888755&partnerID=8YFLogxK

U2 - 10.1080/1028602021000049069

DO - 10.1080/1028602021000049069

M3 - Article

VL - 4

SP - 271

EP - 280

JO - Journal of Asian Natural Products Research

JF - Journal of Asian Natural Products Research

SN - 1028-6020

IS - 4

ER -