zi cao decoction, shilonin and b,b-dimethylacryloylshikonin, etc. had inhibitory effect on staphylococcus aureus, bacillus coli and bacillus subilis, etc.. Shilonin had significant inhibitory effect on bacillus coli, typhoid bacillus, shigella dysenteriae, bacillus pyocyaneus and staphylococcus aureus. 10% physiological saline infusion of zi cao had inhibitory effect on microsporum lanosum, etc.. At the concentration of 0.5mg~10mg/ml, zi cao had inhibitory effect on amoeba. Its water decoction had certain therapeutic effect on TB in mice.

Aether, water and ethanol extract of zi cao had certain anti-inflammatory effect.

Shikonin which is extracted from Arnebia euchroma at the dosage of 5~10g could completely inhibit the growth of sarcoma180, at the dosage of 10mg/kg, it could prolong the survival time of tumor bearing mice at the rate of 92.5%. zi cao had anticancer effect. It had certain inhibitory effect on the multiplication cycle of Hela cells.

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.

zi cao gen ecoction had obvious excitatory effect on isolated or in vivo heart of rabbits and toads. zi cao decoction could significantly lower the blood pressure of nearly half aminals under general anesthesia state.

Oral administration of 50% zi cao syrup to mice could significantly inhibit the estrus cycle which could restore 2 months after suspension of the drug, it could also inhibit the fertility rate and obviously reduce the weight of the ovaries.

zi cao ye extract could lower the blood sugar of rabbits.

Zi Cao Injection, 2ml for intramusclar injection, 1~2 times daily. 13 cases of infectious hepatitis with jaundice were all cured, among 157 cases of acute infectious hepatitis without jaundice, 139 were cured, 6 markedly effective, 12 improved and 13 ineffective.

zi cao extract was made into tablets, 2 tablets, tid. 25 cases of phlebitis were treated, and the effective rate was 100%.

Dried zi cao was decocted with 8000g sesame oil and removed the dregs. The oil could be used to treat burn. Among 1153 cases of burn, all were cured after 10~42 days' treatment except one death.

0.1% Zi Cao Injection, 2ml, once daily, no other drugs were applied except anti-histamine. 50 cases were of psoriasis were treated, 13 cured, 8 basically cured, 18 markedly effective, 9 improved and 2 ineffective.

zi cao was made into tablets, 0.2g each tablet. Take the drug after menstrual period, 9 tablets, tid for 9 days. 102 cases were effective, and the effective rate of contraception was 82.4%.

Except those noted, all references come from Weng Weiliang, et al., Clinical Chinese materia medica, Henan Science & Technology Press, 1998