Silybin is the main active flavanolignan constituent in the extract of Silybam inarianwn. In order to increase its poor oral absorption, 1dB 1016, a complex with phosphatidylcholine, was synthesized (1, 2).The comparative pharmacokinetics of 1dB 1016 and silybin were investigated by measuring free and total plasma silybin levels, as well as total biliary and urinary excretion in rats following oral administration of a single dose (200 mg/kg as silybin). A specific and sensitive HPLC method (detection limit: 5 ng/ml) for the detection of silybin in biological fluids was developed.Peak levels of free and total silybin (mean values respectively 8 and 74 .tg/ml) were obtained 0.5 and 1 h after 1dB 1016 dosing. The respective AUG values (0-24 h) were 9 and 232 h .tg/ml, demonstrating that about 95 % of the plasma silybin is present in a conjugated from.After the administration of silybin, plasma levels were hardly detectable only during the first hour following the administration.Cumulative biliary excretion after 1dB 1016 administration (0-8 h) was 3.73% and urinary excretion (0-72 h) was 3.26% of the administered dose. As the prolonged urinary excretion indicates, the drug is readsorbed from the bile compartment through an enterohepatic recycle. The quantities excreted were respectively more than 2000 and 300 times higher than after administration of silybin alone.Our results indicate that 1dB 1016 is well absorbed in rats, probably due to its remarkable lipophilic character.Artemisia annua L. is used in traditional Chinese medicine and has been investigated as part of the search for novel antimalarial drugs. The major constituent responsible for the antimalarial activity of this plant is the sesquiterpene lactone artemisinin (QHS, qinghaosu) (1) and this constituent has been found to be particularly active against chloroquine-resistant Plasinodiwn falciparum in the treatment of cerebral malaria (2). We have reported that the antimalarial activity of artemisinin is markedly enhanced by the presence of such methoxylated flavones as casticin (3). Further investigation of R' R2 R' R R1 casticin H3c0 H3CO OCH, OH OCH, artemetin H3CO H3CO OCH, OCH3 OCH, ctirysotplenetin H,CO H3cO OCH, OCH3 OH chrysophenol-D H,CO H,cO OCH, OH OH circilineol H,cO H,CO H OCH, OH eupatorin H,CO H,CO OH OH OCH,the flavonoids of this plant yielded seventeen methoxylated flavonoids, three of which were new naturally occurring flavonoids. The major constituents were chrysosplenol-D (0.1% dw), chrysoplenetin (0.035% dw), eupatorin (0.019% dw) and cirsilineol (0.006% dw) with casticin (0.004% dw) as a minor constituent (4).Cell suspension cultures were developed using seed from plants high yielding in artemisinin. Cultures were maintained at 25°C under continuous illumination and sub-cultured every four weeks. Third generation cells were harvested, freeze-dried, and extracted successively with n-hexane, chloroform, and methanol. These extracts were assayed for antimalarial activity using an assay based on the incorporation of E'RJ-hypoxanthine int...

No abstract

Wound healing in diabetic patients is a difficult problem to be solved at present. In addition, patients with diabetes have an increased risk of postoperative wound complications. “She-Xiang-Yu-Hong” (SXYH) ointment is a type of traditional Chinese medicine (TCM) compound used to treat wounds. Over the past few years, SXYH has been applied in the Affiliated Hospital of Chengdu University of TCM (Chengdu, China) for the treatment of diabetic foot infections and bedsores, whereas there has been rare research on the effect of SXYH ointment on wound healing. In this study, SXYH ointment was first applied to streptozotocin (STZ)-triggered diabetic ICR mice (4–6 weeks, 20 ± 2 g) to observe the accelerated wound healing and the shortened wound healing period. As indicated by the histology and biochemistry analyses of skin biopsies, the wounds treated using SXYH ointment showed an increase in the granulation tissue. Moreover, SXYH also modulated the inflammation response by regulating affinity proinflammatory cytokines release (e.g., IL-6 and TNF-α). Furthermore, SXYH ointment obviously improved collagen fiber deposition and tissue on the wound surface. On the whole, this study indicated that SXYH ointment could accelerate wound healing, promote blood vessel formation, and suppress inflammations. Thus, the clinical potential of SXYH ointment was demonstrated in the treatment of diabetes and refractory wounds.