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ABSTRACT: ETHNOPHARMACOLOGICAL RELEVANCE: AjugadecumbensThunb is a medicinal plant native to China popularly used to treat chronic pelvic inflammation and hysteromyoma. Its main bioactive components are iridoid glycosides, such as 8-O-acetylharpagide and harpagide that had presented antibacterial, anti-inflammatory, and antiviral activities. AIM OF THE STUDY: To establish a sensitive LC-MS/MS method and compare the pharmacokinetics of 8-O-acetylharpagide and harpagide in rats after oral administration of their pure forms and from compounds obtained from A. decumbens extract. MATERIALS AND METHODS: Rats received orally 15mg/kg(equivalent of 6mg/kg 8-O-acetylharpagide and 1.5mg/kg harpagide), 30mg/kg and 60mg/kg of Ajugadecumbens Thunb extract and were compared to animals that received 12mg/kg of 8-O-acetylharpagide or 3mg/kg of harpagidep.o. Concentrations of 8-O-acetylharpagide and harpagide in plasma were determined by LC-MS/MS method at different time points and all pharmacokinetic parameters were estimated by non-compartmental analysis. RESULTS: Results showed that the iridoid glycosides were quickly absorbed by oral route and showed a dose-dependence profile. Pharmacokinetic parameters of both glycosides were essentially the same except Tmax when dosed as the extract or pure forms. CONCLUSION: 8-O-acetylharpagide was metabolized to harpagide, which affected the pharmacokinetic profiles of harpagide when dosed as the extract. This pharmacokinetic study seems to be useful for a further clinical study of AjugadecumbensThunb extract.
Journal of ethnopharmacology 03/2013; · 2.32 Impact Factor
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ABSTRACT: To study the effect of Badu Shengji San (BDSJS) and its decomposed recipes on morphological changes of injured skin in rats.
SD rats with injured skin were treated with BDSJS and its different decomposed recipes for consecutively 14 days. Morphological changes in the injured skin were observed by H&E staining.
Mercury and lead-containing ingredients significantly decreased epidermal thickness and caused vascular hemorrhage, hyperemia and inflammatory cell infiltration in reticular layer of dermis. The compatible herbs alleviated epidermal thickness and reduced dermal lesions.
BDSJS' mercury and lead-containing ingredients can accelerate the healing of skin wound and its compatible herbs can relieve the dermis injury induced by mercury and lead.
Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica 03/2012; 37(6):715-8.
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ABSTRACT: To study the mercury accumulation in injured skin rats induced by Badu Shengji San (BDSJS), a traditional Chinese medicine preparation for external use.
Injured skin rats were treated with BDSJS for consecutively 4 weeks. During the 4 weeks and the following 4 weeks after the drug withdrawal, samples were collected for determining mercury contents in blood, urine and kidney, with urinary N-acetyl-beta-D-glucosaminidase(NAG) and beta2-microglobulin (beta2-MG) as indicators of renal toxicity and serum biochemical indicators of hepatic and renal functions. Additionally, activated partial thromboplastin time (APTT), prothrombin time (PT) and kidney and renal pathological changes were also observed.
Compared to injured skin rats, mercury contents of blood, urine and kidney were increased significantly in low, middle and high-dose BDSJS groups administered for consecutive 4 weeks. The levels of mercury showed decreases in urine (89%, 78%, 93%) and kidney (55%, 51%, 57%), and blood mercury concentration recovered to the normal range in low, middle and high-dose BDSJS groups after the drug withdrawal for 4 weeks. Kidney coefficient and beta2-MG were remarkably increased and renal tubular epithelial cell swelling could be found in the high-dose group, and kidney coefficient, beta2-MG and renal morphology basically recovered to the normal levels after the drug withdrawal for 4 weeks.
The administration of BDSJS for consecutively 4 weeks can cause mercury accumulation in blood and mainly in kidney. Once the accumulated mercury concentration of kidney reaches a certain level, renal tubular epithelial cells would be injured. 1.1 mg x cm(-2) of BDSJS is proved to be safe and 2.2 mg x cm(-2) can cause mild but reversible injury in the function of kidney which can be recovered after drug withdrawal for 4 weeks.
Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica 03/2012; 37(6):700-5.
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ABSTRACT: To compare the sensitivity of early renal injury induced by mercury-containing medicine in rats, including urinary N-acetyl-beta-D-glucosdminidase (NAG), beta2-microglobulin (beta2-MG), retinol binding protein (RBP) and clusterin (CLU).
Badu Shengji San(BDSJS), a mercury-containing preparation of traditional Chinese medicine, was adopted as the mercury contact drug. The lowest effective toxic dose was used to observe its effect on serum creatinine (SCr), blood urea nitrogen (BUN), and such early renal injury indicators as NAG, RBP, beta2-MG and CLU and compare the sensitivity of tested indicators.
Compared to the broken skin group, groups with administration of 60 and 120 mg x kg(-1) doses of BDSJS showed no obvious difference in SCr and BUN when kidney indicators is remarkably increased and obvious pathological changes were found in kidney tubules but with significant increase in the urinary level of CLU and the levels of NAG and RBP. H&E staining of renal tubule showed that exposure of 30 mg x kg(-1) BDSJS had no significant morphological changes, but at the same concentrations, the level of RBP was markedly increased. Urinary beta2-MG levels were markedly decreased in BDSJS 30, 60 mg x kg(-1) group rats, whereas 120 mg x kg(-1) dose group showed no obvious change in urinary beta2-MG levels.
Urinary RBP, NAG and CLU were more sensitive than SCr and BUN as indicators for early renal injury in the order of RBP > NAG > CLU, and urinary RBP, NAG would increase earlier than beta2-MG.
Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica 03/2012; 37(6):706-10.
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ABSTRACT: To compare the effects of Badu Shengji San (BDSJS) on rats with different injured skins.
The injured and ulcerous skin rat model was established to observe the renal injury induced by BDSJS, a mercury-containing external preparation of Chinese medicine, with urinary N-acetyl-beta-D-glucosaminidase (NAG) and retinol binding protein (RBP) as indicators of renal toxicity.
Compared to injured skin rats with the same dose, both of high and low-dose ulcerous skin groups showed obvious increase in urinary RBP and kidney coefficients, significant pathomorphological changes in renal tubules and notable epithelial cytopathic effects. In terms of NAG, the high-dose ulcerous skin group saw no significant increase, but the low-dose group recorded sharp rise.
The renal toxicity induced by BDSJS in ulcerous skin rats was more toxic than that in injured skin ones.
Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica 03/2012; 37(6):711-4.
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ABSTRACT: To study the effect of repeated administration of Zhuhong ointment on renal antioxidant capability of ulcerous skin in rats, in order to further discuss the mechanism of mercury contained in Zhuhong ointment on the antioxidant capability of kidney in skin ulcer rats.
Eighty SD rats were randomly divided into eight groups: Zhuhong ointment A, B, C, D, E (1.219, 0.609, 0.305, 0.152, 0.76 g x kg(-1)) groups, the vaseline group, the ulcer model group and the impairment control group. The levels of NAG and RBP of toxicity for early kidney tubular injury and T-AOC, SOD, GSH-PX and GSH in kidney were determined after consecutive administration for 14 days.
Compared with ulcer model group, the levels of RBP in groups A, B, C and D increased, while the levels of NAG increased only in the group A. The level of T-AOC increased in groups A, B and C. The level of T-SOD increased in the group E, while it dropped down greatly in the group A. The level of GSH-PX increased in groups A, B and C. The content of GSH increased in every dose groups.
Antioxidant capacity in rats can be increased in a reasonable dose of Zhuhong ointment, but some antioxidant activity can be notably inhibited by with the increase of dose.
Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica 03/2012; 37(6):735-8.
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ABSTRACT: To study the effects of Zhuhong ointment on accumulation in the body of mercury and the pathological morphology changes of kidney, via the measurement of related indicators of the skin-impaired model rat.
Eighty-eight SD rats were randomly divided into the impairment control group, and high-, middle-, low-dose Zhuhong ointment groups. Each group was treated by corresponding methods for 4 weeks, and recovering for 4 weeks. Urinary potein (PRO), pH, Beta N-acetyl aminoglycosidase enzymes (NAG) and beta2-microglobulin (beta2-MG) contents in urine were taken as monitoring indexes, blood urea nitrogen (BUN) and serum creatinine (SCr) in blood and the levels of mercury in urine, blood and kidney were tested, and the pathological morphology changes of kidney were observed.
After treatment for 4 weeks, compared with impairment control group, the levels of mercury in urine, blood and kidney in every dose group increased significantly (P < 0.01). And the relation exists between toxicity and dose on Zhuhong ointment. After recovery for 4 weeks, the levels of mercury in urine and blood in every dose group restore normal, while the level of mercury in kidney in high- dose group still increased (P < 0.01). The level of NAG increased only in high-dose group. There was no significant difference in NAG contents between Zhuhong ointment groups and the impairment control group (P < 0.05).
Excess using Zhuhong ointment repeatedly may lead to accumulation of mercury and pathological morphology changes of kidney. So the levels of mercury in the body and related indicators of renal functions should be tested in clinical when long-term using Zhuhong ointment.
Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica 03/2012; 37(6):739-43.
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ABSTRACT: To investigate the anticancer and anti-metastatic effect of Ajuga decumbens extraction (HBG) on breast cancer and to clarify the effect of HBG on MMPs and TIMPs.
The antitumor and antimetastic effect of HBG was determined using orthotopic 4T1 breast cancer mouse model. Western blot analysis was employed to detect the expression of associated proteins in breast cancer metastasis.
Administration with 50-200 mg x kg(-1) doses of HBG significantly reduced the tumor weight, tumor volume and numbers of lung tumor nodules in a dose-dependent manner. Tumor metastasis correlated proteins were altered following HBG treatment, MMP-2 and MMP-9 were down-regulated while TIMP-1 and TIMP-2 were up-regulated.
HBG showed anticancer and antimetastatic effect towards breast cancer through regulating the expression of MMPs and TIMPs. These data sustain our contention that HBG might be used as a potential therapeutic agent.
Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica 12/2011; 36(24):3511-4.
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ABSTRACT: Badu Shengji San(BDSJS) is a traditional Chinese medicine (TCM) used for drawing out toxin, eliminating suppuration and promoting granulation. Toxic minerals such as arsenic and lead are the two most important components of BDSJS. Previous hypothesis indicated that according to the compatibility theory of TCM, the toxicity of the entire BDSJS was weaker than that of arsenic and lead, respectively. In the present study, SD rats with injured skin were treated with distilled water and different composition of BDSJS (complete formulations, compatible herbs, mineral medicine containing arsenic and lead, mineral medicine containing arsenic and mineral medicine containing lead) once a day for consecutive 2 weeks. Kidney coefficient and urinary beta-N-acetyl glucosidase (NAG) were used as the indicators of renal toxicity and the content of malondiadehyde (MDA), superoxide dismutase (SOD), glutathione peroxidase (GSH-PX), glutathione (GSH) and metallothionein (MT) in the renal tissue were measured. Our data showed that kidney coefficient, the severity of renal pathological lesion and MT level in the kidney of the entire BDSJS group decreased significantly compared with arsenic and lead group. Additionally, the NAG content of the entire BDSJS group had the decreased trend. The kidney CuZn-SOD level of the entire BDSJS group had the increased trend, but the MDA, GSH-PX, GSH level had no obvious difference. Our results suggested that compatible herbs in BDSJS relieved renal injury induced by arsenic and lead, and the attenuation mechanism may be related to MT and CuZn-SOD, but not to MDA, GSH-PX and GSH directly.
Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica 08/2011; 36(15):2118-23.
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ABSTRACT: To provide evidences for evaluating the role of chlorogenic acid (CA) on the adverse reaction of traditional Chinese medicine injection and promoting clinical rational usage of CA, the effect of CA and chlorogenic acid-HSA(CA-HSA) on the degranulation in mast cell RBL-2H3 were compared and the allergenic effect and its mechanism were investigated.
The unsensitized and sensitized RBL-2H3 cells were used. The releasing rate of histamine and beta-hexosaminidase was detected by colormetric assays. The degranulating rate was detected by neutral red staining and Annexin V positive cell rate was detected by flow cytometry.
CA and CA-HSA could not induce degranulation in unsensitized RBL-2H3 cells. CA and CA-HSA could significantly increase the release of histamine and beta-hexosaminidase, degranulating rate and Annexin V positive cell rate.
CA has strong allergenicity after combination with serum proteins. As an active ingredient of Shuanghuanglian injection, CA is a kind of possible allergen which caused hypersensitivity reactions induced by Shuanghuanglian injection.
Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica 04/2011; 36(7):912-7.
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ABSTRACT: To compare the effect of Magnolia officinalis and M. officinalis var. biloba on gastrointestinal motility dysfunction.
The gastrointestinal motility dysfunction induced by atropine and L-Arg were used in this study. The effect of M. officinalis on the gastrointestinal function was evaluated by propulsive motility of the total gastrointestinal tract test by recording the time of excreting carbo medicinalis, the gastric residualrate, the intestinal propulsion rate, the serum levels of D-xylose, motilin (MTL) and gastrin (GAS). ED50 were calculated with Bliss's method.
M. officinalis and M. officinalis var. biloba improved the gastrointestinal motility, decreased the gastric residual rate, enhanced the intestinal propulsion rate and increased serum levels of D-xylose, motilin (MTL) and gastrin(GAS). The ED50 value of M. officinalis var. biloba was much higher than that of M. officinalis.
The effect of improving gastrointestinal motility of M. officinalis was proved to be superior to that of M. officinalis var. biloba.
Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica 10/2010; 35(19):2624-7.
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ABSTRACT: To compare the acute toxicity and the pharmacological effect of Huoxiang Zhengqi microemulsion and Huoxiang Zhengqi tincture.
The acute toxicities of Huoxiang Zhengqi microemulsion and Huoxiang Zhengqi tincture were observed by the test of maximum dose in mice and the antidiarrheal effects of them were evaluated by ED50 values of the diarrhea index, the serum levels of gastrin and motilin in the mice diarrhea model induced by senna.
The acute toxicity of Huoxiang Zhengqi tincture was much higher than that of Huoxiang Zhengqi microemulsion and the ED50 values of the two formulations were similar.
The microemulsion of Huoxiang Zhengqi prescription was much safer than that of tincture, but the antidiarrheal effects of them in diarrhea model induced by senna were similar.
Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica 08/2010; 35(15):2004-7.
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ABSTRACT: Platycodon grandiflorum (Jacq.) A. DC., a Chinese food and medicine, has been used as expectorant traditionally. The present study aimed to investigate the effect of Platycodon grandiflorum extract (PGE) on SKOV3 ovarian cancer cells. 3-(4,5- dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromide (MTT) assay was used to monitor cell numbers, Annexin-V/propidium iodide (PI) staining, RT-PCR and Western blot were used to examine cell apoptosis, caspases activation. Bcl-2 and Bax expressions and mitochondrial cytochrome c release. Our result showed that PGE-induced apoptosis was associated with activation of caspase-3, -8 and -9, down-regulation of Bcl-2, up-regulation of Bax and release of mitochondrial cytochrome c to cytosol. The data indicate that PGE may have anti-tumor effect mainly via caspase-3 and caspase-9 dependent apoptotic pathway.
The American Journal of Chinese Medicine 01/2010; 38(2):373-86. · 1.98 Impact Factor
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ABSTRACT: Kai Xin San (KXS), a traditional Chinese herbal medicine, has been used clinically for the treatment of depressive disorders and cognitive impairment for centuries. However, the effects of KXS on cognitive dysfunction induced by depression have not been evaluated scientifically. The present study aimed to explore the antidepressant-like and nootropic effects of an aqueous extract of KXS (at doses of 0.3, 0.9, and 2.7 g/kg/day) using chronic mild stress (CMS) as a model of depression. Depressive symptoms were analyzed using the sucrose-preference and novelty-induced inhibition of feeding tests. Cognitive function was evaluated using a two-way active avoidance task. Serum corticosterone and adrenocorticotropic hormone (ACTH) levels, acetylcholinesterase (AChE) protein expression in the hippocampus, and monoamine neurotransmitter concentrations in the prefrontal cortex and hippocampus were also determined to elucidate the neurochemical mechanisms. Experimental results showed that KXS aqueous extract significantly ameliorated the CMS-induced depressive symptoms, including the reduced preference index and prolonged latency to novelty-suppressed feeding. Simultaneously, KXS significantly reversed the CMS-induced decrease in the numbers of active avoidance and active movement distances and increase in the numbers of the passive avoidance and passive movement distances, thereby producing nootropic effects in the two-way active avoidance test. KXS also inhibited the increased AChE expression in the hippocampus, up-regulated the decreased monoamine neurotransmitter concentrations of both brain areas and reduced the elevated ACTH concentrations in the serum induced by CMS. Taken together, these results indicate that KXS exerts its antidepressant-like and nootropic effects in the CMS model by modulating the HPA axis, monoamine neurotransmitter and cholinergic systems.
Experimental Biology and Medicine 06/2009; 234(7):785-93. · 2.64 Impact Factor
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ABSTRACT: Duchesnea indica (Andr.) Focke has been commonly used to treat cancer in Asian countries for centuries, and recently has been shown to possess anticancer properties in vitro and in vivo. But the underlying mechanism of the anticancer action is unclear, especially in in vivo studies. In this study, we investigated the anticancer effect and associated mechanisms of Duchesnea phenolic fraction (DPF) on cervical cancer in vitro and in vivo. Our results showed that DPF significantly inhibited cervical cancer cell proliferation in dose- and time-dependent manners. DPF induced apoptosis as determined by AO/EB staining, DNA fragmentation and flow cytometry. Some apoptosis correlated proteins were altered following DPF treatment. Bax was up-regulated while Bcl-2 was down-regulated, and the expression ratio of Bax/Bcl-2 was increased. These resulted in the translocation of Bax to mitochondria, the release of cytochrome c from the mitochondria to the cytosol and caspase-3 activation. Concurrently, DPF provoked S phase arrest along with significant down-regulation of S phase-associated proteins, such as cyclin A, cyclin E, cyclin D1 and cdk2. Transplanted U14 cervical cancer mouse model was used to evaluate the antitumor effect of DPF in vivo. Compared with control, DPF treatment markedly prolonged survival of tumor-bearing mice and dose-dependently reduced the tumor weight. DPF could induce apoptosis in tumor tissues as evidenced by increased TUNEL-positive cells, activation of caspase-3, up-regulation of Bax and down-regulation of Bcl-2. In addition, DPF significantly decreased the expression of cell proliferation markers PCNA and ki67 in tumors. All together, these data sustain our contention that DPF has anticancer properties and merits further investigation as a potential therapeutic agent.
Experimental Biology and Medicine 01/2009; 234(1):74-83. · 2.64 Impact Factor
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ABSTRACT: Duchesnea indica (Andr.) Focke has been commonly used to treat cancer in Asian countries of centuries, and more recently, has been shown to possess anticancer properties in vivo and in vitro. However, little is known about the underlying mechanism of its anticancer action. In the present study, we investigated the effect of Duchesnea phenolic fraction (DPF) on SKOV-3 ovarian cancer cells to provide insights into the mechanisms of growth suppression involved in DPF-mediated apoptosis and cell cycle arrest.
Cytotoxic activity of DPF on SKOV-3 cells was determined using MTT assay, apoptosis (AO/EB staining, DNA fragmentation, FACS), caspase-3 activation and cell cycle analysis studies. The role of the molecules in apoptosis and cell cycle regulation was analyzed by Western blot and RT-PCR.
DPF significantly inhibited SKOV-3 cell proliferation in a dose-dependent manner and markedly induced apoptosis evidenced by characteristic apoptotic morphological changes, nuclear DNA fragmentation and sub-G1 peak. DPF suppressed Bcl-2 levels, enhanced Bax levels and Bax/Bcl-2 ratio, and simultaneously translocated Bax to mitochondria followed by mitochondrial release of cytochrome c into the cytosol and activation of effector caspase-3. Furthermore, DPF provoked S phase arrest in SKOV-3 cells with down-regulation of cyclin A, E, D1 and CDK2.
DPF exhibits cytotoxicity towards human ovarian cancer SKOV-3 cells through induction of apoptosis via mitochondrial pathway and arresting cell cycle progression in S phase. All together, these data sustain our contention that DPF has anticancer properties and merits further investigation as a potential therapeutic agent.
Gynecologic Oncology 02/2008; 108(1):173-81. · 3.89 Impact Factor
