Shuangdan Mingmu Capsule for Diabetic Retinopathy: A Systematic Review and Meta-Analysis of Randomized Controlled Trials.

Objective: To systematically evaluate the efficacy and safety of the Shuangdan Mingmu capsule in the treatment of diabetic retinopathy (DR). Methods: Common Chinese and English databases, including PubMed, Medline, Embase, VIP, Wanfang, and the Chinese National Knowledge Infrastructure (CNKI), were searched from their inception to May 31, 2022. According to the Cochrane Handbook, two reviewers independently evaluated and collected data on the included studies. Meta-analysis was performed by RevMan software 5.4. Results: Seven trials with a total of 835 patients were included. The clinical effectiveness rate was defined as the primary outcome, and the TCM symptom score, Chinese-Version Low Vision Quality of Life Questionnaire (CLVQOL) scores, macular thickness, hemorrhagic spot area, vascular endothelial growth factor levels, platelet-derived growth factor levels, and the incidence of adverse effects were the secondary outcome. The results of the meta-analysis showed that, compared with conventional medical treatment alone, the Shuangdan Mingmu capsule combined with conventional treatment could significantly improve the clinical effectiveness rate of treating DR (OR = 4.07, 95% CI (2.10, 7.89), p < 0.0001), and reduce the incidence of adverse reactions in DR patients (OR = 0.47, 95% CI (0.26, 0.86), p=0.01). In addition, other results showed that TCM symptom score(OR = -3.47, 95% CI (-3.84, -3.10), p < 0.00001); CLVQOL scores (OR = 23.93, 95% CI (21.37, 26.49), p < 0.00001); macular thickness (OR = -47.34, 95% CI (-50.67, 44.00), p < 0.00001); hemorrhagic spot area (OR = -0.91, 95% CI (-1.01, -0.81), p < 0.00001); vascular endothelial growth factor levels (OR = -45.76, 95% CI (-49.74, 41.79), p < 0.00001); platelet-derived growth factor levels (OR = -1.73, 95% CI (-2.15, -1.31), p < 0.00001). Conclusion: Compared with conventional treatment alone, the Shuangdan Mingmu capsule combined with conventional treatment is more effective and safer in the treatment of diabetic retinopathy. However, due to the limitations of the included studies, more high-quality studies are still needed to further assess the efficacy and safety of the Shuangdan Mingmu capsule in the treatment of diabetic retinopathy.

Research Progress of Chinese Herbal Medicine Intervention in Renal Interstitial Fibrosis.

Chronic kidney diseases usually cause renal interstitial fibrosis, the prevention, delay, and treatment of which is a global research hotspot. However, no definite treatment options are available in modern medicine. Chinese herbal medicine has a long history, rich varieties, and accurate treatment effects. Hitherto, many Chinese herbal medicine studies have emerged to improve renal interstitial fibrosis. This paper reviews the mechanisms of renal interstitial fibrosis and recent studies on the disease intervention with Chinese herbal medicine through literature search, intend to reveal the importance of Chinese herbal medicine in renal interstitial fibrosis. The results show that Chinese herbal medicine can improve renal interstitial fibrosis, and the effects of Chinese herbal medicine on specific pathological mechanisms underlying renal interstitial fibrosis have been explored. Additionally, the limitations and advantages of Chinese herbal medicine in the treatment of renal interstitial fibrosis, possible research directions, and new targets of Chinese herbal medicine are discussed to provide a basis for studies of renal interstitial fibrosis.

A systematic review and meta-analysis of integrated traditional Chinese medicine and Western medicine in treating glomerulosclerosis.

BACKGROUND: The combination of Traditional Chinese medicine and Western medicine (TCM+WM) has been widely used in the treatment of glomerulosclerosis, but the results are still controversial. This study will assess the clinical efficacy of TCM+WM for glomerulosclerosis and provide evidence-based medical data via meta-analysis. METHOD: The MEDLINE, EMBASE, PubMed, Cochrane Central Registry of Controlled Trials, and multiple Chinese databases (Wan Fang, CNKI, and VIP) were searched for randomized controlled trials (RCT) that compared the effects of WM and TCM+WM. Review Manager 5.3 software was used for the meta-analysis of selected studies, and appropriate tests were performed to determine the quality, heterogeneity and sensitivity of these studies. RESULTS: Sixteen RCTs met the inclusion criteria and were selected for the analysis. Compared with the placebo or WM-treated glomerulosclerosis patients, TCM+WM intervention significantly improved renal function indices including 24-hour urine protein quantity (24 h U-Pro), serum creatinine (Scr), blood urea nitrogen (BUN), creatinine clearance (Ccr). In addition, the serum albumin (ALB), triglyceride (TG), and cholesterol (CHOL) levels were also significantly improved (P < .05) in patients receiving the combination therapy. Finally, the combination of TCM+WM reduced the indices of glomerulosclerosis more effectively compared with WM alone. CONCLUSION: The combination of TCM+WM can significantly improve the renal function and prognosis of patients with glomerulosclerosis.

Aidi injection, a traditional Chinese biomedical preparation for gynecologic tumors: a systematic review and PRISMA-compliant meta-analysis.

Aidi injection (ADI), a traditional Chinese biomedical preparation, is a promising adjuvant therapy for gynecologic tumors (GTs), including cervical cancer (CC), endometrial cancer (EC), and ovarian cancer (OC). Although studies have reported positively on ADI therapy, its exact effects and safety in GT patients remain controversial. Therefore, a wide-ranging systematic search of electronic databases was performed for this meta-analysis. Data from 38 trials including 3309 GT patients were analyzed. The results indicated that the combination of conventional treatment and ADI markedly improved the patients' overall response rate (P<0.00001), disease control rate (P<0.00001), and quality of life (P<0.05) compared with conventional treatment alone. Furthermore, patient immunity was enhanced with combined treatment, as indicated by significantly increased percentages of CD3+ (P=0.005) and CD4+ (P<0.00001) and increased CD4+/CD8+ ratio (P=0.001). Most of the adverse events caused by radiochemotherapy such as gastrointestinal issues, leukopenia, thrombocytopenia, and hepatotoxicity, (P<0.05 for all) were significantly alleviated when ADI was used in the GT patients. However, other adverse events such as nephrotoxicity, diarrhea, alopecia, and neurotoxicity did not significantly differ between the two groups. Overall, these results suggest that the combination of conventional and ADI treatment is more effective than conventional treatment alone.

Exploration of the Two-Way Adjustment Mechanism of Rhei Radix et Rhizoma for Cardiovascular Diseases.

AIM AND OBJECTIVE: Myocardial infarction, cerebral infarction, and other diseases caused by vascular obstruction have always jeopardized human life and health. Several reports indicate that Rhei Radix et Rhizoma has a good clinical effect in the prevention and treatment of cardiovascular diseases. Owing to the complexity of herbal medicine, the pharmacodynamic mechanism of Rhei Radix et Rhizoma is still unclear. The objectives of this study were to explore the two-way adjustment mechanism of Rhei Radix et Rhizoma and provide a new solution for the prevention and treatment of cardiovascular disease. MATERIALS AND METHODS: This study used data mining, reverse pharmacophore matching, network construction, GO and KEGG Analysis, and molecular docking to investigate the two-way adjustment mechanism of Rhei Radix et Rhizoma. The methods used were based on systems pharmacology and big data analysis technology. RESULTS: The results suggest that Rhei Radix et Rhizoma uses a two-way adjustment of activating blood circulation, as well as blood coagulation in the prevention and treatment of cardiovascular diseases. The components involved in activating blood circulation are mainly anthraquinone components. The corresponding targets are NOS2, NOS3, CALM1, and the corresponding pathways are calcium signaling pathway, VEGF signaling pathway, platelet activation, and the PI3K-Akt signaling pathway. For blood coagulation, the components are mainly tannin components; the corresponding targets are F2, F10, ELANE, and the corresponding pathways are the neuroactive ligand-receptor interaction, complement and coagulation cascades. CONCLUSION: This study indicated that Rhei Radix et Rhizoma exerts the two-way adjustment of activating blood circulation and blood coagulation in the prevention and treatment of cardiovascular diseases. It can make up for the side effects of the existing blood circulation drugs for cardiovascular disease, only activating blood circulation, and the uncontrollable large-area bleeding due to the long-term use of the drugs. This study provides a material basis for the development of new blood-activating drugs based on natural medicine.

Virtual Screening of the Multi-pathway and Multi-gene Regulatory Molecular Mechanism of Dachengqi Decoction in the Treatment of Stroke Based on Network Pharmacology.

BACKGROUND: Stroke is ranked second among diseases that cause mortality worldwide. Owing to its complicated pathogenesis, no satisfactory treatment strategies for stroke are available. Dachengqi decoction (DCQD), a traditional Chinese herbal medicine, has been widely used in China for a long time, as it has a good effect on stroke. However, the molecular mechanism underlying this effect of DCQD is unclear. OBJECTIVE: In the present study, we aimed to reveal and explore the multi-pathway and multi-gene regulatory molecular mechanism of Dachengqi decoction in the treatment of stroke. METHODS: In this study, a network pharmacology method, in combination with oral bioavailability prediction and drug-likeness evaluation, was employed to predict the active ingredients of DCQD. The target genes of the active components and the traced pathways related to these target genes were predicted. Gene Ontology (GO) enrichment and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway analyses were performed using clusterProfiler software package on the R platform and ClueGo+CluePedia plug-ins. Finally, the key DCQD targets were verified using the Gene Expression Omnibus (GEO) dataset. RESULTS AND DISCUSSION: According to the ADME model, 52 active components were screened from 296 active components of DCQD. After prediction and screening, 215 stroke-related targets were obtained and analyzed via GO and KEGG analyses. GO analysis showed that DCQD targets were mainly involved in the regulation of oxidative stress, lipid metabolism, inflammation, and other biological processes. KEGG pathway analysis further revealed pathways involved in stroke, such as arachidonic acid metabolic, HIF-1 signaling pathway, estrogen signaling pathway, MAPK signaling pathway, PI3K-Akt signaling pathway, platelet activation pathway, VEGF signaling pathway, and cAMP signaling pathway. Network analysis revealed that DCQD might be involved in the regulation of lipid metabolism, blood pressure, inflammation, angiogenesis, neuroprotection, platelet aggregation, apoptosis, and oxidation in stroke treatment. GEO dataset analysis showed that DCQD's therapeutic effects might be exerted via the bidirectional regulation principle. CONCLUSION: Based on the methods of network pharmacology and GEO analysis, it was found that, during stroke treatment, DCQD regulates and controls multiple genes and multiple pathways in a synergistic manner, providing a new strategy for stroke treatment.

Identification of higenamine as a novel α1 -adrenergic receptor antagonist.

The α1 -adrenoceptor (α1 -AR) antagonists are potential candidates for the treatment of blood pressure. Higenamine (HG) is a novel α1 -AR antagonist. In this study, we investigated the effects of HG in HEK293A cells transfected with α1A -, α1B -, and α1D -AR in vitro, rat mesenteric artery ex vivo, Wistar-Kyoto rats and spontaneously hypertensive rats in vivo. The radioligand binding assay showed that HG competitively inhibited the binding of [3 H]-prazosin to α1 -AR in a concentration-dependent manner. The affinities (pKi) of HG for the cloned α1A -, α1B -, and α1D -AR were 6.57, 6.48, and 6.35, respectively, indicating that HG displayed no selectivity for the three α1 -AR subtypes. In in vitro studies, HG was able to blunt inositol monophosphate production. It also displayed an inhibitory effect on the influx and entry of calcium ions and phosphorylation of extracellular signal-regulated kinase 1 and 2 induced by phenylephrine (PE). In ex vivo studies, PE caused a dose-dependent inotropic response curve, and the pA2 value for HG was 6.86 ± 0.29. In addition, the in vivo results showed that HG could decrease the blood pressure in normotension, spontaneous hypertension, and PE-induced hypertension models. These results indicate that HG can directly bind to α1 -AR and it appears to be a novel antagonist for α1 -AR, which may contribute to its hypotensive effect.

Prognostic predictors for patients with hepatocellular carcinoma receiving adjuvant transcatheter arterial chemoembolization.

OBJECTIVES: We aimed to confirm the clinical effectiveness of postoperative adjuvant transcatheter arterial chemoembolization (PA-TACE) in patients with hepatocellular carcinoma after liver resection, and further identify the patients who could benefit most from PA-TACE. PATIENTS AND METHODS: Propensity score matching at a ratio of 1 : 2 was used between hepatectomy patients with and without receiving PA-TACE. Kaplan-Meier analysis was performed to compare overall survival and recurrence-free survival between two groups. Univariate COX regression and stratified analyses were performed to screen and identify survival predictors for PA-TACE patients. The identified predictive markers were validated in an external cohort. RESULTS: The propensity analysis matched 116 patients in PA-TACE group to 232 in the control group. Visible protective effect of PA-TACE was shown by survival curves in matched series (log-rank P=0.009 and 0.008), with hazard ratio of being 0.599 (95% confidence interval: 0.420-0.855) and 0.623 (95% confidence interval: 0.449-0.866), respectively, for overall survival and recurrence-free survival. The identified prognostic predictors for PA-TACE included TNM stage, tumor size and number, hepatitis B infection, spleen diameter, preoperative serum α-fetoprotein, alkaline phosphatase, γ-glutamyl transpeptidase and monocyte, and three risk signatures (aspartate aminotransferase-to-alanine aminotransferase ratio, neutrophil-to-lymphocyte ratio, and systemic immune-inflammation index). CONCLUSION: The treatment effectiveness of adjuvant transcatheter arterial chemoembolization for patients with hepatocellular carcinoma after surgery was validated in this study, and the best candidates for PA-TACE were identified as well, including patients with late-stage tumor, portal hypertension, and high preoperative serum levels of α-fetoprotein, alkaline phosphatase, γ-glutamyl transpeptidase, and monocytes.

Diallyl disulphide inhibits apolipoprotein(a) expression in HepG2 cells through the MEK1-ERK1/2-ELK-1 pathway.

BACKGROUND: Lipoprotein(a) [LP(a)] is implicated as a common and independent risk factor for cardiovascular diseases. The therapeutic options currently available for reducing plasma LP(a) concentrations are limited. Diallyl disulphide (DADS), the main component of garlic, regulates lipid metabolism in hepatocytes and adipocytes through ERK1/2 signalling. This study aimed to assess the effect of DADS on apolipoprotein(a) [apo(a)] in HepG2 cells. We also determined the effects of DADS on apo(a) expression and secretion in HepG2 cells as well as the underlying mechanisms. METHODS: We examined the role of DADS on apo(a) expression in HepG2 cells by treating cell with different concentrations of DADS (10, 20, 40 and 80 µg/mL) for 24 h or treating cells with 40 µg/mL DADS for 0, 6, 12, 24 and 48 h. Then we used quantitative real-time PCR to analysis apo(a) mRNA levels, used Western blot to analysis apo(a) protein levels and used enzyme-linked immunosorbent assay to test apo(a) secreted levels. To farther determined the role of DADS, we applied Transfection of small interfering RNA to knockdown ELK-1levels and applied PD98059, a specific inhibitor of ERK1/2, to block ERK1/2 signal. RESULTS: The results show DADS inhibited apo(a) at both the mRNA and protein levels in HepG2 cells in a dose-dependent manner. DADS-mediated inhibition of apoa(a) expression in HepG2 cells was attenuated when the cells were cultured in medium containing PD98059 (ERK1/2 inhibitor) or were transfected with siRNAs against MEK1 or ELK-1. Overexpression of apo(a) yielded similar results. CONCLUSIONS: This study reveals that DADS can downregulate apo(a) expression in a dose-dependent manner via the MEK-ERK12-ELK-1 pathway.

Quantitative Metabolomic Profiling of Plasma, Urine, and Liver Extracts by 1H NMR Spectroscopy Characterizes Different Stages of Atherosclerosis in Hamsters.

Atherosclerosis (AS) is a progressive disease that contributes to cardiovascular disease and shows a complex etiology, including genetic and environmental factors. To understand systemic metabolic changes and to identify potential biomarkers correlated with the occurrence and perpetuation of diet-induced AS, we applied 1H NMR-based metabolomics to detect the time-related metabolic profiles of plasma, urine, and liver extracts from male hamsters fed a high fat and high cholesterol (HFHC) diet. Conventional biochemical assays and histopathological examinations as well as protein expression analyses were performed to provide complementary information. We found that diet treatment caused obvious aortic lesions, lipid accumulation, and inflammatory infiltration in hamsters. Downregulation of proteins related to cholesterol metabolism, including hepatic SREBP2, LDL-R, CYP7A1, SR-BI, HMGCR, LCAT, and SOAT1 was detected, which elucidated the perturbation of cholesterol homeostasis during the HFHC diet challenge. Using "targeted analysis", we quantified 40 plasma, 80 urine, and 60 liver hydrophilic extract metabolites. Multivariate analyses of the identified metabolites elucidated sophisticated metabolic disturbances in multiple matrices, including energy homeostasis, intestinal microbiota functions, inflammation, and oxidative stress coupled with the metabolisms of cholesterol, fatty acids, saccharides, choline, amino acids, and nucleotides. For the first time, our results demonstrate a time-dependent metabolic progression of multiple biological matrices in hamsters from physiological status to early AS and further to late-stage AS, demonstrating that 1H NMR-based metabolomics is a reliable tool for early diagnosis and monitoring of the process of AS.

Effects of ligustilide on lipopolysaccharide-induced endotoxic shock in rabbits.

In this study, we investigated the protective effects of ligustilide against lipopolysaccharide (LPS)-induced endotoxic shock in Japanese white rabbits and attempted to elucidate the possible mechanism underlying these effects. Forty-two rabbits were randomized into 6 groups: normal group, LPS group, dexamethasone group (5 mg/kg), and 3 ligustilide groups (20, 40, and 80 mg/kg). After the rabbits had received a LPS infusion (0.3 mg/kg), dexamethasone and ligustilide were intravenously injected at the above-mentioned dosages. Heart rate (HR), mean arterial pressure (MAP), and rectal temperature (RT) were recorded throughout the experiment. Tumor necrosis factor- α (TNF- α), interleukin-1 ß (IL-1 ß), and nitric oxide (NO) levels were measured by radioimmunoassay every 30 minutes for the first hour and every 60 minutes thereafter until the end of the experiment. The serum levels of alanine transaminase (ALT), aspartate transaminase (AST), alkaline phosphatase (ALP), γ-glutamyl transpeptidase (GGT), creatinine kinase (CK), lactate dehydrogenase (LDH), total protein (TP), creatinine (Scr), blood urea nitrogen (BUN), total bilirubin (T. BIL), and counts of formed elements of blood were measured at 0, 120, and 300 minutes after the administration of LPS. Hemorheology was assayed 300 minutes after the LPS injection. The vital organs were collected and weighed before histopathologic examination. A comparison between the LPS group and the ligustilide groups showed that ligustilide significantly inhibited the decline in MAP and RT and decreased the levels of TNF- α, IL-1 ß, and NO, but had no apparent effect on HR. Ligustilide also inhibited the increase in the levels of biochemical markers, such as ALT, AST, ALP, GGT, LDH, CK, BUN, and Scr, but showed no apparent effect on T. BIL and TP. Furthermore, ligustilide partly restored the function of injured vital organs, including the heart, liver, lungs, and kidneys. These results suggest that ligustilide protected the rabbits against LPS-induced endotoxic shock.

[Common syndrome factors of traditional Chinese medicine in chronic renal failure based on the questionnaire investigation among experts].

OBJECTIVE: To screen common traditional Chinese medicine (TCM) syndrome factors of chronic renal failure (CRF) via questionnaire investigation among experts. METHODS: A questionnaire was developed based on the results of our previous researches. The investigation was carried out with the questionnaire among experts who are engaged in clinical research and treatment of nephrosis with the title of chief or associate chief physician from 15 hospitals in China. Common TCM syndrome factors of CRF were obtained based on the data analysis of the mean value on general evaluation, cumulative percentage and coefficient of variation. RESULTS: A total of 114 sets of the questionnaire were sent out and all of them were returned back, 113 of which were effective. The recovery rate is 100%. The TCM syndrome factors were regarded as common factors of CRF syndrome if the cumulative percentage was more than or equal to 60% and the coefficient of variation was less than or equal to 0.35. The syndrome factors related to the disease location were the kidney, spleen, stomach, heart, and lung; the syndrome factors related to the disease type were dampness, turbid toxin, blood stasis, water retention, and phlegm which belong to excess type, and qi deficiency, yin deficiency, yang deficiency, blood deficiency, and essence deficiency which belong to deficiency type. CONCLUSION: The common TCM syndrome factors of CRF were obtained from the representative experts through the questionnaire investigation among the experts. The results enable us to have a deeper understanding of the disease in view of TCM compared with the previous literature data and may contribute to the establishment of TCM syndrome diagnosis criteria of the disease in the future.

[A perspective of developing syndrome diagnostic criteria based on syndrome factors and combination of disease in modern medicine system and syndrome in traditional Chinese medicine system].

Syndrome differentiation treatment is the traditional model of diagnosis and treatment of diseases in traditional Chinese medicine (TCM). To establish scientific diagnostic criteria of TCM syndrome is one of the key points in TCM study. In this paper, the basic models of the relevant diagnostic criteria of TCM syndrome and existed problems were reviewed. The authors pointed out the advantages of establishing diagnostic criteria of TCM syndrome based on TCM syndrome factors and combination of disease in Western medicine system and TCM syndrome, in which not only the characteristics of the disease in Western medicine were considered, but also the complexity and flexibility of syndrome identification and convenient application in clinical practice were resolved. The basic model and frame of the above diagnostic criteria and the procedures and methods used in developing the diagnostic criteria were also described and discussed.

Antihypertensive effect of 3,3,5,5-tetramethyl-4-piperidone, a new compound extracted from Marasmius androsaceus.

AIM OF THE STUDY: To evaluate the antihypertensive effect of 3,3,5,5-tetramethyl-4-piperidone (TMP), a new compound extracted from Marasmius androsaceus. Besides, the hemodynamic profiles and pertinent mechanism of the compound were explored. MATERIALS AND METHODS: Acute and chronic antihypertensive effects of TMP were examined in spontaneous hypertensive rats (SHRs) and reno-hypertensive rats (two kidneys one clip model, 2K1C). Anesthetized dogs were used to evaluate the hemodynamic effects of TMP. Moreover, the cat nictitating membrane response was used to test the ganglionic blocking property of TMP. RESULTS: TMP (2.5, 5 and 10mg/kg, p.o.) notably reduced the blood pressure of SHR in 30 min. Two-week administration of TMP (2.5, 5 and 10mg/kg, p.o.) also decreased the blood pressure of 2K1C rats. TMP (30 mg/kg, i.v.) abolished the response of the nictitating membrane induced by preganglionic stimulation. The results of hemodynamic study in anesthetized dogs showed that, except for the reduction in blood pressure and left ventricular work, no other changes were detected. The results of heart rate variability analysis indicated an intact sympathetic-vagal balance after TMP treatment. CONCLUSIONS: TMP is a new antihypertensive compound, and the effect is partially related to ganglionic blocking.

Gossypium herbaceam extracts inhibited NF-kappaB activation to attenuate spatial memory impairment and hippocampal neurodegeneration induced by amyloid-beta in rats.

Amyloid-beta (Abeta) is considered to be responsible for the pathogenesis of Alzheimer's disease. In the present study, the protective effect of Gossypium herbaceam extracts (GHE) on learning and memory impairment induced by Abeta were examined in vivo using Morris water maze and step through task. Furthermore, the antioxidant activity and neuroprotective effect of GHE was investigated with methods of histochemistry and biochemistry. These data showed that oral administration with GHE at the doses of 35, 70 and 140 mg/kg exerted an improved effect on the learning and memory impairment in rats induced by intracerebroventricular (i.c.v.) injection of 10 microg of Abeta(25-35). Subsequently, the GHE afforded a beneficial action on promotion on the activity of glutathione peroxidase and catalase, as well as inhibition on the NF-kappaB activation in the hippocampus followed by the presence of Abeta(25-35). Meanwhile, the number of degenerating neurons with an apoptotic feature was dramatically decreased in hippocampus after treatment with GHE, implicating that its antioxidant stress and inhibition of NF-kappaB activation could be involved in the mechanism underlying neuroprotection of GHE against Abeta-induced cell death. These findings suggested that GHE might be a potential agent for treatment of Alzheimer's disease.

Fast profiling of the integral metabolism of flavonols in the active fraction of Gossypium herbaceam L. using liquid chromatography/multi-stage tandem mass spectrometry.

A method of fast profiling the constituents in an active herbal extract and their metabolites in biological fluids based on the combination of fragmentation behavior and metabolic pathways is described. The complementary information from fragmentation behavior and metabolic pathways helped not only to identify the structure of parent constituents and metabolites, but also to correlate metabolites back to their parent forms. An active fraction obtained from Gossypium herbaceam L., named AB-8-2, and bile samples from rats administered it orally and intravenously were analyzed using high-performance liquid chromatography/multi-stage tandem mass spectrometry (HPLC-MSn) in a single chromatographic run. Fifty-eight flavonols comprising mixed sulfate, methyl, glucuronide and glycoside derivatives of quercetin or kaempferol were detected, including several groups of isomers. By contrasting the analytical results from AB-8-2 and from bile samples derived from different administration routes, a profile of the biotransformation of the flavonols in AB-8-2 was obtained. The results should be of benefit in targeting potential active ingredients in complex mixtures, such as herbs or their active extracts.