Herbal Active Ingredients Research Articles

HIM-herbal ingredients in-vivo metabolism database

BackgroundHerbal medicine has long been viewed as a valuable asset for potential new drug discovery and herbal ingredients’ metabolites, especially the in vivo metabolites were often found to gain better pharmacological, pharmacokinetic and even better safety profiles compared to their parent compounds. However, these herbal metabolite information is still scattered and waiting to be collected.DescriptionHIM database manually collected so far the most comprehensive available in-vivo metabolism information for herbal active ingredients, as well as their corresponding bioactivity, organs and/or tissues distribution, toxicity, ADME and the clinical research profile. Currently HIM contains 361 ingredients and 1104 corresponding in-vivo metabolites from 673 reputable herbs. Tools of structural similarity, substructure search and Lipinski’s Rule of Five are also provided. Various links were made to PubChem, PubMed, TCM-ID (Traditional Chinese Medicine Information database) and HIT (Herbal ingredients’ targets databases).ConclusionsA curated database HIM is set up for the in vivo metabolites information of the active ingredients for Chinese herbs, together with their corresponding bioactivity, toxicity and ADME profile. HIM is freely accessible to academic researchers at http://www.bioinformatics.org.cn/.

1339 – Sh-sy5y/cmc, a new screening method of antipsychotic chinese herbal active ingredients

We describe an analytical method of SH-SY5Y cell membrane chromatography (SH-SY5Y/CMC) for recognition, separation and identification of active components from traditional Chinese medicines (TCMs). SH-SY5Y cells by means of culture with SH-SY5Y cell lines were used for preparation of the stationary phase in the CMC model. Retention components by the SH- SY5Y/CMC model were collected and active components then analyzed by SH-SY5Y/CMC under the optimized conditions. After investigating the suitability and reliability of the SH-SY5Y /CMC method using risperidone, sertraline and clozapine as standard compounds, this method was applied in screening active components from the extracts of TCMs such as Radix Gentianae, Radix Bupleuri, stir-baked semen ziziphi spinosae, rehmannia dride rhizome, uncaria rhynchophylla. Retention components from the extracts in the SH-SY5Y/CMC model were gentiopicrin and rosmarinci acid identified by the GC/MS method. In vitro pharmacological trials indicated that gentiopicrin and rosmarinci acid could concentration dependently protect the SH-SY5Y pre-treated by H 2 O 2 (P

Variable inhibitory effect of herbal supplements of different brands on human P450 CYP1A2.

Herbal supplements are not governed by the same regulations as prescription drugs, we hypothesize that the content of their active ingredients may vary largely among different manufacturers. This may produce variable therapeutic outcomes. This study aims to examine this hypothesis on commonly used herbal supplements among cancer patients. CYP1A2 has been implicated in the activation of many carcinogens and alteration in its activity may be a mechanism associated with the protective effect of herbal products. Activity of human CYP1A2 was used to determine the effect of four herbal supplements of different brands, namely, black cohosh (BC), ginseng, grape seed extract (GSE) and green tea extract (GTE). The herbal content was extracted with methanol, and extract aliquots were used to determine their effect on CYP1A2. Human liver microsomes, the CYP1A2 probe (7-ethoxyresorufin) and NADPH in buffer were incubated with and without herbal extract. Metabolite (resorufin) formation was monitored by HPLC. Seven BC products caused a mild inhibition of CYP1A2, ranging from 2.4 % by GNC Plus to 21.9 % by Nature's Resource. Among nine ginseng products tested, the inhibitory effect varied from 4.2 % by Imperial to 44.6 % by Solarays. The effect of nine GSE brands also varied, ranging from 1.7 % (Country Life) to 26.5 % (Veg Life). Of twelve GTE products, the inhibitory effect varied from 2.9 % by Henry's to 46.6 % by GNC Plus. It appears that the inhibition of selected herbal supplements on CYP1A2 activity varies considerably among different brands of the products. This may be due to variations in the herbal products' active ingredients content.

Novel Natural Inhibitors of CYP1A2 Identified by in Silico and in Vitro Screening

Inhibition of cytochrome P450 (CYP) is a major cause of herb–drug interactions. The CYP1A2 enzyme plays a major role in the metabolism of drugs in humans. Its broad substrate specificity, as well as its inhibition by a vast array of structurally diverse herbal active ingredients, has indicated the possibility of metabolic herb–drug interactions. Therefore nowadays searching inhibitors for CYP1A2 from herbal medicines are drawing much more attention by biological, chemical and pharmological scientists. In our work, a pharmacophore model as well as the docking technology is proposed to screen inhibitors from herbal ingredients data. Firstly different pharmaphore models were constructed and then validated and modified by 202 herbal ingredients. Secondly the best pharmaphore model was chosen to virtually screen the herbal data (a curated database of 989 herbal compounds). Then the hits (147 herbal compounds) were continued to be filtered by a docking process, and were tested in vitro successively. Finally, five of eighteen candidate compounds (272, 284, 300, 616 and 817) were found to have inhibition of CYP1A2 activity. The model developed in our study is efficient for in silico screening of large herbal databases in the identification of CYP1A2 inhibitors. It will play an important role to prevent the risk of herb–drug interactions at an early stage of the drug development process.

A Study of Antimicrobial Activity of Few Medicinally Important Herbal Single Drugs Extracted in Ethanol, Methanol and Aqueous Solvents

There is a currently worldwide upsurge in the use of herbal preparations and active ingredients of medicinal plant in health care. This is particularly true in the rural areas of Asian countries where herbal medicines are the only choice for treating human ailments. Present study reveals the difference in the antimicrobial activity pattern of Hemidesmus indicus, Smilax china,Ocimum basilicum, Ocimum sanctum, Ocimum cannum, Azadirachta indica A.Juss, Trigonella Foenum graceum and piper cubeba extracted in Ethanol, Methanol and Aqueous solvents against the pathogenic organisms E.coli (ATCC-25922), Staphylococcus aureus (ATCC-25923), Pseudomonas aeruginosa (ATCC-27853), Bacillus subtilis(L10969), Bacillus subtilis (SL5740) and clinically isolated strains Shigella, Klebsiella, Proteus, Salmonella paratyphi, Salmonella typhi and Stapylococcus aureus. Among all the extracts Ethanol shows more activity with a zone of inhibition ranges from 10mm to 22mm. And Aqueous extract shows less inhibition which ranges from 6mm to 11mm.

Gene Expression Profiling as an Initial Approach for Mechanistic Studies of Toxicity and Tumorigenicity of Herbal Plants and Herbal Dietary Supplements

Dietary supplements are consumed by more than 300 million people worldwide, and herbal dietary supplements represent the most rapidly growing portion of this industry. Even though adverse health effects of many herbal dietary supplements have been reported, safety assurances are not being addressed adequately. Toxicological data on the identification of genotoxic and tumorigenic ingredients in many raw herbs are also lacking. Currently, more than 30 herbal dietary supplements and active ingredients have been selected by the National Toxicology Program (NTP) for toxicity and tumorigenicity studies. Due to the complexity of the chemical components present in plant extracts, there are no established methodologies for determining the mechanisms of toxicity (particularly tumorigenicity) induced by herbs, such as Gingko biloba leaf extract (GBE) and other herbal plant extracts. Consequently, the understanding of toxicity of herbal dietary supplements remains limited. We have proposed that application of DNA microarrays could be a highly practical initial approach for revealing biological pathways and networks associated with toxicity induced by herbal dietary supplements and the generation of hypotheses to address likely mechanisms. The changes in expression of subsets of genes of interest, such as the modulation of drug metabolizing genes, can be analyzed after treatment with an herbal dietary supplement. Although levels of gene expression do not represent fully the levels of protein activities, we propose that subsequent biochemical and genomic experiments based on these initial observations will enable elucidation of the mechanisms leading to toxicity, including tumorigenicity. This review summarizes the current practices of microarray analysis of gene expressions in animals treated with herbal dietary supplements and discusses perspectives for the proposed strategy.