Diterpenes

Publication Title: 
Basic & Clinical Pharmacology & Toxicology

Transient receptor potential melastatin 7 (TRPM7) plays a role in a number of physiological and pharmacological functions in variety of cells. The aim of this study was to clarify the role for TRPM7 channels and the effect of waixenicin A on the pacemaking activity of interstitial cells of Cajal (ICCs) and on the cell viability of the human gastric and breast adenocarcinoma cell lines, AGS and MCF-7, respectively.

Author(s): 
Kim, Byung J.
Nam, Joo H.
Kwon, Young K.
So, Insuk
Kim, Seon J.
Publication Title: 
Cell

Traditional medicines provide fertile ground for modern drug development, but first they must pass along a pathway of discovery, isolation, and mechanistic studies before eventual deployment in the clinic. Here, we highlight the challenges along this route, focusing on the compounds artemisinin, triptolide, celastrol, capsaicin, and curcumin.

Author(s): 
Corson, Timothy W.
Crews, Craig M.
Publication Title: 
Current Drug Discovery Technologies

Traditional Chinese Medicines (TCM) are rapidly gaining attention in the West as sources of new drugs, dietary supplements and functional foods. However, lack of consistent manufacturing practices and quality standards, fear of adulteration, and perceived deficiencies in scientific validation of efficacy and safety impede worldwide acceptance of TCM. In addition, Western pharmaceutical industries and regulatory agencies are partial toward single ingredient drugs based on synthetic molecules, and skeptical of natural product mixtures.

Author(s): 
Graziose, Rocky
Lila, Mary Ann
Raskin, Ilya
Publication Title: 
Journal of Ethnopharmacology

ETHNOPHARMACOLOGICAL RELEVANCE: Ajuga bracteosa Wall Ex Benth. (Labiateae) is described in Ayurveda for the treatment of rheumatism, gout, palsy and amenorrhea. AIM OF THE STUDY: The aim of present investigation is to study anti-inflammatory activity of Ajuga bracteosa, to understand possible mechanism of action and to identify the constituents responsible for its activity.

Author(s): 
Gautam, Raju
Jachak, Sanjay M.
Saklani, Arvind
Publication Title: 
Xenobiotica; the Fate of Foreign Compounds in Biological Systems

Andrographolide is a major labdane diterpenoid of the traditional Chinese and Ayurvedic medicine. Andrographis paniculate (Burm) Nees, is used in clinical situations in China mainly to treat fever, cold, and inflammation. In our previous study, fifteen metabolites of andrographolide were identified in human urine. However, there are still two other unknown metabolites. The aim of this study was to elucidate the structures of these two metabolites. 3.

Author(s): 
Qiu, Feng
Cui, Liang
Chen, Lixia
Sun, Jiawen
Yao, Xinsheng
Publication Title: 
Alcohol (Fayetteville, N.Y.)

Andrographis paniculata (AP) is a traditional medicinal plant of Ayurveda. It grows widely in Asia and is prescribed in the treatment of liver diseases. Here we have investigated the beneficial role of 14-deoxyandrographolide (14-DAG), a bioactive diterpenoid from AP, against alcoholic steatosis in rats. 14-DAG was extracted from aerial parts (leaves and stems) of AP. Rats were fed with ethanol for 8 weeks. Animals were treated with 14-DAG during the last 4 weeks of ethanol treatment. In vitro studies were undertaken in a human hepatocellular liver carcinoma cell line culture.

Author(s): 
Mandal, Samir
Mukhopadhyay, Sibabrata
Bandhopadhyay, Sukdeb
Sen, Gargi
Biswas, Tuli
Publication Title: 
The Journal of Biological Chemistry

Many transient receptor potential (TRP) channels are activated or blocked by various compounds found in plants; two prominent examples include the activation of TRPV1 channels by capsaicin and the activation of TRPM8 channels by menthol. We sought to identify additional plant compounds that are active on other types of TRP channels. We screened a library of extracts from 50 Chinese herbal plants using a calcium-imaging assay to find compounds active on TRPV3 and TRPV4 channels. An extract from the plant Andrographis paniculata potently activated TRPV4 channels.

Author(s): 
Smith, Paula L.
Maloney, Katherine N.
Pothen, Randy G.
Clardy, Jon
Clapham, David E.
Publication Title: 
Phytochemistry

Plants in the genus Tripterygium, such as Tripterygium wilfordii Hook.f., have a long history of use in traditional Chinese medicine. In recent years there has been considerable interest in the use of Tripterygium extracts and of the main bioactive constituent, the diterpene triepoxide triptolide (1), to treat a variety of autoimmune and inflammation-related conditions.

Author(s): 
Brinker, Anita M.
Ma, Jun
Lipsky, Peter E.
Raskin, Ilya
Publication Title: 
Phytochemical analysis: PCA

Extracts of Tripterygium wilfordii Hook F. have been widely used in China to treat a variety of autoimmune and inflammatory diseases. The diterpenoids triptolide and tripdiolide are two major active components in the T. wilfordii ethyl acetate extract. An efficient solid-phase extraction and high-performance liquid chromatography (SPE-HPLC) method to measure triptolide content in the extract has been previously reported. However, a suitable means of tripdiolide quantification is not available because of interfering compounds in the extract that co-elute with tripdiolide.

Author(s): 
Ma, Jun
Schmidt, Barbara M.
Poulev, Alexander
Raskin, Ilya
Publication Title: 
Frontiers in Bioscience: A Journal and Virtual Library

Cancer chemoprevention by phytochemicals may be one of the most feasible approaches for cancer control. Phytochemicals obtained from vegetables, fruits, spices, teas, herbs and medicinal plants, such as terpenoids and other phenolic compounds, have been proven to suppress experimental carcinogenesis in various organs in pre-clinical models.

Author(s): 
Rabi, Thangaiyan
Gupta, Sanjay

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