Since the middle of this century and especially since the 1960s and 1970s. Chinese scientists have put considerable effort and resources into the search for new antimalarial compounds extracted from Chinese traditional herbs. Archaeological findings indicate that qinghao (Artemisia annua L.) has been used as a traditional remedy in China for over two thousand years. Its antimalarial principle was finally isolated in 1971 and named artemisinin or qinghaosu (meaning the principle of qinghao in Chinese). Its rapid action, low toxicity and powerful effect against falciparum malaria made it a favored subject for research. In 1976, the unique structure of the molecule, characterized by an endoperoxide and an alternative O-C-O-C segment, was identified. The specific lactone reduction discovered during the determination of the structure opened the way for the synthesis of qinghaosu derivatives, and thereafter a series of more active and more oil- or water-soluble derivatives was developed. Subsequent studies of the structure/activity relationship led to the discovery of dihydroartemisinin, artemether and artesunate. Now qinghaosu and these three derivatives are being used around the world as effective new antimalarial drugs in the fight against falciparum malaria, including multi-drug-resistant Plasmodium falciparum. At the present time new qinghaosu analogues or derivatives are being developed and studies of their structure/activity relationships, their antimalarial mechanisms, their interaction with ferrous ions and the DNA damage associated with these processes are being actively pursued. In addition, recent studies also indicate that some qinghaosu derivatives have other bioactivities, including antiparasitic (against Schistosoma japonicum, Toxoplasma gondii and so on) and anticancer activities. Research into qinghaosu and its derivatives has already produced and will no doubt continue to produce results of the utmost importance in the fight against malaria and other diseases.
[Show abstract][Hide abstract] ABSTRACT: In recent years, increasing numbers of people have been choosing herbal medicines or products to improve their health conditions, either alone or in combination with others. Herbs are staging a comeback and herbal "renaissance" occurs all over the world. According to the World Health Organization, 75% of the world's populations are using herbs for basic healthcare needs. Since the dawn of mankind, in fact, the use of herbs/plants has offered an effective medicine for the treatment of illnesses. Moreover, many conventional/pharmaceutical drugs are derived directly from both nature and traditional remedies distributed around the world. Up to now, the practice of herbal medicine entails the use of more than 53,000 species, and a number of these are facing the threat of extinction due to overexploitation. This paper aims to provide a review of the history and status quo of Chinese, Indian, and Arabic herbal medicines in terms of their significant contribution to the health promotion in present-day over-populated and aging societies. Attention will be focused on the depletion of plant resources on earth in meeting the increasing demand for herbs.
Evidence-based Complementary and Alternative Medicine 04/2014; 2014:525340. DOI:10.1155/2014/525340 · 1.88 Impact Factor
"In recent years, studies have demonstrated that artemisinin and its derivatives had a significant cytotoxic effects toward cancer cells and could reverse multiple drug resistance of tumors –. Artemisinin was first isolated from leaves of Artemisia annua, a Chinese traditional herb, by Chinese pharmacists in 1971 . Artemether, the methyl ether derivative of artemisinin, is widely used in the therapy of malaria . "
[Show abstract][Hide abstract] ABSTRACT: Artemether is the derivative extracted from Chinese traditional herb and originally used for malaria. Artemether also has potential therapeutic effects against tumors. Vascular cell adhesion molecule-1 (VCAM-1) is an important cell surface adhesion molecule associated with malignancy of gliomas. In this work, we investigated the role and mechanism of artemether combined with shRNA interference of VCAM-1 (shRNA-VCAM-1) on the migration, invasion and apoptosis of glioma cells. U87 human glioma cells were treated with artemether at various concentrations and shRNA interfering technology was employed to silence the expression of VCAM-1. Cell viability, migration, invasiveness and apoptosis were assessed with MTT, wound healing, Transwell and Annexin V-FITC/PI staining. The expression of matrix metalloproteinase-2 (MMP-2), matrix metalloproteinase-9 (MMP-9) and phosphorylated Akt (p-Akt) was checked by Western blot assay. Results showed that artemether and shRNA-VCAM-1 not only significantly inhibited the migration, invasiveness and expression of MMP-2/9 and p-Akt, but also promoted the apoptosis of U87 cells. Combined treatment of both displayed the maximum inhibitory effects on the malignant biological behavior of glioma cells. Our work revealed the potential therapeutic effects of artemether and antiVCAM-1 in the treatments of gliomas.
PLoS ONE 04/2013; 8(4):e60834. DOI:10.1371/journal.pone.0060834 · 3.23 Impact Factor
"Reduction of the lactone in dihydroartemisinin and artemether has led to increased oil solubility, whereas the acidic moiety lends water solubility to artesunate [88, 89]. Consequently, artemisinin derivatives, such as dihydroartemisinin, artemether, and artesunate, are developed and being used around the world as effective antimalarial drugs, including those targeted against multidrug-resistant Plasmodium falciparum . These derivatives appear to be more potent than the parent compound and the most rapidly acting among all other antimalarial agents . "
[Show abstract][Hide abstract] ABSTRACT: With tens of thousands of plant species on earth, we are endowed with an enormous wealth of medicinal remedies from Mother Nature. Natural products and their derivatives represent more than 50% of all the drugs in modern therapeutics. Because of the low success rate and huge capital investment need, the research and development of conventional drugs are very costly and difficult. Over the past few decades, researchers have focused on drug discovery from herbal medicines or botanical sources, an important group of complementary and alternative medicine (CAM) therapy. With a long history of herbal usage for the clinical management of a variety of diseases in indigenous cultures, the success rate of developing a new drug from herbal medicinal preparations should, in theory, be higher than that from chemical synthesis. While the endeavor for drug discovery from herbal medicines is "experience driven," the search for a therapeutically useful synthetic drug, like "looking for a needle in a haystack," is a daunting task. In this paper, we first illustrated various approaches of drug discovery from herbal medicines. Typical examples of successful drug discovery from botanical sources were given. In addition, problems in drug discovery from herbal medicines were described and possible solutions were proposed. The prospect of drug discovery from herbal medicines in the postgenomic era was made with the provision of future directions in this area of drug development.
Evidence-based Complementary and Alternative Medicine 03/2013; 2013:627375. DOI:10.1155/2013/627375 · 1.88 Impact Factor
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