Folk Chinese

Two major breakthroughs of the past few decades have renewed the assault of scientists to this infective disease. The first is the complete sequencing of the genome of Plasmodium falciparum [4] that is expected to provide useful information for the identification of new drug targets. The second is the discovery by Chinese researchers of artemisinin (qinghaosu), an endoperoxide sesquiterpene lactone, as the active principle of the sweet wormwood, Artemisia annua, an herbal remedy used in folk Chinese medicine for 2000 years [5]. This molecule and its... 

Antibiotics were used in folk medicine at least as early as 2500 years ago when the Chinese reported the medicinally beneficial effects of moldy bean curd. Evidence for some type of tetracycline antibiotic usage by the Sudanese-Nubian civilization (350 AD) was reported in 1980 (6). Fluorescent areas in human bones from this eta were observed that were identical in location and characteristics to modern bone from patients treated with tetracyclines. Identification of tetracycline in the ancient bones was further substantiated by fluorescence spectmm measurements and microbiological inhibition studies (7). 

Copper hydride species, notably Stryker s reagent [Ph3PCuH]6, are capable of promoting the conjugate reduction of a,( >-unsalurated carbonyl compounds [42], Taking advantage of this trustworthy method, Chiu et al. demonstrated in 1998 an intramolecular reductive aldol reaction in the synthesis of novel terpenoid pseudolaric acids isolated from Chinese folk medicine (Scheme 28) [43]. Two equivalents of [Ph3PCuH]6 enabled cycli-zation of keto-enone 104 to provide the bicyclic diastereomers 105 (66%) and 106 (16%). The reaction also was applied to the transformation of 107... 

Hirsutine (2-795), which belongs to the corynanthe subgroup of the indole alkaloids, was isolated from the plant Uncaria rhynchophylla MIQ and used for the preparation of the old Chinese folk medicine Kampo [397]. It is of pharmacological interest as it shows a strong inhibitory effect on the influenza A virus (subtype H3N2) with an EC50 = 0.40-0.57 pg ml. which is about 11- to 20-fold higher than that of the clinically used ribavirin [398]. 

The hypocrellins (7-9) are Class B perylenequinones that have also been the subject of much investigation due to their biological activity, having been used in Chinese folk medicine for the treatment of vitiligo, psoriasis, and other diseases for... 

Cucurbitine (47) is the active principle from the seeds of Cucurbita moschata Duch., which are used in Chinese folk medicine. The structure of this unique a-amino acid was established through a combination of chemical and spectroscopic techniques (81, 82). A single-crystal X-ray analysis of the perchlorate of cucurbitine has confirmed the original hypothesis and has established the absolute configuration of 47 (83). 

A new medicine that seems to be promising in this field is artimisinine (19) isolated from Artimisia annua. Extracts of this plant have been known for centuries in Chinese folk medicine under the name of Qinghaosu or Qinghao. For solubility reasons and hydrolysis stability, artimisinine is converted via the dihydro compound into water-soluble artesunate or oil soluble artemether and arteether (Scheme 5.12) [43]. 

Native to tropical America, sweet potato (I. batatas) is a perennial morning glory vine that has been cultivated for over 5,000 years for its edible tubers in Mexico, Central and lowland South America, and the West Indies. Today, sweet potato is cultivated around the world, especially in developing countries (Plate 4). A decoction made from the leaves of this plant is used in folk remedies as a gargle to treat mouth and throat tumors, and poultices are prepared for inflammatory tumors (64). In Mexico, leaf decoctions are considered to be of cold nature , to reduce excessive body heat, contemporarily defined as such illnesses as diarrhea, dysentery, heart disease, stomach distress, fever, and gastrointestinal infection. In Chinese traditional medicine, the tubers have been used as a medicinal herb to eliminate secretion in perceived abnormal quantities of blood or other body fluids (79). 

Quinghaosu is the latest fundamental discovery in this area and is a heterocyclic compound that does not have a nitrogen atom in its structure. It is taken from a Chinese folk medicine. It is isolated from the plmt Artemisia annua. It is amazing that this compound, which is completely different than the other drugs described in this chapter in terms of structure, exhibits the exact same therapeutic effect. The main interest in quinoghaosu is based on the fact that it is active against resistant forms of malaria caused by P falciparum, and even its cerebral forms. Synonyms of this drug are artemisine, artemisinin, and others. 

Fukai, T. et al.. Phenolic constituents of Glycyrrhiza species. 17. Three isoprenoid-substituted isoflavans, gancaonins X-Z, from Chinese folk medicine Tiexin Gancao (root xylems of Glycyrrhiza species). Natural Medicines, 48, 203, 2004. 

The use of sulfoximines in the syntheses of optically active compounds has been reported [429]. A remarkable ketone methylcnation with optical resolution was realized. A highly selective diastereofacial addition of an enantiopure sulfoximine to a racemic ketone, chromatographic separation of the two diastereoisomers and reductive cleavage yielded both enantiomers of p-panasinsene [430], isolated from the root of ginseng, a herb used in Chinese folk medicine. 

Only four inhibitors of AChE have been approved as therapeutic drugs for combating dementia diseases. The very first is tacrine or Cognex [Figure 2] from Parke-Davis8 and the second is aricept from Eisai [Japan] and Pfizer [U.S.].9 A third inhibitor available is huperzine A, a "nootropic" agent isolated from a Chinese folk medicine and used by Chinese for centuries to improve memory.10 Other known reversible AChE inhibitors... 

Various species of Ephedra grow in different parts of the world. It is believed that the Chinese species contain the official levorotatory ephedrine, whereas the same species and other varieties from Europe yield only dextrorotatory pseudoephedrine. East Indian species range from rich to none. Ephedrine exists in the seed of another, totally unrelated Indian plant, Sida cordifolia, which was also used in folk medicine. Ma huang also contains another alkaloid, ephedine, which lowers blood pressure and has other complex actions. 

In folk medicine and traditional systems of medicine, various species of valerian have been used as an oral infusion to treat migraine headaches, hysteria, nervous unrest, neurasthenia, fatigue, seizures, stomach cramps that cause vomiting, and other nervous conditions. Valerian also has been used internally as a spasmolytic, a carminative, and a stomachic, and externally on cuts, sores, and acne. Some herbalists recommend it as a possible vermifuge. In Chinese medicine, valerian is used to treat the aforementioned conditions, as well as chronic headache, numbness due to rheumatic conditions, colds, menstrual difficulties, and bruises. Because there has been no extensive research conducted on uses other that the sedative properties of valerian and its constituents, these other uses cannot be scientifically evaluated. 

Many of the herbal drugs used in the United Sates and Europe are derived from traditional Chinese medicine and Ayurvedic medicine in India. These traditions are thousands of years old, and they rely heavily on plant-based prescriptions to treat various illnesses. Many other herbal drugs are folk remedies from other cultures. Historians of medicine note that every culture has its own tradition of folk medicine treatments or cures widely believed to be effective, based on information gathered from trial and error on the curative properties of plants and passed down through generations. 

An interesting approach toward the total synthesis of the Stemona alkaloid, (-)-stenine (25), which have been used in Chinese and Japanese folk medicine as insecticides, as drugs for the treatment of respiratory diseases, via spirolactone... 

The alkaloids hirsutine (1) and its 3or-epimer dihydrocorynantheine (2a) belong to the corynanthe group of indole alkaloids. They have been isolated from the plant Uncaria rhynchophylla MIQ, which was used for the preparation of the old Chinese folk medicine kampo . Nowadays, 1 and related compounds attract great attention in medicine because of their growth inhibition of the influenza A subtype H3N2 virus. With an EC50 value of 0.40-0.57 ig/mL 1 has shown itself to be 10-20 times more active than the clinically used drug ribavirine (3).1,2 Furthermore, 1 is known for its antihypertensive and antiarrhythmic activity.3... 

It seems that Chinese alchemy is the oldest of the Eastern branches, and may even predate Western alchemy. (The Chinese word for elixir, chin-je, may be the root of the Arabic imic i.)The Yellow Emperor EhiangTi (2704-2595 BCE) is the legendary first alchemist in China, who learnt the art from three immortal women, who also generously saw fit to instruct him in the arts of love. Chinese alchemy inherited a number of facets from folk belief, such as the idea of a plant that, when eaten, will grant immortality, together with the mystic quest for spiritual illumination. 

The hexahydropyrrolo[2,l-a]isoquinoline alkaloid crispine A was isolated in 2002 from Carduus crispus ]15]. Extracts of this plant have been applied in Chinese folk medicine for the treatment of colds, stomach ache, and rheumatism moreover they inhibit the growth of several human cancer cell lines. The useful biological activities induced a strong interest over the last few years in the synthesis of this alkaloid [7,16]. 

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