Drug Development
The therapeutic value of grape seed proanthocyanidins for vascular diseases has been recognized by the world in the early 1980s. In France, patented products made from grape seed proanthocyanidins are used to treat microcirculatory diseases, including ocular and peripheral capillary permeability diseases and venous and lymphatic insufficiency. Bonnaure et al. in France invented a preparation for treating periodontal disease using proanthocyanidin oligomers or monomers as active ingredients (≥1%) and obtained patent protection. The French company Sanofi uses grape seed proanthocyanidins and soy lecithin to make a complex, which is used as a vascular protective agent and anti-inflammatory agent. Each tablet contains 250 mg of the complex. Vennat and others from France have also made high-dose tablets (50mg tablets) containing 80% proanthocyanidins, and improved the prescription so that the tablets can be released quickly and completely, and are still very stable under different conditions after being stored for 10 months. sex. In addition, Berkhman et al. in Germany developed a proanthocyanidin preparation for the treatment of alcoholism and obtained patent protection. In Romania, a proanthocyanidin preparation named Endotelon has been marketed for the treatment of capillary diseases.
Cosmetic development
In 1990, Masquelie in France specialized in therapeutic effects such as anti-inflammatory, anti-radiation and other activities that were not included in the indications of proanthocyanidin preparations on the market, especially in dermatology. Applications were studied. The therapeutic effect of proanthocyanidins is closely related to its ability to scavenge free radicals, and the degradation process of lipids, proteins and nucleic acids caused by environmental stimulation of the skin, mucous membranes and hair is inseparable from free radicals. The special antioxidant activity and free radical scavenging ability of proanthocyanidins have opened up broad prospects for their application in the field of cosmetics. France has developed night cream, hair lotion and mouthwash made of liposome microcapsules made of Markush structure proanthocyanidin oligomers. In order to make it easier for active ingredients to pass through the stratum corneum of the skin, the Italian company Indena spent 5 years successfully developing functional cosmetics using phospholipids (natural phospholipids or synthetic phospholipids) as carriers, with the trade name Phytosome. This product contains 5% Ginkgo proanthocyanidin dimer, which is used to reduce skin inflammation and improve microcirculation. Tested on 18 healthy subjects (who had skin inflammation and erythema due to UV exposure). It shows that the cosmetics have better protection against ultraviolet damage. In 1990, Japan's Yamaskosh developed an oily cosmetic containing 1% proanthocyanidin oligomers that can brighten the skin. Japan's Ariga and others have also developed proanthocyanidins used as antioxidants in medicines, foods and cosmetics, and have obtained patent protection.
After more than 30 years of research and development, proanthocyanidins have been recognized for their superior antioxidant activity. They have made significant progress in improving microcirculation and treating ophthalmic diseases, and have been used in the fields of drugs and cosmetics. It is widely used; it is rich in resources, has precise curative effect and has minimal side effects. Not only has it become popular in Europe and Japan, but it has also become popular in the United States in recent years. It indicates the broad development prospects of proanthocyanidins in medical applications.
my country’s development of proanthocyanidins did not start late. Since 1986, it has joined the ranks of the world in developing proanthocyanidins. In that year, the Nanjing Forest Products Research Institute of the Chinese Academy of Forestry and the University of Nottingham in the United Kingdom jointly developed proanthocyanidins from the bark of Larix gmelini, and separated dimers B1 to B4 and others with an average degree of polymerization of 6 to 7 and an average molecular weight of 1700 to 2000D polymer. In 1987, the Department of Chemistry of Nanjing Forestry University isolated mixed proanthocyanidins and proanthocyanidins from the bark of Myrica esculenta and Phyllanthus emblica, and conducted structural identification. In the same year, the department also isolated proanthocyanidins from Dioscorea cirrhosa and the red roots of roses. Two kinds of proanthocyanidins are found in the skin. Taijin College of Pharmacy in Taiwan and Kyushu University in Japan jointly isolated 3 proanthocyanidin glucosides from the fern Davallia divaricata, 2 dimers (B1, B2), and a triad. polymer and a tetramer, and their structures were identified. In 1994, Nanjing Forestry University isolated and identified procyanidin polymer glucoside from the aqueous extract of Ternstroemia gymnathera. This was the first proanthocyanidin glucoside discovered in China.
No matter what, the development of proanthocyanidins in my country is mostly in the phytochemical research stage. Although different parts of pine trees (such as pine knots, pine needles, pine cones and pollen) are used as medicine, the active ingredients have not been isolated and identified, and it is difficult to clearly explain the efficacy and effectiveness. relationship with proanthocyanidins. Although proanthocyanidins are widely present in the plant kingdom, and my country is also rich in hawthorn, ginkgo and grape resources, no real proanthocyanidin products are currently available.