Studies On The Bioactive Constituents Of The Fruits Of Lycium Barbarum Originated In Ningxia And The Application And Development Of The Fruits

Lycium barbarum (Solanaceae) is distributed in Central China, South China, EastChina, northwest and southwest of China, and in all these districts it was also cultivated.The fruits of L. barbarum are used as traditional Chinese medicinal, which have showedsignificant effects of strengthening the immune system, antioxidant and free radicalscavenging, and have mainly been used to adjuvant therapy against tumor and someage-related diseases including atherosclerosis, diabetes and so on. However, few studieshave been reported on the application and development of the bioactive components inthis plant as drugs in clinic, and the research on monomer compositions of this plant havenot carried out thotoughly.There are two parts in the studies.1. Application and development of the bioactive components in the fruits ofLycium barbarum1.1Research and development of total Lycium barbarum polysaccharides ashospital preparationAccording to the literature, Lycium barbarum polysaccharides (LBP) showed significant effect on prevention and treatment of diabetes. This research adopted optimizedwater extraction and alcohol precipitation to purify polysaccharides, and yielded total LBPwith high purity. Then the preparation technology, pharmacology effect, quality standards,stability and acute toxicity of the preparation of total LBP were studied, along with thedesign of the clinical trial. These preparation has been applied for and obtained the clinicalresearch approval documents of military medical organization.1.2Studies on the extraction and purification technology of total flavonoids inthe fruits of Lycium barbarumUp to date, the methods to extract and purify the total flavonoids from the fruits of L.barbarum were mainly by macroporous resin chromatography alone or polyamidechromatography alone. But the purity of total flavonoids was not high enough throughthese methods, and the efficiencies of the purification steps were low. Based on thereported studies, our research group adopted macroporous resin combination withpolyamide chromatogrphies to extract and purify the total flavonoids from the fruits of L.barbarum. The influencing factors were investigated to obtain the optimized technologycondition. The result indicated that the purity of the total flavonoids reached42.8%by thetechnology. And a national patent has been applied according to the method.2. Studies on the bioactive constituents of the fruits of Lycium barbarumThe constituents of the fruits of L. barbarum were studied by Sephadex LH-20, silicagel chromatographies and HPLC preparation to obtain21compounds. Fifteen of thecompounds have been identified by extensive spectral analysis. They are seven phenolicacid amide compounds, i.e. N-E-coumaroyl tyramine (1), dihydro-N-caffeoyltyramine (2),trans-N-caffeoyltyramine (3), N-E-feruloyl tyramine (4), lyciumamide A (5), lyciumamideB (6) and lyciumamide C (7), one flavonoid compound, i.e. quercetin (15), two phenolicacid compounds, i.e. Z-p-hydroxy-cinnamic acid (11) and E-p-hydroxy-cinnamic acid (12),two coumarin compounds, i.e. scopoletin (13) and isoscopoletin (14), one vitamincompound, i.e. nicotinamide (10), one benzylidene acetophenone derivative, i.e.artamenone (8), and one alkaloid compound, i.e.2-furylcarbinol-(5’-11)-1,3-cyclopentadi- ene [5,4-c]-1H-cinnoline (9). Compounds5–7are new compounds, while compounds1,4,8and9were obtained from genus Lycium for the first time.Compounds1and4–7were evaluated for their antioxidant activities in scavengingDPPH free radical and inhibiting lipid peroxidation in rat liver microsomes induced byascorbate/Fe2+, cumine hydroperoxide (CHP) or CCl4/reduced form of nicotinamide-adenine dinucleotide phosphate (NADPH), and the results showed that all of themexhibited strong activities while compounds1and4were more potent.Innovations and significance:1. The total LBP as the effective parts of Lycium barbarum was purified anddeveloped. On the foundation of the studies, the Lycium barbarum polysaccharide capsulehas been developed as hospital preparation. The research and development showed greatsignificance in developing traditional Chinese medicine.2. The method of macroporous resin combination with polyamide chromatogrphieswere used to extract and purify the total flavonoids from the fruits of L. barbarum. Themethod possess more advantages than the macroporous resin chromatography alone orpolyamide chromatography alone. The purity of the total flavonoids was improved greatlyby the advantages of macroporous resin combination with polyamide chromatographies.3. Twenty-three compounds were isolated and fifteen of them115have beenidentified from the fruits of L. barbarum. Compounds17belong to amide compounds,and compounds5–7are new compounds. Compounds1,4,8and9were obtained fromgenus Lycium for the first time. Compounds5–7are phenolic acid amide dimers and theirderivative, and their structures show certain novelty. There have been a certain amount ofphenolic acid amides reported in genus Lycium, but mostly isolated from the undergroundparts of these plants. This kind of dimer has never been reported from the genus. Theseresults showed significance for the chemotaxonomy of these Lycium species.4. Compounds1and4–7were evaluated for their antioxidant activities, and theresults showed that all of them exhibited strong activity. These phenolic acid amidespossessed the similar antioxidant capacities in comparison with other antioxidants such as polysaccharides, flavonoides and carotenoid. This suggested that phenolic acid amidesmight play an important role of antioxidant activity similar to these antioxidants in thefruits of L. barbarum.