Polysaccharide enhances Radix Saposhnikoviae efficacy through inhibiting chromones decomposition in intestinal tract

Abstract

Vegetative but not reproductive stage of Saposhnikovia divaricate (Turxz.) schischk possesses pharmacological activities. However, our recent study showed that reproductive S. divaricate supplemented with polysaccharide showed evidently elevated pharmacological activities and increased cimifugin content in rat serum. The aims of present study were to assess the influence of polysaccharides on the chromones pharmacological activities in Radix Saposhnikoviae (RS), the dried root of vegetative stage of S. divaricate, and to explore the underlying mechanisms. Only cimifugin was detected in the plasma of chromone treated animals and RS polysaccharide significantly increased the plasma content of cimifugin. It was shown that neither cimifugin absorption nor glycoside components transformation in simulated digestive fluid was affected by RS polysaccharide. However, a significant promotion of transformation of cimifugin to more stable prime-O-glucosylcimifugin (PGCN) by RS polysaccharide, and a protective effect of polysaccharide on chromone components were observed in small intestine solutions. Meanwhile, RS polysaccharide produced a significant elevation of cimifugin and PGCN concentration in vivo. Based on these findings, we concluded that RS polysaccharide could greatly increase the content of cimifugin, which might be related to its degradation-proof effect on cimifugin, via transforming cimifugin to comparatively more stable PGCN and spatial structure protection.Radix Saposhnikoviae (RS) is the dried root of vegetative stage of perennial herb Saposhnikovia divaricate (Turxz.) schischk in family Umbelliferae, and is commonly used for treating febrility, rheumatism, headache, vertigo, generalized aching, convulsion, arthralgia and inflammatory symptoms for thousands of years in China, Japan, and Korea 1-5 . Modern scientific experiments have also confirmed the beneficial effects of RS using its extracts 1,5-7 . RS contains various bioactive substances, such as chromones, coumarins, polyacetylenes, and polysaccharides. Among them, chromones and coumarins are the main components of RS 4,8,9 . Furthermore, chromones have also been identified as the main bioactive constituents with most-evident pharmacological activities as they possess potent analgesic, antifebric, anti-inflammatory and immune-regulatory effects 1,5 .Currently, three major types of chromones were found in RS, including prime-O-glucosylcimifugin (PGCN), 4′ -O-β -D-glucosyl-5-O-methylvisamminol (GML), and cimifugin (Fig. 1). In Chinese pharmacopoeia, PGCN and GML are designated as marker compounds for RS quality control due to their relatively high content and GML is also used for the identification of RS in Japanese Pharmacopoeia 3,4,10,11 . Cimifugin is aglycone of PGCN and has much lower content than that of PGCN and GML. Huge amount of cimifugin and trace amount of PGCN and GML were detected in the plasma sample of overdose chromone 4,12 . Generally, cimifugin is regarded as the pharmacologically active form of inactive chromone derivatives such as P...

Medicinal Plants to Strengthen Immunity during a Pandemic

“…In the Russian Federation, Saposhnikovia divaricata grows in Eastern Siberia and the Far East. The anti-inflammatory, analgesic, antipyretic, anti-allergic, antioxidant, antitumor and antiviral activity of its root extracts has been established [ 75 , 76 , 77 , 78 ]. Chromones, coumarins, unsaturated fatty acids, volatile oils and polyacetylene compounds were isolated from the chemical composition [ 74 , 79 , 80 ].…”

“…Chromones, coumarins, unsaturated fatty acids, volatile oils and polyacetylene compounds were isolated from the chemical composition [ 74 , 79 , 80 ]. Polysaccharides of the dried root of Saposhnikovia divaricata possess immunoregulatory and antitumor characteristics [ 77 ].…”