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Current Research in Chemistry

Year: 2011 | Volume: 3 | Issue: 1 | Page No.: 1-15
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Review Article

Chemical Constituents and Biological Importance of Swertia: A Review

Jagmohan S. Negi, Pramod Singh and Bipin Rawat

ABSTRACT

Swertia, commonly known as ‘Chirata’ in indigenous systems of medicine, are used for treatment of a variety of ailments. Literature survey revealed that much phytochemical analysis has been done on genus Swertia by several groups. In this study, we had planned to document the active chemical constituents of valuable medicinal plants of genus Swertia. The major bioactives of Swertia are xanthones, however, other secondary metabolites such as flavonoids, iridoid glycosides and triterpenoids are also active constituents of this genus. These secondary metabolites played significant role in biological activities such as hepatoprotective, antihepatotoxic, antimicrobial, anti-inflammatory, anticarcinogenic, antileprosy, hypoglycemic, antimalarial, antioxidant, anticholinergic, CNS depressant and mutagenicity.
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Received: October 22, 2010;   Accepted: February 19, 2011;   Published: April 22, 2011

INTRODUCTION

Swertia (family Gentianaceae) is a large genus of herbs distributed in the mountainous regions of tropical area at an altitude of 1200-3600 m. The herbal drug “chiretta” obtained from the dried plants of swertia species. The whole plants of Swertia are medicinal but roots are the most powerful parts (Anonymous, 1976). These are useful as a tonic without aroma or astringency. In Indian medical system chiretta is used as remedy for bronchial asthma, liver disorders, chronic fever, anemia, stomachic and diarrhoea. Chiretta is also used in dying cotton cloth and in liquor industry as bitter ingredients. In Ayurveda, S. chirayita is used as antipyretic, anthelminitic, antiperiodic, laxative and in asthma and leucorrhoea. In Yunani system the plant is used as astringent, tonic, stomachic, lessens inflammation, sedative to pregnant uterus and chronic fevers (Kirtikar and Basu, 1984).

S. chirayita has an established domestic (India) and international market which is increasing at a rate of 10% annually. In spite of the increasing demand by herbal industry the plant is still collected from wild. It is sparsely cultivated and negligible efforts have gone into developing proper agro-techniques of plant. It is harvested for the drug industry (Bentley and Trimen, 1880). S. chirayita is also used in British and American pharmacopoeias as tincture and infusions (Joshi and Dhawan, 2005). S. angustifolia resembles to S. chirayita very closely but differs from it in having thinner root, small wings and ridges on the stem. The dried plants of S. angustifolia and S. paniculata are used as substitute for S. chirayita. About 22,000 kg of the drug are said to be collected and sold annually in Himanchal Pradesh while the annual demand for chiretta in India is reported to be 37,300 kg. Plants belonging to these families are found in all parts of world. They have been widely used in folk medicine. Simple polyoxygenated xanthones have been isolated from most of them. Xanthone derivatives, flavonoids, iridoid glycosides, triterpenoids and dimeric xanthones have been isolated from the genus Swertia (Tan et al., 1991; Zhou et al., 1989). The genus Swertia exhibit variety of biological activity such as hepatoprotective, antihepatotoxic, antimicrobial, anti-inflammatory, anticarcinogenic, antileprosy, hypoglycemic, antimalarial, antioxidant, anticholinergic, CNS depressant and mutagenicity. The pharmacological properties of Swertia have raised great interest. The purpose of this review to collect all the possible information regarding the chemical constituents and biological effects of the genus Swertia, thus will help to the researchers and scientists to take action for future study in this discipline.

CHEMICAL CONSTITUENTS

Xanthones are main secondary metabolites of Swertia species. Structures of xanthones are related to that of flavonoids and their chromatographic behaviors are also similar. Although flavonoids are frequently encountered in nature, xanthones have been found in limited number of families. They always occur in Gentianaceae and Guttiferae. Xanthones are sometimes found as the parent polyhydroxylated compounds but most xanthones are mono or poly methyl ethers or are found as glycosides (Hostettmann and Miura, 1977). Unlike iridoids, xanthones are apparently not present in all plant species investigated in the family Gentianaceae. This is documented by the systematic study of Hostettmann-Kaldas et al. (1981). The natural xanthones have been isolated mainly from about 150 plants associated with four families; Guttiferae, Gentianaceae, Moraceae and Polygalaceae. According to Vieira and Kijjoa (2005), 278 natural xanthones were reported from total of 515 xanthones. In this period, the xanthones from higher plants appear to be associated mainly with the families Clusiaceae (55 species in 12 genera) and Gentianaceae (28 species in 8 genera). Isolated compounds and biological activities of Swertia species are listed in Table 1. Xanthones isolated from nature are classified into six main groups; simple xanthones, xanthone glycosides, prenylated xanthones, xanthonolignoids, bis-xanthones and miscellaneous xanthones. These are further subdivided according to the degree of oxygenation into non-, mon-o, di-, tri-, tetra-, penta- and hexa-oxygenated substances (Mandal et al., 1992b; Sultanbawa, 1980; Demirkiran, 2007).

Xanthones and their glycosides (Fig. 1) have been isolated from Swertia species. Mangiferin is the most common C-glycosides in S. chirayita, S. mussotii, S. cordata, S. macrosperma and S. connata. Xanthone O-glycosides (swertianolin) from S. japonica and S. ciliata (Plouvier et al., 1967) have been reported. The first xanthone O-glycoside, norswertianin-1-O-glucosyl-3-O-glucoside has been isolated from S. perennis (Hostettmann and Wagner, 1977). The isolated chemical constituents, ethno-pharmacology as well as the biological activities and pharmacological applications of Swertia species, covering the literature up to 2003 are compiled by Brahmachari et al. (2004). Xanthones in Swertia chirata, S. speciosa and S. paniculata were determined by HPLC (Negi et al., 2009a, 2010a, b). Mineral elements, based on their concentration can play different roles in human health and plant life. Nine elements (Zn, Cu, Mn, Fe, Co Na, K, Ca and Li) in S. chirayita and S. speciosa have been analyzed by atomic absorption spectrometry (Negi et al., 2009b, 2010c). Kaempferol, catechin, epicatechin and Polyphenol Contents were also isolated and identified from Swietenia macrophylla, Rhus coriaria and Rhus typhina (Falah et al., 2008; Kossah et al., 2010). Extracts of G. senegalensis are rich in flavonoid content and showed anti-inflammatory activity (Sombie et al., 2011). Leaf and stem of Swertia chirata showed significant antimicrobial activities against some Gram-positive and Gram-negative bacteria (Alam et al., 2009).

Table 1: Isolated compounds and activity of different parts of Swertia species
Image for - Chemical Constituents and Biological Importance of Swertia: A Review
Image for - Chemical Constituents and Biological Importance of Swertia: A Review
Image for - Chemical Constituents and Biological Importance of Swertia: A Review
Image for - Chemical Constituents and Biological Importance of Swertia: A Review
Image for - Chemical Constituents and Biological Importance of Swertia: A Review

Several isolated chemical constituents viz, coumarins, flavonoids, phytosterol, phenols, tenins, alkaloids, triterpenes, anthraquinons and biological activities of Toona species were documented by Negi et al. (2011).

Image for - Chemical Constituents and Biological Importance of Swertia: A Review
Fig. 1: Structures of some isolated xanthones from Swertia

BIOLOGICAL PROPERTIES

Plants belonging to the family Gentianaceae, are best known for their bitter taste and used in traditional remedies against loss of appetite, fever and are still included in many “tonic” formulations (Gaur, 1999). Some specific activities have been reported for xanthones and iridoids from Gentianaceae. Iridoids such as swertiamarin have anticholinergic propertiy (Bhattacharya et al., 1974). For sweroside and gentiopicroside hepatoprotective activities have been reported (Kondo et al., 1994) and both compounds are being used as antihepatitis drugs. Xanthones (especially mangiferin) are reported to give CNS stimulation (Bhattacharya et al., 1972). They should also have anti-inflammatory activity (Mandal et al., 1992a). For bellidifolin and swerchirin a strong hypoglycemic activity has been reported by Saxena et al. (1993) and Basnet et al. (1994). S. paniculata is used in the Indian System of Medicine as a bitter tonic and in the treatment of some mental disorders (Prakash et al., 1982). S. hookeri extract is used in the treatment of microbial infections and as a mood elevator (Ghosal et al., 1980). Swertifrancheside isolated from S. franchetiana was found to be potent inhibitor of the DNA polymerase activity of human immunodeficiency virus-1 reverse transcriptase (HIV-1RT). Naturally occurring xanthones have emerged out as an important class of organic compounds in view of their remarkable pharmacological and other biological activities. It has now been observed that a number of plant products which are in regular use as chemotherapeutic agents contain xanthones as active constituents. Mangiferin was the first xanthone to be investigated pharmacologically and has been found to exhibit a broad spectrum of biological activities. It shows monoamine oxidase inhibition, cardiotonic, convulsant and choleretic activities (Ghosal et al., 1973; Bhattacharya et al., 1972). Pronounced anti-inflammatory activity has also been observed in mangiferin. Oral and topical compounds containing mangiferin are useful for the treatment of diseases caused by herpes virus. Mangiferin has been found to protect the liver of the rats from high altitude hypoxia. On the other hand Ghosal et al. (1975) have observed the opposite CNS depressant effect for xanthone-O-glycosides in mice and rats. The extract of most of Swertia species showed mutagenic activities. The antimalarial drug AYUSH-64 contains S. chirayita as one of the ingredients. Xanthones of S. chirayita are reported to produce CNS depression (Ghosal et al., 1973). The total extract of S. chirayita showed significant antifeedant activity against Jute semilooper (Malic et al., 1985). Norswertianolin, an O-glycoside has been reported to produce antitubercular activity. The O-glycosides of S. purpurescens are known to produce CNS depression in albino rate and mice (Ghosal et al., 1974). 1,8-Dihydroxy-3,5-dimethoxyxanthone (swerchirin), isolated from the hexane fraction of Swertia chirayita, has a very significant blood sugar lowering effect in fasted, fed, glucose loaded and tolbutamide pre-treated albino rats.

CONCLUSION

As a conclusion, the present study has shown that mainly xanthones from genus Swertia are responsible for several types of biological activities. Apart from these flavonoids, iridoid glycosides and triterpenoids are also secondary metabolites isolated from this genus which also contribute their role in biological activities.

ACKNOWLEDGMENT

The authors are thankful to Dr. Asha Budakoti, NCL, Pune for providing some references.

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Vinod Visht Reply

The MS is very well written in informative way

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