Introduction. Benchalokawichian (BCW), a Thai traditional herbal formulation, has long been used as antipyretic and to treat skin disorders. It comprises roots from five herbs: Ficus racemosa, Capparis micracantha, Clerodendrum petasites, Harrisonia perforata, and Tiliacora triandra. This polyherbal remedy has recently been included in the Thailand National List of Essential Medicines (Herbal Products list). Methodology. A Bioassay-guided fractionation technique was used to evaluate antiallergy activities of crude extracts, and those obtained by the multistep column chromatography isolation of pure compounds. Inhibitory effect on the release of β-hexosaminidase from RBL-2H3 cells was used to determine antiallergic activity. Results. Two pure compounds from BCW formulation showed higher antiallergic activity than crude or semipure extracts. Pectolinarigenin showed the highest antiallergic activity, followed by O-methylalloptaeroxylin, with IC50 values of 6.3 μg/mL and 14.16 μg/mL, respectively. Moreover, the highest activities of pure compounds were significantly higher than chlorpheniramine (16.2 μg/mL). Conclusions. This study provides some support for the use of BCW in reducing itching and treatment of other skin allergic disorders. The two isolated constituents exhibited high antiallergic activity and it is necessary to determine their mechanism of action. Further phytochemical and safety studies of pure compounds are required before development of these as antiallergy commercial remedies.
A Thai traditional remedy called Benchalokawichian (BLW) consists of 5 plant species, Ficus racemosa, Capparis micracantha, Clerodendrum petasites, Harrisonia perforata, and Tiliacora triandra. It has long been used in Thai traditional medicine to reduce fever in respiratory tract infection, but there is no report on either cytotoxicity against cancer cell lines of the respiratory tract system or anti-inflammatory effect. Thus, the objectives of this research were to investigate the cytotoxic activity of the ethanolic and water extracts of BLW, its single plant ingredients and its isolated compounds against 5 cancer cell lines of the respiratory tract, by SRB assay. Anti-inflammatory activity of all extracts and compounds was also tested by using lipopolysaccharide-induced nitric oxide (NO) in RAW 264.7 cells. The main compounds were isolated by high-performance liquid chromatography and compared with BLW and plant ingredients. A major compound of BLW and H. perforata ethanolic extracts is perforatic acid, which inhibited the growth of 2 lung cancer cell lines, A549 and H226, with IC 50 values of 6.7 and 13.2 µg/mL. The ethanolic extract of BLW and T. triandra showed cytotoxic activity against all cancer cell lines with IC 50 values in the range of 10.1 to 45.2 µg/mL. In contrast, all EtOH extracts showed moderate anti-inflammatory activity, but the water extract had no inhibitory effect on either activity. Pectolinarigenin and O-methyllaloptaeroxyrin, 2 minor compounds, exhibited NO inhibitory effect with IC 50 values of 7.1 and 7.9 µg/mL, respectively, whereas perforatic acid was inactive (>50 µg/mL). Moreover, pectolinarigenin showed high cytotoxic activity against all cancer cell lines of the respiratory system with IC 50 values in the range of 1.9 to 9.1 µg/mL. As a result, these 2 minor compounds can be used as markers for quality control of BLW for anti-inflammatory activity. Perforatic acid and pectolinarigenin are of interest for further study on their cytotoxic mechanism. Remarkably, T. triandra, one of the plant components of BLW, is possibly the source of the active cytotoxic compounds.
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