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Potential in vitro anti-allergic, anti-inflammatory and cytotoxic activities of ethanolic extract of Baliospermum montanum root, its major components and a validated HPLC method.

ABSTRACT:

Background

The root of Baliospermum montanum has been used as an ingredient of traditional Thai medicines for the treatments of several diseases including itching eczema, muscle and joint inflammation, and cancer. Few studies have been done on phytochemical components of this root. In this study, we isolated major compounds of the crude ethanolic extract of B. montanum root and developed and validated a high performance liquid chromatographic (HPLC) method for the determination of its major components. We then investigated anti-allergic, anti-inflammatory and cytotoxic activities of the extract.

Methods

The aims of this study were to investigate in vitro activities including inhibitory effect of ?-hexosaminidase released from RBL-2H3 cells, inhibition of nitric oxide (NO) production from RAW 264.7 cells and cytotoxic activity against cancerous liver cell lines (HepG2 and KKU M156) by using sulforhodamine B (SRB) assay. Isolation of major components was conducted by using column chromatographic method. Isolated major compounds were analyzed by using high performance liquid chromatography (HPLC).

Results

The crude extract exhibited the highest cytotoxic activity, with IC₅₀ less than 1??g/mL, while its anti-allergy and anti-inflammation were also potent with IC₅₀ less than 6??g/mL. Three propiophenones isolated from B. montanum root exhibited moderate cytotoxic activities (IC₅₀?>?20??g/mL). Two of the propiophenones found were major components that can be detected by HPLC. The developed and validated HPLC method showed good accuracy, precision, and linearity.

Conclusion

The results of this study suggested that ethanolic extract of of B.montanum root can be a potential source of anti-allergy, anti-inflammation, and anti-cancer compounds. The isolated compounds can serve as markers when B. montanum is used in herbal remedies but not as overall responsive markers. The HPLC method developed may be useful for quality control in the production of the extract and for further formulation developments. However, investigation of several associated biological activities is necessary before the development can proceed further. Minor active compounds should be isolated and a more sensitive analytical method should be developed to detail the key responsive components of the ethanolic extract of B. montanum root.

SUBMITTER: Pipatrattanaseree W

PROVIDER: S-EPMC6373163 | biostudies-literature | 2019 Feb

REPOSITORIES: biostudies-literature

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Potential in vitro anti-allergic, anti-inflammatory and cytotoxic activities of ethanolic extract of Baliospermum montanum root, its major components and a validated HPLC method.

Pipatrattanaseree Weerachai W Itharat Arunporn A Mukkasombut Nichamon N Saesiw Ubonwan U

BMC complementary and alternative medicine 20190212 1

<h4>Background</h4>The root of Baliospermum montanum has been used as an ingredient of traditional Thai medicines for the treatments of several diseases including itching eczema, muscle and joint inflammation, and cancer. Few studies have been done on phytochemical components of this root. In this study, we isolated major compounds of the crude ethanolic extract of B. montanum root and developed and validated a high performance liquid chromatographic (HPLC) method for the determination of its ma ...[more]

PMID: 30755219

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Project description:Background: Hypercholesterolemia, high cholesterol levels in the blood, can contribute to many forms of disease, most notably cardiovascular disease. Anti-hypercholesterolemic agents generally used for those conditions have several side effects for patients. Zingiber montanum, known locally as "bangle", belongs to the family Zingiberaceae and is a potential plants for alternative anti-hypercholesterolemic agents. This plant, from East Kalimantan, is used in traditional medicine for health problems caused by high cholesterol levels. The aim of this research was to find alternatives to anti-hypercholesterolemic agents, especially from natural sources. Methods: This study was an experimental study using 30 Wistar male white rats. Subjects were randomly divided into 6 groups (n=5): (1) normal control group; (2) high fat diet control group; (3) high fat diet with simvastatin; (4-6) high fat diet with Zingiber montanum extracts 100, 200, and 400 mg/kg. After 4 weeks of treatment, blood was collected from all groups, and plasma concentrations of triglycerides, total cholesterol, high density lipoproteins (HDL), and low density lipoproteins (LDL) were measured. Results: The results showed significant differences in total cholesterol (p=0.000), LDL (p=0.000) and triglycerides (p=0.001) in the high-fat diet group with Z. montanum extract, as compared to the high-fat diet control. Meanwhile, there were no significant differences in HDL levels (p=0.830) between the high-fat diet group and other groups. The results also showed significant differences in total cholesterol and LDLs for rats treated with Z. montanum extract, 100 mg/kg (p=0.000), 200 mg/kg (p=0.000), and 400 mg/kg (p=0.000) compared to the high-fat diet group. The result of Z. montanum 400 mg/kg also showed a significant reduction, not only for total cholesterol and LDLs, but also for triglycerides (p=0.030). Conclusion: It could be concluded that Z. montanum extracts have the potency to be further developed as a new natural source of the anti-hypercholesterolemic agents.

Project description:Ethnopharmacological relevanceCaesalpinia sappan is a common remedy in Traditional Chinese Medicine and possesses diverse biological activities including anti-inflammatory properties. Osteoarthritis (OA) is a degenerative joint disease with an inflammatory component that drives the degradation of cartilage extracellular matrix. In order to provide a scientific basis for the applicability of Caesalpinia sappan in arthritic diseases, the present study aimed to assess the effects of an ethanolic Caesalpinia sappan extract (CSE) on human chondrocytes and macrophages.Materials and methodsPrimary human chondrocytes were isolated from cartilage specimens of OA patients. Primary cells, SW1353 chondrocytes and THP-1 macrophages were serum-starved and pretreated with different concentrations of CSE prior to stimulation with 10 ng/ml of interleukin-1beta (IL-1?) or lipopolysaccharide (LPS). Following viability tests, nitric oxide (NO) and tumor necrosis factor-alpha (TNF-?) were evaluated by Griess assay and ELISA, respectively. Using validated real-time PCR assays, mRNA levels of IL-1?, TNF-?, inducible nitric oxide synthase (iNOS), and cyclooxygenase-2 (COX-2) were quantified. SW1353 cells were cotransfected with a COX-2 luciferase reporter plasmid and nuclear factor-kappa-B (NF-?B) p50 and p65 expression vectors in the presence or absence of CSE.ResultsCSE dose-dependently inhibited the expression of pro-inflammatory cytokines IL-1? and TNF-? in IL-1?-stimulated chondrocytes and LPS-stimulated THP-1 macrophages. CSE further suppressed the synthesis of NO in primary OA chondrocytes by blocking iNOS mRNA expression. The inhibition of COX-2 transcription was found to be related with the CSE inhibition of the p65/p50-driven transactivation of the COX-2 promoter.ConclusionsThe present report is first to demonstrate the anti-inflammatory activity of CSE in an in vitro cell model of joint inflammation. CSE can effectively abrogate the IL-1?-induced over-expression of inflammatory mediators at the transcriptional level in human chondrocytes and macrophages, most likely by inhibiting NF-?B (p65/p50) signaling. Blockade of IL-1?-induced NF-?B signaling and its downstream pro-inflammatory targets by CSE may be beneficial for reducing cartilage breakdown in arthritis.

Dataset Information

Potential in vitro anti-allergic, anti-inflammatory and cytotoxic activities of ethanolic extract of Baliospermum montanum root, its major components and a validated HPLC method.

Background

Methods

Results

Conclusion

Publications

Potential in vitro anti-allergic, anti-inflammatory and cytotoxic activities of ethanolic extract of Baliospermum montanum root, its major components and a validated HPLC method.

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