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Isolation of antiosteoporotic compounds from seeds of Sophora japonica.

Abdallah HM, Al-Abd AM, Asaad GF, Abdel-Naim AB, El-halawany AM - PLoS ONE (2014)

Bottom Line: Compounds 1, 2 and 5 showed significant estrogenic proliferative effect in MCF-7 cell in sub-cytotoxic concentration range.SPH (15 mg/kg) did not significantly increase the serum level of osteocalcin (OC) compared to OVX group.The drug showed thicker bony trabeculae, more osteoid, and more osteoblastic rimming compared to OVX group.

View Article: PubMed Central - PubMed

Affiliation: Department of Natural Products, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia; Department of Pharmacognosy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.

ABSTRACT
Chemical investigation of Sophora japonica seeds resulted in the isolation of seven metabolites identified as: genistin (1), sophoricoside (2), sophorabioside (3), sophoraflavonoloside (4), genistein 7,4'-di-O-β-D-glucopyransoide (5), kaempferol 3-O-α-L-rhamnopyranosyl(1 → 6)β-D-glucopyranosyl(1 → 2)β-D-glucopyranoside (6) and rutin (7). Compounds 1, 2 and 5 showed significant estrogenic proliferative effect in MCF-7 cell in sub-cytotoxic concentration range. Compounds 1 and 2 showed minimal cell membrane damaging effect using LDH leakage assay. Accordingly, compound 2 (sophoricoside, (SPH)) was selected for further in-vivo studies as a potential anti-osteoporosis agent. The anti-osteoporotic effect of SPH was assessed in ovarectomized (OVX) rats after oral administration (15 mg/kg and 30 mg/kg) for 45 days compared to estradiol (10 µg/kg) as a positive control. Only in a dose of 30 mg/kg, SPH regained the original mechanical bone hardness compared to normal non-osteoporotic group. However, SPH (15 mg/kg) significantly increased the level of alkaline phosphatase (ALP) to normal level. Treatment with SPH (30 mg/kg) increased the level of ALP to be higher than normal group. SPH (15 mg/kg) did not significantly increase the serum level of osteocalcin (OC) compared to OVX group. On the other hand, treatment with SPH (30 mg/kg) significantly increased the level of OC to 78% higher than normal non-ovarectomized animals group. In addition, SPH (15 mg/kg) decreased the bone resorption marker, acid phosphatase (ACP) to normal level and SPH (30 mg/kg) further diminished the level of serum ACP. Histopathologically, sophoricoside ameliorated the ovarectomy induced osteoporosis in a dose dependent manner. The drug showed thicker bony trabeculae, more osteoid, and more osteoblastic rimming compared to OVX group.

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Mechanical and biochemical assessment for anti-osteoporosis effect of sophoricoside in-vivo.Ovariectomized rats were treated with SPH (15 mg/kg and 30 mg/kg) for 6 weeks and compared to E2 treated animals (10 µg/kg) and sham-operation group. Mechanical hardness was evaluated using hardness tester along (A) and perpendicular (B) to femur bone shaft. Biochemical assessment of osteoporosis was evaluated by measuring serum alkaline phosphatase (C) and osteocalcin (D) at the end of treatment period.
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pone-0098559-g003: Mechanical and biochemical assessment for anti-osteoporosis effect of sophoricoside in-vivo.Ovariectomized rats were treated with SPH (15 mg/kg and 30 mg/kg) for 6 weeks and compared to E2 treated animals (10 µg/kg) and sham-operation group. Mechanical hardness was evaluated using hardness tester along (A) and perpendicular (B) to femur bone shaft. Biochemical assessment of osteoporosis was evaluated by measuring serum alkaline phosphatase (C) and osteocalcin (D) at the end of treatment period.

Mentions: Mechanically, the forces required to break the femur bones longitudinally and vertically were significantly decreased in response to ovarectomy to be 34% and 56% of the normal bone hardness, respectively. Treatment with E2 (10 µg/kg) and low dose SPH (15 mg/kg) did not affect the bone hardness in response to longitudinal force; however high dose SPH (30 mg/kg) improved the bone hardness by 43.3% compared to OVX group. In other words, treatment with SPH (30 mg/kg) regained the original longitudinal bone hardness (Figure 3-A). On the other hand, treatment with E2 (10 µg/kg), SPH (15 mg/g) and SPH (30 mg/kg) significantly improved bone hardness to vertical force by 89.3% and 97.4%, respectively compared to OVX group (Figure 3-B).


Isolation of antiosteoporotic compounds from seeds of Sophora japonica.

Abdallah HM, Al-Abd AM, Asaad GF, Abdel-Naim AB, El-halawany AM - PLoS ONE (2014)

Mechanical and biochemical assessment for anti-osteoporosis effect of sophoricoside in-vivo.Ovariectomized rats were treated with SPH (15 mg/kg and 30 mg/kg) for 6 weeks and compared to E2 treated animals (10 µg/kg) and sham-operation group. Mechanical hardness was evaluated using hardness tester along (A) and perpendicular (B) to femur bone shaft. Biochemical assessment of osteoporosis was evaluated by measuring serum alkaline phosphatase (C) and osteocalcin (D) at the end of treatment period.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4043785&req=5

pone-0098559-g003: Mechanical and biochemical assessment for anti-osteoporosis effect of sophoricoside in-vivo.Ovariectomized rats were treated with SPH (15 mg/kg and 30 mg/kg) for 6 weeks and compared to E2 treated animals (10 µg/kg) and sham-operation group. Mechanical hardness was evaluated using hardness tester along (A) and perpendicular (B) to femur bone shaft. Biochemical assessment of osteoporosis was evaluated by measuring serum alkaline phosphatase (C) and osteocalcin (D) at the end of treatment period.
Mentions: Mechanically, the forces required to break the femur bones longitudinally and vertically were significantly decreased in response to ovarectomy to be 34% and 56% of the normal bone hardness, respectively. Treatment with E2 (10 µg/kg) and low dose SPH (15 mg/kg) did not affect the bone hardness in response to longitudinal force; however high dose SPH (30 mg/kg) improved the bone hardness by 43.3% compared to OVX group. In other words, treatment with SPH (30 mg/kg) regained the original longitudinal bone hardness (Figure 3-A). On the other hand, treatment with E2 (10 µg/kg), SPH (15 mg/g) and SPH (30 mg/kg) significantly improved bone hardness to vertical force by 89.3% and 97.4%, respectively compared to OVX group (Figure 3-B).

Bottom Line: Compounds 1, 2 and 5 showed significant estrogenic proliferative effect in MCF-7 cell in sub-cytotoxic concentration range.SPH (15 mg/kg) did not significantly increase the serum level of osteocalcin (OC) compared to OVX group.The drug showed thicker bony trabeculae, more osteoid, and more osteoblastic rimming compared to OVX group.

View Article: PubMed Central - PubMed

Affiliation: Department of Natural Products, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia; Department of Pharmacognosy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.

ABSTRACT
Chemical investigation of Sophora japonica seeds resulted in the isolation of seven metabolites identified as: genistin (1), sophoricoside (2), sophorabioside (3), sophoraflavonoloside (4), genistein 7,4'-di-O-β-D-glucopyransoide (5), kaempferol 3-O-α-L-rhamnopyranosyl(1 → 6)β-D-glucopyranosyl(1 → 2)β-D-glucopyranoside (6) and rutin (7). Compounds 1, 2 and 5 showed significant estrogenic proliferative effect in MCF-7 cell in sub-cytotoxic concentration range. Compounds 1 and 2 showed minimal cell membrane damaging effect using LDH leakage assay. Accordingly, compound 2 (sophoricoside, (SPH)) was selected for further in-vivo studies as a potential anti-osteoporosis agent. The anti-osteoporotic effect of SPH was assessed in ovarectomized (OVX) rats after oral administration (15 mg/kg and 30 mg/kg) for 45 days compared to estradiol (10 µg/kg) as a positive control. Only in a dose of 30 mg/kg, SPH regained the original mechanical bone hardness compared to normal non-osteoporotic group. However, SPH (15 mg/kg) significantly increased the level of alkaline phosphatase (ALP) to normal level. Treatment with SPH (30 mg/kg) increased the level of ALP to be higher than normal group. SPH (15 mg/kg) did not significantly increase the serum level of osteocalcin (OC) compared to OVX group. On the other hand, treatment with SPH (30 mg/kg) significantly increased the level of OC to 78% higher than normal non-ovarectomized animals group. In addition, SPH (15 mg/kg) decreased the bone resorption marker, acid phosphatase (ACP) to normal level and SPH (30 mg/kg) further diminished the level of serum ACP. Histopathologically, sophoricoside ameliorated the ovarectomy induced osteoporosis in a dose dependent manner. The drug showed thicker bony trabeculae, more osteoid, and more osteoblastic rimming compared to OVX group.

Show MeSH
Related in: MedlinePlus