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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: SPH (15 mg/kg) did not significantly increase the serum level of osteocalcin (OC) compared to OVX 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.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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Histopathological assessment of the anti-osteoporosis effect of sophoricoside.Normal group (A) shows normal bony tissue with intact well-formed dense trabeculae (star in the inner panel) with osteoblastic rimming (arrow) and average intervening bone marrow. OVX group (B) showed scant, disconnected (arrow in inner panel), thin (arrow in the outer panel), and widely separated trabeculae (double-headed arrow in the outer panel) with eroded surface (star in the outer panel). Estrogen treated group (C) showed widely distributed osteoid and osteoblastic rimming (arrow). SPH-15 group (D) showed thick trabeculae (double-headed arrow), more osteoid, and osteoblastic activity (arrow). SPH-30 group (E) showed thick trabeculae (double-headed arrow), more osteoid and osteoblastic activity (arrow).
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pone-0098559-g004: Histopathological assessment of the anti-osteoporosis effect of sophoricoside.Normal group (A) shows normal bony tissue with intact well-formed dense trabeculae (star in the inner panel) with osteoblastic rimming (arrow) and average intervening bone marrow. OVX group (B) showed scant, disconnected (arrow in inner panel), thin (arrow in the outer panel), and widely separated trabeculae (double-headed arrow in the outer panel) with eroded surface (star in the outer panel). Estrogen treated group (C) showed widely distributed osteoid and osteoblastic rimming (arrow). SPH-15 group (D) showed thick trabeculae (double-headed arrow), more osteoid, and osteoblastic activity (arrow). SPH-30 group (E) showed thick trabeculae (double-headed arrow), more osteoid and osteoblastic activity (arrow).

Mentions: The anti-osteoporotic effect of sophoricoside was confirmed pathologically. Histological pictures of femurs of normal animals showed intact, well-formed, dense bony trabeculae with osteoblastic rimming and average intervening bone marrow (Fig. 4-A). Ovarectomy resulted in prominent osteoporosis in OVX group manifested as thin and widely separated trabeculae with notched and eroded surfaces (Fig. 4-B). Estradiol partly reversed the osteoporosis status showing thicker bony trabeculae and more osteoid and osteoblastic rimming compared to OVX group (Fig. 4-C). Sophoricoside ameliorated the ovarectomy induced osteoporosis in a dose dependent manner. Femurs of animals treated with SPH (15 mg/kg) showed thicker bony trabeculae, more osteoid, and more osteoblastic rimming compared to OVX group (Fig. 4-D). Femurs of animals treated with higher dose of SPH (30 mg/kg) showed thicker bony trabeculae, higher osteoid activity with narrow bone marrow spaces compared to OVX group (Fig. 4-E).


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)

Histopathological assessment of the anti-osteoporosis effect of sophoricoside.Normal group (A) shows normal bony tissue with intact well-formed dense trabeculae (star in the inner panel) with osteoblastic rimming (arrow) and average intervening bone marrow. OVX group (B) showed scant, disconnected (arrow in inner panel), thin (arrow in the outer panel), and widely separated trabeculae (double-headed arrow in the outer panel) with eroded surface (star in the outer panel). Estrogen treated group (C) showed widely distributed osteoid and osteoblastic rimming (arrow). SPH-15 group (D) showed thick trabeculae (double-headed arrow), more osteoid, and osteoblastic activity (arrow). SPH-30 group (E) showed thick trabeculae (double-headed arrow), more osteoid and osteoblastic activity (arrow).
© Copyright Policy
Related In: Results  -  Collection

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

pone-0098559-g004: Histopathological assessment of the anti-osteoporosis effect of sophoricoside.Normal group (A) shows normal bony tissue with intact well-formed dense trabeculae (star in the inner panel) with osteoblastic rimming (arrow) and average intervening bone marrow. OVX group (B) showed scant, disconnected (arrow in inner panel), thin (arrow in the outer panel), and widely separated trabeculae (double-headed arrow in the outer panel) with eroded surface (star in the outer panel). Estrogen treated group (C) showed widely distributed osteoid and osteoblastic rimming (arrow). SPH-15 group (D) showed thick trabeculae (double-headed arrow), more osteoid, and osteoblastic activity (arrow). SPH-30 group (E) showed thick trabeculae (double-headed arrow), more osteoid and osteoblastic activity (arrow).
Mentions: The anti-osteoporotic effect of sophoricoside was confirmed pathologically. Histological pictures of femurs of normal animals showed intact, well-formed, dense bony trabeculae with osteoblastic rimming and average intervening bone marrow (Fig. 4-A). Ovarectomy resulted in prominent osteoporosis in OVX group manifested as thin and widely separated trabeculae with notched and eroded surfaces (Fig. 4-B). Estradiol partly reversed the osteoporosis status showing thicker bony trabeculae and more osteoid and osteoblastic rimming compared to OVX group (Fig. 4-C). Sophoricoside ameliorated the ovarectomy induced osteoporosis in a dose dependent manner. Femurs of animals treated with SPH (15 mg/kg) showed thicker bony trabeculae, more osteoid, and more osteoblastic rimming compared to OVX group (Fig. 4-D). Femurs of animals treated with higher dose of SPH (30 mg/kg) showed thicker bony trabeculae, higher osteoid activity with narrow bone marrow spaces compared to OVX group (Fig. 4-E).

Bottom Line: SPH (15 mg/kg) did not significantly increase the serum level of osteocalcin (OC) compared to OVX 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.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