Immunoregulatory and anti-HIV-1 enzyme activities of antioxidant components from lotus (Nelumbo nucifera Gaertn.) rhizome.
In the present study, two antioxidant micromolecular components (L2f-2 and L2f-3) and an antioxidant macromolecular component LB2 were extracted from lotus (Nelumbo nucifera Gaertn.) rhizomes. MS, FTIR (Fourier-transform IR) spectroscopy and NMR were used to identify these compounds. L2f-2 was (+/-)-gallocatechin, L2f-3 was (-)-catechin and LB2 was a polysaccharide-protein complex with a molecular mass of 18.8 kDa. LB2 was identified as a polysaccharide sulfate containing α/β-pyranose and α-furanose according to its FTIR spectrogram. It was composed of mannose, rhamnose, glucose, galactose and xylose with a molar ratio 2:8:7:8:1. The antioxidant components L2f-2, L2f-3 and LB2 strongly inhibited HIV-1 RT (reverse transcriptase) and IN (integrase). LB2 inhibited RT with an IC50 value of 33.7 μM. It also exhibited the highest HIV-1 3'-processing inhibitory activity with an IC50 value of 5.28 μM. Both L2f-2 and L2f-3 up-regulated the expression of IL-2 (interleukin-2) and down-regulated IL-10, while LB2 exhibited positive regulation on IL-2, IL-4 and IL-10. Moreover, L2f-3 and LB2 might inhibit HIV-1 directly by down-regulating TNFα (tumour necrosis factor α). These natural antioxidant components with antiviral and immunoregulatory activities could be potentially important for anti HIV-1 drug development and application to HIV-1 therapy.
*Center for AIDS Research, Nankai University, Tianjin, People's Republic of China.
Yun
Y
Jiang
†School of Biomedical Sciences, Faculty of Medicine, The Chinese University of Hong Kong, Shatin, New Territories, Hong Kong, People's Republic of China.
Tzi Bun
TB
Ng
*Center for AIDS Research, Nankai University, Tianjin, People's Republic of China.
Zhaokun
Z
Liu
*Center for AIDS Research, Nankai University, Tianjin, People's Republic of China.
Changrong
C
Wang
*Center for AIDS Research, Nankai University, Tianjin, People's Republic of China.
Ning
N
Li
*Center for AIDS Research, Nankai University, Tianjin, People's Republic of China.
Wentao
W
Qiao
‡Department of Microbiology, Nankai University, Tianjin, People's Republic of China.
Fang
F
Liua
D000818:Animals; D000975:Antioxidants / Q000737:chemistry / Q000494:pharmacology*; D002392:Catechin / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology; D016207:Cytokines / Q000235:genetics / Q000378:metabolism; D015870:Gene Expression / Q000187:drug effects; D019427:HIV Integrase / Q000737:chemistry; D019428:HIV Integrase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors; D007155:Immunologic Factors / Q000737:chemistry / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D015227:Lipid Peroxidation; D008297:Male; D008807:Mice, Inbred BALB C; D031653:Nelumbo / Q000737:chemistry*; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology*; D011134:Polysaccharides / Q000737:chemistry / Q000494:pharmacology*; D018894:Reverse Transcriptase Inhibitors / Q000737:chemistry / Q000494:pharmacology; D027343:Rhizome / Q000737:chemistry*; D013463:Sulfuric Acid Esters / Q000737:chemistry / Q000494:pharmacology*
D000975:Antioxidants; D016207:Cytokines; D019428:HIV Integrase Inhibitors; D007155:Immunologic Factors; D010936:Plant Extracts; D011134:Polysaccharides; D018894:Reverse Transcriptase Inhibitors; D013463:Sulfuric Acid Esters; D002392:Catechin; D019427:HIV Integrase; C514824:reverse transcriptase, Human immunodeficiency virus 1; D054303:HIV Reverse Transcriptase; C057580:gallocatechol; C514801:p31 integrase protein, Human immunodeficiency virus 1