|
|
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char = s;code = 115
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char = ,;code = 44
char = ;code = 32
char = A;code = 65
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char = ;code = 32
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char = t;code = 116
char = y;code = 121
char = .;code = 46
result sql = Cocrystal Formation of Betulinic Acid and Ascorbic Acid: Synthesis, Physico-Chemical Assessment, Antioxidant, and Antiproliferative Activity.
Cocrystal Formation of Betulinic Acid and Ascorbic Acid: Synthesis, Physico-Chemical Assessment, Antioxidant, and Antiproliferative Activity.char = B;code = 66
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char = ;code = 32
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char = A;code = 65
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result sql = Betulinic acid (BA) was demonstrated to be a very promising anticancer agent against various tumor cell lines such as breast, colon, lung, and brain. Despite its strong cytotoxic effect, betulinic acid exhibits low water solubility, feature that is reflected in its poor bioavailability. To overcome these drawbacks, numerous strategies were conducted to improve its physicochemical and pharmacokinetic profile, among which cocrystalization emerged as a promising approach. Thus, our work consisted in obtaining slowly grown cocrystals of BA and ascorbic acid (BA+VitC) in isopropyl alcohol obtained in a hydrothermal experiment. The newly formed cocrystals were characterized by physico-chemical methods such asSEM, DSC, XRPD, and FT-IR spectroscopy demonstrating BA+VitC cocrystal formation while their antioxidant activity revealed an additive antioxidant effect. To investigate the biological effect, BA+VitC cocrystals were tested on HaCat (immortalized human keratinocytes), B164A5 and B16F0 (murine melanoma), MCF7 and MDA-MB-231 (human breast cancer), and HeLa (cervical cancer) cell lines. Results of BA upon the tested tumor cell lines, after co-crystallization with vitamin C, indicated a superior cytotoxic effect with the preservation of a good selectivity index assumably due to an improved BA water solubility and consequently an optimized bioavailability.
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result sql = Cocrystal Formation of Betulinic Acid and Ascorbic Acid: Synthesis, Physico-Chemical Assessment, Antioxidant, and Antiproliferative Activity.
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char = D;code = 68
char = e;code = 101
char = s;code = 115
char = p;code = 112
char = i;code = 105
char = t;code = 116
char = e;code = 101
char = ;code = 32
char = i;code = 105
char = t;code = 116
char = s;code = 115
char = ;code = 32
char = s;code = 115
char = t;code = 116
char = r;code = 114
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char = n;code = 110
char = g;code = 103
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char = c;code = 99
char = y;code = 121
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char = t;code = 116
char = o;code = 111
char = x;code = 120
char = i;code = 105
char = c;code = 99
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char = e;code = 101
char = f;code = 102
char = f;code = 102
char = e;code = 101
char = c;code = 99
char = t;code = 116
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char = ;code = 32
char = b;code = 98
char = e;code = 101
char = t;code = 116
char = u;code = 117
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char = i;code = 105
char = c;code = 99
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char = a;code = 97
char = c;code = 99
char = i;code = 105
char = d;code = 100
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char = e;code = 101
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char = t;code = 116
char = s;code = 115
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char = w;code = 119
char = ;code = 32
char = w;code = 119
char = a;code = 97
char = t;code = 116
char = e;code = 101
char = r;code = 114
char = ;code = 32
char = s;code = 115
char = o;code = 111
char = l;code = 108
char = u;code = 117
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char = i;code = 105
char = l;code = 108
char = i;code = 105
char = t;code = 116
char = y;code = 121
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char = ;code = 32
char = f;code = 102
char = e;code = 101
char = a;code = 97
char = t;code = 116
char = u;code = 117
char = r;code = 114
char = e;code = 101
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char = t;code = 116
char = h;code = 104
char = a;code = 97
char = t;code = 116
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char = i;code = 105
char = s;code = 115
char = ;code = 32
char = r;code = 114
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char = f;code = 102
char = l;code = 108
char = e;code = 101
char = c;code = 99
char = t;code = 116
char = e;code = 101
char = d;code = 100
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char = i;code = 105
char = n;code = 110
char = ;code = 32
char = i;code = 105
char = t;code = 116
char = s;code = 115
char = ;code = 32
char = p;code = 112
char = o;code = 111
char = o;code = 111
char = r;code = 114
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char = b;code = 98
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char = o;code = 111
char = a;code = 97
char = v;code = 118
char = a;code = 97
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char = l;code = 108
char = a;code = 97
char = b;code = 98
char = i;code = 105
char = l;code = 108
char = i;code = 105
char = t;code = 116
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char = ;code = 32
char = T;code = 84
char = o;code = 111
char = ;code = 32
char = o;code = 111
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char = e;code = 101
char = r;code = 114
char = c;code = 99
char = o;code = 111
char = m;code = 109
char = e;code = 101
char = ;code = 32
char = t;code = 116
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char = e;code = 101
char = s;code = 115
char = e;code = 101
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char = d;code = 100
char = r;code = 114
char = a;code = 97
char = w;code = 119
char = b;code = 98
char = a;code = 97
char = c;code = 99
char = k;code = 107
char = s;code = 115
char = ,;code = 44
char = ;code = 32
char = n;code = 110
char = u;code = 117
char = m;code = 109
char = e;code = 101
char = r;code = 114
char = o;code = 111
char = u;code = 117
char = s;code = 115
char = ;code = 32
char = s;code = 115
char = t;code = 116
char = r;code = 114
char = a;code = 97
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char = e;code = 101
char = g;code = 103
char = i;code = 105
char = e;code = 101
char = s;code = 115
char = ;code = 32
char = w;code = 119
char = e;code = 101
char = r;code = 114
char = e;code = 101
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char = c;code = 99
char = o;code = 111
char = n;code = 110
char = d;code = 100
char = u;code = 117
char = c;code = 99
char = t;code = 116
char = e;code = 101
char = d;code = 100
char = ;code = 32
char = t;code = 116
char = o;code = 111
char = ;code = 32
char = i;code = 105
char = m;code = 109
char = p;code = 112
char = r;code = 114
char = o;code = 111
char = v;code = 118
char = e;code = 101
char = ;code = 32
char = i;code = 105
char = t;code = 116
char = s;code = 115
char = ;code = 32
char = p;code = 112
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char = y;code = 121
char = s;code = 115
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char = c;code = 99
char = o;code = 111
char = c;code = 99
char = h;code = 104
char = e;code = 101
char = m;code = 109
char = i;code = 105
char = c;code = 99
char = a;code = 97
char = l;code = 108
char = ;code = 32
char = a;code = 97
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char = d;code = 100
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char = p;code = 112
char = h;code = 104
char = a;code = 97
char = r;code = 114
char = m;code = 109
char = a;code = 97
char = c;code = 99
char = o;code = 111
char = k;code = 107
char = i;code = 105
char = n;code = 110
char = e;code = 101
char = t;code = 116
char = i;code = 105
char = c;code = 99
char = ;code = 32
char = p;code = 112
char = r;code = 114
char = o;code = 111
char = f;code = 102
char = i;code = 105
char = l;code = 108
char = e;code = 101
char = ,;code = 44
char = ;code = 32
char = a;code = 97
char = m;code = 109
char = o;code = 111
char = n;code = 110
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char = w;code = 119
char = h;code = 104
char = i;code = 105
char = c;code = 99
char = h;code = 104
char = ;code = 32
char = c;code = 99
char = o;code = 111
char = c;code = 99
char = r;code = 114
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char = s;code = 115
char = t;code = 116
char = a;code = 97
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char = i;code = 105
char = z;code = 122
char = a;code = 97
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char = o;code = 111
char = n;code = 110
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char = e;code = 101
char = m;code = 109
char = e;code = 101
char = r;code = 114
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char = e;code = 101
char = d;code = 100
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char = a;code = 97
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char = ;code = 32
char = a;code = 97
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char = p;code = 112
char = r;code = 114
char = o;code = 111
char = m;code = 109
char = i;code = 105
char = s;code = 115
char = i;code = 105
char = n;code = 110
char = g;code = 103
char = ;code = 32
char = a;code = 97
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char = p;code = 112
char = r;code = 114
char = o;code = 111
char = a;code = 97
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char = .;code = 46
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char = T;code = 84
char = h;code = 104
char = u;code = 117
char = s;code = 115
char = ,;code = 44
char = ;code = 32
char = o;code = 111
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char = r;code = 114
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char = w;code = 119
char = o;code = 111
char = r;code = 114
char = k;code = 107
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char = c;code = 99
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char = s;code = 115
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char = s;code = 115
char = t;code = 116
char = e;code = 101
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char = n;code = 110
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char = o;code = 111
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char = t;code = 116
char = a;code = 97
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char = n;code = 110
char = i;code = 105
char = n;code = 110
char = g;code = 103
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char = s;code = 115
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char = o;code = 111
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char = l;code = 108
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char = w;code = 119
char = n;code = 110
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char = c;code = 99
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char = s;code = 115
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char = a;code = 97
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char = s;code = 115
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char = f;code = 102
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char = B;code = 66
char = A;code = 65
char = ;code = 32
char = a;code = 97
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char = A;code = 65
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char = m;code = 109
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char = ;code = 32
char = T;code = 84
char = h;code = 104
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char = e;code = 101
char = w;code = 119
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char = s;code = 115
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char = c;code = 99
char = h;code = 104
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char = S;code = 83
char = E;code = 69
char = M;code = 77
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char = ;code = 32
char = D;code = 68
char = S;code = 83
char = C;code = 67
char = ,;code = 44
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char = X;code = 88
char = R;code = 82
char = P;code = 80
char = D;code = 68
char = ,;code = 44
char = ;code = 32
char = a;code = 97
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char = d;code = 100
char = ;code = 32
char = F;code = 70
char = T;code = 84
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char = I;code = 73
char = R;code = 82
char = ;code = 32
char = s;code = 115
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char = e;code = 101
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char = r;code = 114
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char = s;code = 115
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char = a;code = 97
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char = A;code = 65
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char = V;code = 86
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char = C;code = 67
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char = f;code = 102
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char = B;code = 66
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char = V;code = 86
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char = t;code = 116
char = C;code = 67
char = ;code = 32
char = c;code = 99
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char = e;code = 101
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char = H;code = 72
char = a;code = 97
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char = a;code = 97
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char = i;code = 105
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char = ,;code = 44
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char = B;code = 66
char = 1;code = 49
char = 6;code = 54
char = 4;code = 52
char = A;code = 65
char = 5;code = 53
char = ;code = 32
char = a;code = 97
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char = F;code = 70
char = 0;code = 48
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char = m;code = 109
char = a;code = 97
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char = ,;code = 44
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char = M;code = 77
char = C;code = 67
char = F;code = 70
char = 7;code = 55
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char = a;code = 97
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char = d;code = 100
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char = M;code = 77
char = D;code = 68
char = A;code = 65
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char = M;code = 77
char = B;code = 66
char = -;code = 45
char = 2;code = 50
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char = 1;code = 49
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char = h;code = 104
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char = m;code = 109
char = a;code = 97
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char = a;code = 97
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char = ,;code = 44
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char = a;code = 97
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result sql = Betulinic acid (BA) was demonstrated to be a very promising anticancer agent against various tumor cell lines such as breast, colon, lung, and brain. Despite its strong cytotoxic effect, betulinic acid exhibits low water solubility, feature that is reflected in its poor bioavailability. To overcome these drawbacks, numerous strategies were conducted to improve its physicochemical and pharmacokinetic profile, among which cocrystalization emerged as a promising approach. Thus, our work consisted in obtaining slowly grown cocrystals of BA and ascorbic acid (BA+VitC) in isopropyl alcohol obtained in a hydrothermal experiment. The newly formed cocrystals were characterized by physico-chemical methods such asSEM, DSC, XRPD, and FT-IR spectroscopy demonstrating BA+VitC cocrystal formation while their antioxidant activity revealed an additive antioxidant effect. To investigate the biological effect, BA+VitC cocrystals were tested on HaCat (immortalized human keratinocytes), B164A5 and B16F0 (murine melanoma), MCF7 and MDA-MB-231 (human breast cancer), and HeLa (cervical cancer) cell lines. Results of BA upon the tested tumor cell lines, after co-crystallization with vitamin C, indicated a superior cytotoxic effect with the preservation of a good selectivity index assumably due to an improved BA water solubility and consequently an optimized bioavailability.
Publication: Front Chem 2019 ;7():92.
Publication Date: 2019
Study Author(s): Nicolov Mirela M ; Ghiulai Roxana M RM ; Voicu Mirela M ; Mioc Marius M ; Duse Adina Octavia AO ; Roman Roxana R ; Ambrus Rita R ; Zupko Istvan I ; Moaca Elena Alina EA ; Coricovac Dorina E DE ; Farcas Claudia C ; Racoviceanu Roxana Marcela RM ; Danciu Corina C ; Dehelean Cristina-Adriana CA ; Soica Codruta C ;
Institution: Faculty of Pharmacy, Victor Babes University of Medicine and Pharmacy, Timisoara, Romania.
Shortcut link to this study:
Publication Date: 2019
Study Author(s): Nicolov Mirela M ; Ghiulai Roxana M RM ; Voicu Mirela M ; Mioc Marius M ; Duse Adina Octavia AO ; Roman Roxana R ; Ambrus Rita R ; Zupko Istvan I ; Moaca Elena Alina EA ; Coricovac Dorina E DE ; Farcas Claudia C ; Racoviceanu Roxana Marcela RM ; Danciu Corina C ; Dehelean Cristina-Adriana CA ; Soica Codruta C ;
Institution: Faculty of Pharmacy, Victor Babes University of Medicine and Pharmacy, Timisoara, Romania.
Shortcut link to this study:
Betulinic acid (BA) was demonstrated to be a very promising anticancer agent against various tumor cell lines such as breast, colon, lung, and brain. Despite its strong cytotoxic effect, betulinic acid exhibits low water solubility, feature that is reflected in its poor bioavailability. To overcome these drawbacks, numerous strategies were conducted to improve its physicochemical and pharmacokinetic profile, among which cocrystalization emerged as a promising approach. Thus, our work consisted in obtaining slowly grown cocrystals of BA and ascorbic acid (BA+VitC) in isopropyl alcohol obtained in a hydrothermal experiment. The newly formed cocrystals were characterized by physico-chemical methods such asSEM, DSC, XRPD, and FT-IR spectroscopy demonstrating BA+VitC cocrystal formation while their antioxidant activity revealed an additive antioxidant effect. To investigate the biological effect, BA+VitC cocrystals were tested on HaCat (immortalized human keratinocytes), B164A5 and B16F0 (murine melanoma), MCF7 and MDA-MB-231 (human breast cancer), and HeLa (cervical cancer) cell lines. Results of BA upon the tested tumor cell lines, after co-crystallization with vitamin C, indicated a superior cytotoxic effect with the preservation of a good selectivity index assumably due to an improved BA water solubility and consequently an optimized bioavailability.
PMID: 30847340
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