This work describes an analytical platform based on semi-high-resolution antileishmanial profilin... more This work describes an analytical platform based on semi-high-resolution antileishmanial profiling combined with hyphenation of high-performance liquid chromatography - high-resolution mass spectrometry - solid-phase extraction - nuclear magnetic resonance spectroscopy, i.e., semiHR-antileishmanial assay/HPLC-HRMS-SPE-NMR. The platform enables fast pinpointing of HPLC peaks representing Leishmania tropica inhibitors in complex matrices, with subsequent structural identification of targeted inhibitors. Active analytes were cumulatively trapped on SPE cartridges and the structures elucidated by analysis of NMR spectra obtained in the HPLC-HRMS-SPE-NMR mode. This led to the identification of six known compounds 2,4,6-trihydroxyacetophenone-2-O-β-D-glucopyranoside (1), lalioside (2), luteolin-4'-O-β-D-glucopyranoside (3), apigenin-4'-O-β-D-glucopyranoside (4), luteolin (5), and apigenin (6). IC50 of the active compounds were determined with luteolin being the most potent inhibit...
Severe Acute Respiratory Syndrome (SARS-CoV2) infected about 93 million people and killed over tw... more Severe Acute Respiratory Syndrome (SARS-CoV2) infected about 93 million people and killed over two million worldwide. The disease transmits very quickly, therefore; due to its severity and widespread the World Health Organization has declared this menace as ‘Global Pandemic’. An urgent need was felt to manage this disease through aggressive and efficient research process all over the globe. That’s why drug re-purposing of 212 chemical entities (CEs) against SARS-COV2 was found to be one of the efficient ways in finding new indications of already discovered drugs amisdst of the discovery of a new drug. Results of this study revealed that out of 212 CEs, only Etodolac forms a hydrogen (H)-bond with a relatively low energy and active central fragment, demonstrating more significant interaction with SARS-CoV2 viral proteins. Other CEs exhibit good pharmacokinetics properties with the least acute toxicity through ADMET analysis. We also discovered other therapeutic applications of these ...
Severe Acute Respiratory Syndrome (SARS-CoV2) infected about 93 million people and killed over tw... more Severe Acute Respiratory Syndrome (SARS-CoV2) infected about 93 million people and killed over two million worldwide. The disease transmits very quickly, therefore; due to its severity and widespread the World Health Organization has declared this menace as ‘Global Pandemic’. An urgent need was felt to manage this disease through aggressive and efficient research process all over the globe. That’s why drug re-purposing of 212 chemical entities (CEs) against SARS-COV2 was found to be one of the efficient ways in finding new indications of already discovered drugs amisdst of the discovery of a new drug. Results of this study revealed that out of 212 CEs, only Etodolac forms a hydrogen (H)-bond with a relatively low energy and active central fragment, demonstrating more significant interaction with SARS-CoV2 viral proteins. Other CEs exhibit good pharmacokinetics properties with the least acute toxicity through ADMET analysis. We also discovered other therapeutic applications of these ...
The current study was planned to assess the different oxidative, Endocrinological and biochemical... more The current study was planned to assess the different oxidative, Endocrinological and biochemical parameters using extract of Catharanthus roseus (C. roseus) on diabetic rats. Three groups of Diabetic rats were assigned viz. Group A have Negative Control which was fed basal diet; Group B have Positive Control and was non-supplemented; and Group C supplemented with C. roseus extract. The results showed that blood glucose level, ALT, TGs and urea concentration was elevated non-significantly (P>0.05), of Group C which was supplemented by C. roseus when compared with non-supplemented Group B animals. In Group C which was supplemented by C. roseus, AST, and Cholesterol results were decreased as showed by statistics analysis (non-significantly). When level of Blood cortisol was compared between Group C and B, there was increased in Group C, as per non-significant statistics measurements (P>0.05). It was observed that level of T4 and T3 hormones was decreased in Group C (supplemented...
Aim: To investigate the different antileishmanial activities of extracts of Cassia Fistula L., Mo... more Aim: To investigate the different antileishmanial activities of extracts of Cassia Fistula L., Morus Nigra L. and Ziziphus Jujuba Mill. Methodology: In this method, three (03) plants having concentrations between 500 – 2000 µg/mL were subjected to KWH23 strains of L. tropica in which Standard drug was Amphotericin B and have negative control for 24 – 48 hours. To check the in-vivo studies, plant extract was tested on BALB/c mice (Iqbal et al., 2016). Results: It showed that inhibition (mean) of KWH23 strains at 500, 1000, 1500, 2000 µg/mL after 48 hours were 92.1 ± 0.02, 95.00 ± 0.05, 97.09 ± 0.07 and 98.05 ± 0.05 % respectively. It decreased the lesion size (mean) from 0.8 ± 0.1 mm to 0.40 ± 0.2 mm having significance value p < 0.01 after 8th week, and cure at 200 mg/Kg against intracellular amastigotes in BALB/c mice was 90.00% (95% Cl = 80.05 – 97.00). Conclusion: The result shows that Ziziphus jujuba Mill. leaves possess significant antileishmanial activity.
Purpose: To examine the anti-leishmanial and cytotoxic effects of five naturally occurring phenol... more Purpose: To examine the anti-leishmanial and cytotoxic effects of five naturally occurring phenolic compounds: luteolin (1), lalioside (2), luteolin-4'-O-β-D-glucopyranoside (3), apigenin 4-O-β-D-glucopyranoside (4) and apigenin (5) on Leishmania tropica KWH23 amastigotes. Methods: The compounds were isolated from the leaves of Lawsonia Inermis via hyphenated high performance liquid chromatography-high resolution mass spectrometry coupled with solid phase extraction-tube transfer nuclear magnetic resonance technique. The isolated compounds were given intraperitoneally to L. tropica KWH23 amastigotes-infected albino mice at a dose of ≥ 3 mg/kg for 5 days. Amphotericin-B was used as standard (reference) drug. Lymphocytes were used to analyze their cytotoxicity. Results: For compound 1, mean lesion size decreased from 0.82 ± 0.12 to 0.10 ± 0.01 after 120 days, with 97 % cure of intracellular L. tropica amastigotes at a dose of 15 mg/kg, compared to amphotericin B which produced 95 % cure at a dose of 30 mg/kg. Half-maximal concentration (IC50) for compound 1 was 4.15 µg/ml against lymphocytes. Conclusion: The results indicate that luteolin is a potent inhibitor of L. tropica amastigotes, with a higher cytotoxic activity against lymphocytes, compared with luteolin-4'-O-β-D-glucopyranoside.
This work describes an analytical platform based on semi-high-resolution antileishmanial
profiling... more This work describes an analytical platform based on semi-high-resolution antileishmanial profiling combined with hyphenation of high-performance liquid chromatography – high-resolution mass spectrometry – solid-phase extraction – nuclear magnetic resonance spectroscopy, i.e., semiHR-antileishmanial assay/HPLC-HRMS-SPE-NMR. The platform enables fast pinpointing of HPLC peaks representing Leishmania tropica inhibitors in complex matrices, with subsequent structural identification of targeted inhibitors. Active analytes were cumulatively trapped on SPE cartridges and the structures elucidated by analysis of NMR spectra obtained in the HPLC-HRMSSPE-NMR mode. This led to the identification of six known compounds 2,4,6trihydroxyacetophenone-2-O-β-D-glucopyranoside (1), lalioside (2), luteolin-4-O-β-Dglucopyranoside (3), apigenin-4-O-β-D-glucopyranoside (4), luteolin (5), and apigenin (6). IC50 of the active compounds were determined with luteolin being the most potent inhibitor with an IC50 value of 4.15µg/ml. The platform proved to be an efficient method for the identification of L. tropica inhibitors.
Purpose: To evaluate the in vitro and in vivo anti-leishmanial and cytotoxic activities of extrac... more Purpose: To evaluate the in vitro and in vivo anti-leishmanial and cytotoxic activities of extracts of different parts of Lawsonia Inermis, Morus nigra and Ziziphus mauritiana. Methods: The methanol extracts of all three plant materials at concentrations of 10-100 µg/mL were tested for their in vitro anti-leishmanial effects on L. tropica KWH23 promastigotes for 24-48 h, relative to negative control and amphotericin-B (standard drug). For in vivo anti-leishmanial activity, the extracts were tested against L. tropica-infected albino mice, while cytotoxicity was investigated against mammalian cells (lymphocytes). Results: For Lawsonia Inermis leaves, mean inhibition of extracellular promastigotes at 10, 25, 50 and 100 µg/mL after 48 h were 98.2 ± 0.06, 98.75 ± 1.09, 99.31 ± 0.00 and 100.00 ± 0.00 %, respectively. After 8 weeks, mean lesion size decreased from 0.8 ± 0.2 mm to 0.3 ± 0.1 mm (p < 0.01), and cure at 150 mg/kg against intracellular amastigotes in albino mice was 97.02 % (95 % CI = 96.14-98.10). IC50 for Lawsonia inermis leaf extract was 12.22 µg/mL (95 % CI = 11.54-13.84) against lymphocytes. Conclusion: The results obtained in this study show that Lawsonia Inermis leaf is safe and possesses potent anti-leishmanial activity.
This work describes an analytical platform based on semi-high-resolution antileishmanial profilin... more This work describes an analytical platform based on semi-high-resolution antileishmanial profiling combined with hyphenation of high-performance liquid chromatography - high-resolution mass spectrometry - solid-phase extraction - nuclear magnetic resonance spectroscopy, i.e., semiHR-antileishmanial assay/HPLC-HRMS-SPE-NMR. The platform enables fast pinpointing of HPLC peaks representing Leishmania tropica inhibitors in complex matrices, with subsequent structural identification of targeted inhibitors. Active analytes were cumulatively trapped on SPE cartridges and the structures elucidated by analysis of NMR spectra obtained in the HPLC-HRMS-SPE-NMR mode. This led to the identification of six known compounds 2,4,6-trihydroxyacetophenone-2-O-β-D-glucopyranoside (1), lalioside (2), luteolin-4'-O-β-D-glucopyranoside (3), apigenin-4'-O-β-D-glucopyranoside (4), luteolin (5), and apigenin (6). IC50 of the active compounds were determined with luteolin being the most potent inhibit...
Severe Acute Respiratory Syndrome (SARS-CoV2) infected about 93 million people and killed over tw... more Severe Acute Respiratory Syndrome (SARS-CoV2) infected about 93 million people and killed over two million worldwide. The disease transmits very quickly, therefore; due to its severity and widespread the World Health Organization has declared this menace as ‘Global Pandemic’. An urgent need was felt to manage this disease through aggressive and efficient research process all over the globe. That’s why drug re-purposing of 212 chemical entities (CEs) against SARS-COV2 was found to be one of the efficient ways in finding new indications of already discovered drugs amisdst of the discovery of a new drug. Results of this study revealed that out of 212 CEs, only Etodolac forms a hydrogen (H)-bond with a relatively low energy and active central fragment, demonstrating more significant interaction with SARS-CoV2 viral proteins. Other CEs exhibit good pharmacokinetics properties with the least acute toxicity through ADMET analysis. We also discovered other therapeutic applications of these ...
Severe Acute Respiratory Syndrome (SARS-CoV2) infected about 93 million people and killed over tw... more Severe Acute Respiratory Syndrome (SARS-CoV2) infected about 93 million people and killed over two million worldwide. The disease transmits very quickly, therefore; due to its severity and widespread the World Health Organization has declared this menace as ‘Global Pandemic’. An urgent need was felt to manage this disease through aggressive and efficient research process all over the globe. That’s why drug re-purposing of 212 chemical entities (CEs) against SARS-COV2 was found to be one of the efficient ways in finding new indications of already discovered drugs amisdst of the discovery of a new drug. Results of this study revealed that out of 212 CEs, only Etodolac forms a hydrogen (H)-bond with a relatively low energy and active central fragment, demonstrating more significant interaction with SARS-CoV2 viral proteins. Other CEs exhibit good pharmacokinetics properties with the least acute toxicity through ADMET analysis. We also discovered other therapeutic applications of these ...
The current study was planned to assess the different oxidative, Endocrinological and biochemical... more The current study was planned to assess the different oxidative, Endocrinological and biochemical parameters using extract of Catharanthus roseus (C. roseus) on diabetic rats. Three groups of Diabetic rats were assigned viz. Group A have Negative Control which was fed basal diet; Group B have Positive Control and was non-supplemented; and Group C supplemented with C. roseus extract. The results showed that blood glucose level, ALT, TGs and urea concentration was elevated non-significantly (P>0.05), of Group C which was supplemented by C. roseus when compared with non-supplemented Group B animals. In Group C which was supplemented by C. roseus, AST, and Cholesterol results were decreased as showed by statistics analysis (non-significantly). When level of Blood cortisol was compared between Group C and B, there was increased in Group C, as per non-significant statistics measurements (P>0.05). It was observed that level of T4 and T3 hormones was decreased in Group C (supplemented...
Aim: To investigate the different antileishmanial activities of extracts of Cassia Fistula L., Mo... more Aim: To investigate the different antileishmanial activities of extracts of Cassia Fistula L., Morus Nigra L. and Ziziphus Jujuba Mill. Methodology: In this method, three (03) plants having concentrations between 500 – 2000 µg/mL were subjected to KWH23 strains of L. tropica in which Standard drug was Amphotericin B and have negative control for 24 – 48 hours. To check the in-vivo studies, plant extract was tested on BALB/c mice (Iqbal et al., 2016). Results: It showed that inhibition (mean) of KWH23 strains at 500, 1000, 1500, 2000 µg/mL after 48 hours were 92.1 ± 0.02, 95.00 ± 0.05, 97.09 ± 0.07 and 98.05 ± 0.05 % respectively. It decreased the lesion size (mean) from 0.8 ± 0.1 mm to 0.40 ± 0.2 mm having significance value p < 0.01 after 8th week, and cure at 200 mg/Kg against intracellular amastigotes in BALB/c mice was 90.00% (95% Cl = 80.05 – 97.00). Conclusion: The result shows that Ziziphus jujuba Mill. leaves possess significant antileishmanial activity.
Purpose: To examine the anti-leishmanial and cytotoxic effects of five naturally occurring phenol... more Purpose: To examine the anti-leishmanial and cytotoxic effects of five naturally occurring phenolic compounds: luteolin (1), lalioside (2), luteolin-4'-O-β-D-glucopyranoside (3), apigenin 4-O-β-D-glucopyranoside (4) and apigenin (5) on Leishmania tropica KWH23 amastigotes. Methods: The compounds were isolated from the leaves of Lawsonia Inermis via hyphenated high performance liquid chromatography-high resolution mass spectrometry coupled with solid phase extraction-tube transfer nuclear magnetic resonance technique. The isolated compounds were given intraperitoneally to L. tropica KWH23 amastigotes-infected albino mice at a dose of ≥ 3 mg/kg for 5 days. Amphotericin-B was used as standard (reference) drug. Lymphocytes were used to analyze their cytotoxicity. Results: For compound 1, mean lesion size decreased from 0.82 ± 0.12 to 0.10 ± 0.01 after 120 days, with 97 % cure of intracellular L. tropica amastigotes at a dose of 15 mg/kg, compared to amphotericin B which produced 95 % cure at a dose of 30 mg/kg. Half-maximal concentration (IC50) for compound 1 was 4.15 µg/ml against lymphocytes. Conclusion: The results indicate that luteolin is a potent inhibitor of L. tropica amastigotes, with a higher cytotoxic activity against lymphocytes, compared with luteolin-4'-O-β-D-glucopyranoside.
This work describes an analytical platform based on semi-high-resolution antileishmanial
profiling... more This work describes an analytical platform based on semi-high-resolution antileishmanial profiling combined with hyphenation of high-performance liquid chromatography – high-resolution mass spectrometry – solid-phase extraction – nuclear magnetic resonance spectroscopy, i.e., semiHR-antileishmanial assay/HPLC-HRMS-SPE-NMR. The platform enables fast pinpointing of HPLC peaks representing Leishmania tropica inhibitors in complex matrices, with subsequent structural identification of targeted inhibitors. Active analytes were cumulatively trapped on SPE cartridges and the structures elucidated by analysis of NMR spectra obtained in the HPLC-HRMSSPE-NMR mode. This led to the identification of six known compounds 2,4,6trihydroxyacetophenone-2-O-β-D-glucopyranoside (1), lalioside (2), luteolin-4-O-β-Dglucopyranoside (3), apigenin-4-O-β-D-glucopyranoside (4), luteolin (5), and apigenin (6). IC50 of the active compounds were determined with luteolin being the most potent inhibitor with an IC50 value of 4.15µg/ml. The platform proved to be an efficient method for the identification of L. tropica inhibitors.
Purpose: To evaluate the in vitro and in vivo anti-leishmanial and cytotoxic activities of extrac... more Purpose: To evaluate the in vitro and in vivo anti-leishmanial and cytotoxic activities of extracts of different parts of Lawsonia Inermis, Morus nigra and Ziziphus mauritiana. Methods: The methanol extracts of all three plant materials at concentrations of 10-100 µg/mL were tested for their in vitro anti-leishmanial effects on L. tropica KWH23 promastigotes for 24-48 h, relative to negative control and amphotericin-B (standard drug). For in vivo anti-leishmanial activity, the extracts were tested against L. tropica-infected albino mice, while cytotoxicity was investigated against mammalian cells (lymphocytes). Results: For Lawsonia Inermis leaves, mean inhibition of extracellular promastigotes at 10, 25, 50 and 100 µg/mL after 48 h were 98.2 ± 0.06, 98.75 ± 1.09, 99.31 ± 0.00 and 100.00 ± 0.00 %, respectively. After 8 weeks, mean lesion size decreased from 0.8 ± 0.2 mm to 0.3 ± 0.1 mm (p < 0.01), and cure at 150 mg/kg against intracellular amastigotes in albino mice was 97.02 % (95 % CI = 96.14-98.10). IC50 for Lawsonia inermis leaf extract was 12.22 µg/mL (95 % CI = 11.54-13.84) against lymphocytes. Conclusion: The results obtained in this study show that Lawsonia Inermis leaf is safe and possesses potent anti-leishmanial activity.
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Papers by Kashif Iqbal
profiling combined with hyphenation of high-performance liquid chromatography –
high-resolution mass spectrometry – solid-phase extraction – nuclear magnetic
resonance spectroscopy, i.e., semiHR-antileishmanial assay/HPLC-HRMS-SPE-NMR.
The platform enables fast pinpointing of HPLC peaks representing Leishmania tropica
inhibitors in complex matrices, with subsequent structural identification of targeted
inhibitors. Active analytes were cumulatively trapped on SPE cartridges and the
structures elucidated by analysis of NMR spectra obtained in the HPLC-HRMSSPE-NMR
mode. This led to the identification of six known compounds 2,4,6trihydroxyacetophenone-2-O-β-D-glucopyranoside
(1), lalioside (2), luteolin-4-O-β-Dglucopyranoside
(3), apigenin-4-O-β-D-glucopyranoside (4), luteolin (5), and apigenin
(6). IC50 of the active compounds were determined with luteolin being the most potent
inhibitor with an IC50 value of 4.15µg/ml. The platform proved to be an efficient method
for the identification of L. tropica inhibitors.
profiling combined with hyphenation of high-performance liquid chromatography –
high-resolution mass spectrometry – solid-phase extraction – nuclear magnetic
resonance spectroscopy, i.e., semiHR-antileishmanial assay/HPLC-HRMS-SPE-NMR.
The platform enables fast pinpointing of HPLC peaks representing Leishmania tropica
inhibitors in complex matrices, with subsequent structural identification of targeted
inhibitors. Active analytes were cumulatively trapped on SPE cartridges and the
structures elucidated by analysis of NMR spectra obtained in the HPLC-HRMSSPE-NMR
mode. This led to the identification of six known compounds 2,4,6trihydroxyacetophenone-2-O-β-D-glucopyranoside
(1), lalioside (2), luteolin-4-O-β-Dglucopyranoside
(3), apigenin-4-O-β-D-glucopyranoside (4), luteolin (5), and apigenin
(6). IC50 of the active compounds were determined with luteolin being the most potent
inhibitor with an IC50 value of 4.15µg/ml. The platform proved to be an efficient method
for the identification of L. tropica inhibitors.