The aerial parts of Triumfetta flavescens H. (N. O. Tiliaceae) afforded a new alkaloidal steroid ... more The aerial parts of Triumfetta flavescens H. (N. O. Tiliaceae) afforded a new alkaloidal steroid glycoside, characterized as stigma 5(6)-ene-7,22-dione-25-methylamino-3 beta,23 beta-diol-3-O-beta-D- glucoside and designated as triumfettoside (1); and a new sterol identified as stigma 5(6)-ene-7,22-dione-3 beta,23 beta-diol, designated as triumfettosterol (2). Their structures were elucidated on the basis of chemical and spectral analysis.
Journal of Biomolecular Structure & Dynamics, Jun 26, 2021
Generally, herbal medicines having remarkable popularity for treating liver ailments, but they ar... more Generally, herbal medicines having remarkable popularity for treating liver ailments, but they are still unacceptable because of the deprivation of herbal drug standardization. Therefore, there is a need for promising synthetic drugs to overcome the critical liver problem. We introduce 1, 3, 4-oxadiazine ring in this study to identify better anti-hepatotoxic agents via a suitable synthetic route. These oxadiazine-based derivatives were structurally confirmed by analytical and spectral data and evaluated for their anti-hepatotoxic potential. Further, in vitro hepatotoxicity studies have been done to check the toxicity level in the synthesized compound. Compounds 5a, 5b, 5c and 9d were selected for further biological evaluation according to in vitro results. After that, CCl4-induced animal model was used to evaluate in vivo anti-hepatotoxicity activity. Compound 5a with 52.99%, 59.3%, 79.34% and 5b with 52.16%, 57.65%, 75.10% revealed to be most promising for reduction in level of SGPT, SGOT and ALKP, respectively. Moreover, it was also observed that the compound 5a with 411.01%, 53.39% and 5b with 378.63%, 48.9% level of albumin and total protein were respectively. The induced-fit docking results of the compounds 5a and 5b reveal some essential binding information and exhibited desirable ADME properties, and obeyed Lipinski's rule of five. In addition, molecular dynamics studies for 100 ns further confirm the protein-ligand complex's stability, supporting the in vitro and in vivo data, and help in establishing the SAR of synthesized compounds. Two compounds, 5a and 5 b, exhibited higher anti-hepatotoxic activity than the standard drug silymarin. Communicated by Ramaswamy H. Sarma.
Background: Diabetes mellitus and Alzheimer’s disease are two common diseases that majorly affect... more Background: Diabetes mellitus and Alzheimer’s disease are two common diseases that majorly affect the elderly population. Patients in both cases are increasing day by day. They are considered two independent diseases, but recent evidence suggests that they have a lot in common. Objective: In this review, we focused on the connection between Alzheimer's disease and diabetes and highlighted the importance of antidiabetic drugs against Alzheimer's disease. Methods: Common pathways such as obesity, vascular diseases, oxidative stress, mitochondrial dysfunction, mutation of the ApoE4 gene, and Sirtuin gene were found to manipulate both diseases. Antidiabetic drugs are found to have promising effects on Alzheimer’s disease, acting by reducing insulin resistance, neuronal protection, and reducing amyloid-beta plaques. Some anti-diabetic drugs have shown promising results in vivo and in vitro studies. Results: No review present focuses on the structural features of the antidiabetic ...
Background: Non-small cell lung cancer (NSCLC) is a deadly disease that affects millions globally... more Background: Non-small cell lung cancer (NSCLC) is a deadly disease that affects millions globally and its treatment includes surgery, chemotherapy, and radiotherapy. Chemotherapy and radiotherapy have many disadvantages, which include potential harmful side effects. Due to the widespread use of drugs in lung cancer, drug treatment becomes challenging due to multidrug resistance and adverse reactions. According to the recent findings, natural products (NPs) and their derivatives are being used to inhibit and suppress cancer cells. Objective: Our objective is to highlight the importance of phytochemicals for treating NSCLC by focusing on the structural features essential for the desired activity with fewer side effects compared to synthetic molecules. Method: This review incorporated data from the most recent literature, including in vitro, in vivo, nanoformulation-based recent advancements, and clinical trials, as well as the structure-activity relationship (SAR), described for a var...
CNS & Neurological Disorders - Drug Targets, 2021
: Pyrimidine is an aromatic and heterocyclic organic compound containing a 6-membered ring consis... more : Pyrimidine is an aromatic and heterocyclic organic compound containing a 6-membered ring consisting of four carbon and two nitrogen atoms on alternative positions. Pyrimidine scaffolds described their existence in the medicinal chemist’s cause for their synthesizing practicability and nonpoisonous nature. However, the reason behind neurological disorders is still an open challenge for scientific research and development organizations. Efficacy voids are widespread before researchers, despite high throughput research in the field of anti-Alzheimer's drugs.Researchers have constantly investigated all the probabilities for restraining the unwanted adverse effects of the anti-Alzheimer’s agents and are focusing more extensively to rehabilitate neurological disorders. The scientific literature on drug development has been an aspiration to medicinal chemists and other researchers to facilitate further research. Therefore, this review emphasizes the structure-activity relationship (SAR) based approach and the pharmacological advancements of pyrimidine moiety in the new era of therapeutics as anti-Alzheimer’s agents.
Quercetin, a bioflavonol is widely found in nature and possesses diverse pharmacological properti... more Quercetin, a bioflavonol is widely found in nature and possesses diverse pharmacological properties. A heterocyclic 1,4 dioxane nucleus was incorporated in Quercetin structure to obtain two structural analogues of silybin. The aim of the study was to antihepatotoxic potential of Quercetin derivatives containing 1,4 dioxane heterocyclic ring in Carbon tetrachloride (CCl4) induced hepatotoxicity in female Wistar Albino rats. Two Quercetin derivatives (QD) were synthesized by reported method. QD were administered orally at dose of 10 mg/kg, once daily for 7 days to Wistar Albino rats. A single dose of CCl4(1mL/kg) was used for inducing liver damage. Antihepatotoxic activity was evaluated by measuring levels of total proteins (TP), total albumin (TA), alkaline phosphatase (ALKP) and liver enzymes such as serum glutamate oxaloacetate (SGOT) and serum glutamate pyruvate transaminase (SGPT).QD exhibited potent antihepatotoxic activity with respect to standard drug silybon-70. However, it w...
: As a source of therapeutic agents, heterocyclic nitrogen-containing compounds and their derivat... more : As a source of therapeutic agents, heterocyclic nitrogen-containing compounds and their derivatives are still interesting and essential. Pyrazole, a five-member heteroaromatic ring with two nitrogen atoms, has a major impact in chemical industries as well as pharmaceutical industries. Due to its wide range of biological activities against various diseases, it has been identified as a biologically important heterocyclic scaffold. The treatment of neurological disorders has always been a difficult task in both the past and present. Therefore, identifying therapeutically effective molecules for neurological conditions remains an open challenge in biomedical research and development. For developing novel entities as neuroprotective agents, recently, pyrazole scaffold has attracted medicinal chemists worldwide. The major focus of research in this area is discovering novel molecules as neuroprotective agents with minimal adverse effects and better effectiveness in improving the neurological condition. This review mainly covers recent developments in the neuropharmacological role of pyrazole incorporated compounds, including their structural-activity relationship (SAR), which also further includes IC50 values (in mM as well as in μM), recent patents, and a brief history as neuroprotective agents.
Ethyl 3, 4, 5-trihydroxybenzoate (GAE) is a major bioactive constituent of Hippophae Rhamnoides L... more Ethyl 3, 4, 5-trihydroxybenzoate (GAE) is a major bioactive constituent of Hippophae Rhamnoides L. leaves and extract prepared from H. rhamnoides leaves exhibited radioprotective and pharmacological activity. Radiomodifying properties of polyphenol compounds through free radical neutralizing have been reported earlier. However, to date pharmacokinetic (PK) and biodistribution of polyphenol compounds post 60Co-γ-irradiation (5 Gy) exposure have not been studied yet. The study aims to investigate the radio modifying and inflammatory action, PK and biodistribution of GAE at a radioprotective dose and changes, if any, induced after irradiation. Male C 57 BL/6 mice (28–30 g) were administered GAE (200 mg/kg b.wt) orally 15 minutes post to irradiation. Mice were sacrificed at 15, 30 min, 1,2,4,8 and 24 h. PK and biodistribution of GAE in plasma and tissues were studied. The radiomodifying potential was assessed in terms of mitigating NF-kB activity and SGOT, SGPT, urea and creatinine leve...
Wedelia calendulaceahas a long history of use in the Indian Ayurvedic System of Medicine for the ... more Wedelia calendulaceahas a long history of use in the Indian Ayurvedic System of Medicine for the treatment, prevention, and cure of a diverse range of human diseases such as diabetes obesity, and other metabolic diseases.
A new compound derivative of glycoside 19-α-hydroxy-ursolic acid glucoside (19-α-hydroxyurs-12(13... more A new compound derivative of glycoside 19-α-hydroxy-ursolic acid glucoside (19-α-hydroxyurs-12(13)-ene-28-oic acid-3-O-β-D-glucopyranoside (HEG) was isolated from whole plant of Wedelia calendulacea (Compositae). The structure was elucidated and established by standard spectroscopy approaches. Diethylnitrosamine (DEN) (200 mg/kg) and ferric nitrilotriacetate (Fe-NTA) (9 mg/kg) were used for induction of renal cell carcinoma (RCC) in the rats. The rats were further divided into different groups and were treated with HEG doses for 22 weeks. Anti-cancer effect in RCC by HEG was dose dependent to restrict the macroscopical changes as compared to DEN + Fe-NTA-control animals. Significant alteration in biochemical parameters and dose-dependent alleviation in Phase I and Phase II antioxidant enzymes were responsible for its chemo-protective nature. HEG in dose-dependent manner was significant to alter the elevated levels of pro-inflammatory cytokines and inflammatory mediators during RCC. ...
In the present study, we evaluated the antihepatotoxic activity of the different fractions of Nym... more In the present study, we evaluated the antihepatotoxic activity of the different fractions of Nymphaea stellata by performing biochemical parameters and histopathological studies against toxicity caused by the carbon tetrachloride. The histopathological studies of the liver showed swelling and necrosis in hepatocytes in CCl4 treated rats, treatment with different fractions have reduced significantly the necrosis and swelling of the hepatocytes. The biochemical parameters also showed the significant antihepatotoxic activity.
Silybum marianum is a medicinal plant used widely for treating liver diseases. The silymarin, a m... more Silybum marianum is a medicinal plant used widely for treating liver diseases. The silymarin, a mixture of three flavolignan isomers namely silybin (1), silydianin (2), and silychristin (3) is an active constituent of the plant. However, silybin containing 1, 4-dioxane ring is the most potent antihepatotoxic agent. In contrast, other isomers do not possess 1, 4-dioxane ring, and thus do not exhibit a significant activity. We, therefore, thought that 1, 4-dioxane ring plays an important role in displaying antihepatotoxic activity, and have prepared some chalcones containing 1, 4-dioxane ring. The synthesized compounds were evaluated for antihepatotoxic activity against carbon tetrachloride induced hepatotoxicity in albino rats. The degree of protection was measured by using biochemical parameters like serum glutamic oxaloacetic transaminase (SGOT), serum glutamic pyruvate transaminase (SGPT), alkaline phosphatase (ALKP), total protein (TP) and total albumin (TA). The compounds namely...
The aerial parts of Triumfetta flavescens H. (N. O. Tiliaceae) afforded a new alkaloidal steroid ... more The aerial parts of Triumfetta flavescens H. (N. O. Tiliaceae) afforded a new alkaloidal steroid glycoside, characterized as stigma 5(6)-ene-7,22-dione-25-methylamino-3 beta,23 beta-diol-3-O-beta-D- glucoside and designated as triumfettoside (1); and a new sterol identified as stigma 5(6)-ene-7,22-dione-3 beta,23 beta-diol, designated as triumfettosterol (2). Their structures were elucidated on the basis of chemical and spectral analysis.
Journal of Biomolecular Structure & Dynamics, Jun 26, 2021
Generally, herbal medicines having remarkable popularity for treating liver ailments, but they ar... more Generally, herbal medicines having remarkable popularity for treating liver ailments, but they are still unacceptable because of the deprivation of herbal drug standardization. Therefore, there is a need for promising synthetic drugs to overcome the critical liver problem. We introduce 1, 3, 4-oxadiazine ring in this study to identify better anti-hepatotoxic agents via a suitable synthetic route. These oxadiazine-based derivatives were structurally confirmed by analytical and spectral data and evaluated for their anti-hepatotoxic potential. Further, in vitro hepatotoxicity studies have been done to check the toxicity level in the synthesized compound. Compounds 5a, 5b, 5c and 9d were selected for further biological evaluation according to in vitro results. After that, CCl4-induced animal model was used to evaluate in vivo anti-hepatotoxicity activity. Compound 5a with 52.99%, 59.3%, 79.34% and 5b with 52.16%, 57.65%, 75.10% revealed to be most promising for reduction in level of SGPT, SGOT and ALKP, respectively. Moreover, it was also observed that the compound 5a with 411.01%, 53.39% and 5b with 378.63%, 48.9% level of albumin and total protein were respectively. The induced-fit docking results of the compounds 5a and 5b reveal some essential binding information and exhibited desirable ADME properties, and obeyed Lipinski's rule of five. In addition, molecular dynamics studies for 100 ns further confirm the protein-ligand complex's stability, supporting the in vitro and in vivo data, and help in establishing the SAR of synthesized compounds. Two compounds, 5a and 5 b, exhibited higher anti-hepatotoxic activity than the standard drug silymarin. Communicated by Ramaswamy H. Sarma.
Background: Diabetes mellitus and Alzheimer’s disease are two common diseases that majorly affect... more Background: Diabetes mellitus and Alzheimer’s disease are two common diseases that majorly affect the elderly population. Patients in both cases are increasing day by day. They are considered two independent diseases, but recent evidence suggests that they have a lot in common. Objective: In this review, we focused on the connection between Alzheimer's disease and diabetes and highlighted the importance of antidiabetic drugs against Alzheimer's disease. Methods: Common pathways such as obesity, vascular diseases, oxidative stress, mitochondrial dysfunction, mutation of the ApoE4 gene, and Sirtuin gene were found to manipulate both diseases. Antidiabetic drugs are found to have promising effects on Alzheimer’s disease, acting by reducing insulin resistance, neuronal protection, and reducing amyloid-beta plaques. Some anti-diabetic drugs have shown promising results in vivo and in vitro studies. Results: No review present focuses on the structural features of the antidiabetic ...
Background: Non-small cell lung cancer (NSCLC) is a deadly disease that affects millions globally... more Background: Non-small cell lung cancer (NSCLC) is a deadly disease that affects millions globally and its treatment includes surgery, chemotherapy, and radiotherapy. Chemotherapy and radiotherapy have many disadvantages, which include potential harmful side effects. Due to the widespread use of drugs in lung cancer, drug treatment becomes challenging due to multidrug resistance and adverse reactions. According to the recent findings, natural products (NPs) and their derivatives are being used to inhibit and suppress cancer cells. Objective: Our objective is to highlight the importance of phytochemicals for treating NSCLC by focusing on the structural features essential for the desired activity with fewer side effects compared to synthetic molecules. Method: This review incorporated data from the most recent literature, including in vitro, in vivo, nanoformulation-based recent advancements, and clinical trials, as well as the structure-activity relationship (SAR), described for a var...
CNS & Neurological Disorders - Drug Targets, 2021
: Pyrimidine is an aromatic and heterocyclic organic compound containing a 6-membered ring consis... more : Pyrimidine is an aromatic and heterocyclic organic compound containing a 6-membered ring consisting of four carbon and two nitrogen atoms on alternative positions. Pyrimidine scaffolds described their existence in the medicinal chemist’s cause for their synthesizing practicability and nonpoisonous nature. However, the reason behind neurological disorders is still an open challenge for scientific research and development organizations. Efficacy voids are widespread before researchers, despite high throughput research in the field of anti-Alzheimer's drugs.Researchers have constantly investigated all the probabilities for restraining the unwanted adverse effects of the anti-Alzheimer’s agents and are focusing more extensively to rehabilitate neurological disorders. The scientific literature on drug development has been an aspiration to medicinal chemists and other researchers to facilitate further research. Therefore, this review emphasizes the structure-activity relationship (SAR) based approach and the pharmacological advancements of pyrimidine moiety in the new era of therapeutics as anti-Alzheimer’s agents.
Quercetin, a bioflavonol is widely found in nature and possesses diverse pharmacological properti... more Quercetin, a bioflavonol is widely found in nature and possesses diverse pharmacological properties. A heterocyclic 1,4 dioxane nucleus was incorporated in Quercetin structure to obtain two structural analogues of silybin. The aim of the study was to antihepatotoxic potential of Quercetin derivatives containing 1,4 dioxane heterocyclic ring in Carbon tetrachloride (CCl4) induced hepatotoxicity in female Wistar Albino rats. Two Quercetin derivatives (QD) were synthesized by reported method. QD were administered orally at dose of 10 mg/kg, once daily for 7 days to Wistar Albino rats. A single dose of CCl4(1mL/kg) was used for inducing liver damage. Antihepatotoxic activity was evaluated by measuring levels of total proteins (TP), total albumin (TA), alkaline phosphatase (ALKP) and liver enzymes such as serum glutamate oxaloacetate (SGOT) and serum glutamate pyruvate transaminase (SGPT).QD exhibited potent antihepatotoxic activity with respect to standard drug silybon-70. However, it w...
: As a source of therapeutic agents, heterocyclic nitrogen-containing compounds and their derivat... more : As a source of therapeutic agents, heterocyclic nitrogen-containing compounds and their derivatives are still interesting and essential. Pyrazole, a five-member heteroaromatic ring with two nitrogen atoms, has a major impact in chemical industries as well as pharmaceutical industries. Due to its wide range of biological activities against various diseases, it has been identified as a biologically important heterocyclic scaffold. The treatment of neurological disorders has always been a difficult task in both the past and present. Therefore, identifying therapeutically effective molecules for neurological conditions remains an open challenge in biomedical research and development. For developing novel entities as neuroprotective agents, recently, pyrazole scaffold has attracted medicinal chemists worldwide. The major focus of research in this area is discovering novel molecules as neuroprotective agents with minimal adverse effects and better effectiveness in improving the neurological condition. This review mainly covers recent developments in the neuropharmacological role of pyrazole incorporated compounds, including their structural-activity relationship (SAR), which also further includes IC50 values (in mM as well as in μM), recent patents, and a brief history as neuroprotective agents.
Ethyl 3, 4, 5-trihydroxybenzoate (GAE) is a major bioactive constituent of Hippophae Rhamnoides L... more Ethyl 3, 4, 5-trihydroxybenzoate (GAE) is a major bioactive constituent of Hippophae Rhamnoides L. leaves and extract prepared from H. rhamnoides leaves exhibited radioprotective and pharmacological activity. Radiomodifying properties of polyphenol compounds through free radical neutralizing have been reported earlier. However, to date pharmacokinetic (PK) and biodistribution of polyphenol compounds post 60Co-γ-irradiation (5 Gy) exposure have not been studied yet. The study aims to investigate the radio modifying and inflammatory action, PK and biodistribution of GAE at a radioprotective dose and changes, if any, induced after irradiation. Male C 57 BL/6 mice (28–30 g) were administered GAE (200 mg/kg b.wt) orally 15 minutes post to irradiation. Mice were sacrificed at 15, 30 min, 1,2,4,8 and 24 h. PK and biodistribution of GAE in plasma and tissues were studied. The radiomodifying potential was assessed in terms of mitigating NF-kB activity and SGOT, SGPT, urea and creatinine leve...
Wedelia calendulaceahas a long history of use in the Indian Ayurvedic System of Medicine for the ... more Wedelia calendulaceahas a long history of use in the Indian Ayurvedic System of Medicine for the treatment, prevention, and cure of a diverse range of human diseases such as diabetes obesity, and other metabolic diseases.
A new compound derivative of glycoside 19-α-hydroxy-ursolic acid glucoside (19-α-hydroxyurs-12(13... more A new compound derivative of glycoside 19-α-hydroxy-ursolic acid glucoside (19-α-hydroxyurs-12(13)-ene-28-oic acid-3-O-β-D-glucopyranoside (HEG) was isolated from whole plant of Wedelia calendulacea (Compositae). The structure was elucidated and established by standard spectroscopy approaches. Diethylnitrosamine (DEN) (200 mg/kg) and ferric nitrilotriacetate (Fe-NTA) (9 mg/kg) were used for induction of renal cell carcinoma (RCC) in the rats. The rats were further divided into different groups and were treated with HEG doses for 22 weeks. Anti-cancer effect in RCC by HEG was dose dependent to restrict the macroscopical changes as compared to DEN + Fe-NTA-control animals. Significant alteration in biochemical parameters and dose-dependent alleviation in Phase I and Phase II antioxidant enzymes were responsible for its chemo-protective nature. HEG in dose-dependent manner was significant to alter the elevated levels of pro-inflammatory cytokines and inflammatory mediators during RCC. ...
In the present study, we evaluated the antihepatotoxic activity of the different fractions of Nym... more In the present study, we evaluated the antihepatotoxic activity of the different fractions of Nymphaea stellata by performing biochemical parameters and histopathological studies against toxicity caused by the carbon tetrachloride. The histopathological studies of the liver showed swelling and necrosis in hepatocytes in CCl4 treated rats, treatment with different fractions have reduced significantly the necrosis and swelling of the hepatocytes. The biochemical parameters also showed the significant antihepatotoxic activity.
Silybum marianum is a medicinal plant used widely for treating liver diseases. The silymarin, a m... more Silybum marianum is a medicinal plant used widely for treating liver diseases. The silymarin, a mixture of three flavolignan isomers namely silybin (1), silydianin (2), and silychristin (3) is an active constituent of the plant. However, silybin containing 1, 4-dioxane ring is the most potent antihepatotoxic agent. In contrast, other isomers do not possess 1, 4-dioxane ring, and thus do not exhibit a significant activity. We, therefore, thought that 1, 4-dioxane ring plays an important role in displaying antihepatotoxic activity, and have prepared some chalcones containing 1, 4-dioxane ring. The synthesized compounds were evaluated for antihepatotoxic activity against carbon tetrachloride induced hepatotoxicity in albino rats. The degree of protection was measured by using biochemical parameters like serum glutamic oxaloacetic transaminase (SGOT), serum glutamic pyruvate transaminase (SGPT), alkaline phosphatase (ALKP), total protein (TP) and total albumin (TA). The compounds namely...
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