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Article: Molecular docking analysis of Withaferin A from Withania somnifera with the Glucose regulated protein 78 (GRP78) receptor and the SARS-CoV-2 main protease.

Sudeep, H V / Gouthamchandra, K / Shyamprasad, K

2020 Volume 16, Issue 5, Page(s) 411–417

Abstract: Design and development of an effective compound to combat COVID-19 is clearly critical in the current circumstances. Therefore, it is of interest to document the molecular docking analysis data of the cellular receptor Glucose regulated protein 78 (GRP78) ...

Abstract	Design and development of an effective compound to combat COVID-19 is clearly critical in the current circumstances. Therefore, it is of interest to document the molecular docking analysis data of the cellular receptor Glucose regulated protein 78 (GRP78) with Withaferin A from Withania somnifera in the context of COVID-19 pandemic for further consideration. Here, we report the optimal interaction features of withaferin A, artemisinin, curcumin and andrographolide with the GRP78 receptor having low binding energies (-8.7, -7.89, -6.21 and -6.17 kcal/mol respectively) in this report. In order to gain additional insights, the interaction pattern of compounds with SARS-CoV-2 main protease (Mpro) was studied.
Keywords	covid19
Language	English
Publishing date	2020-04-30
Publishing country	Singapore
Document type	Journal Article
ZDB-ID	2203786-X
ISSN	0973-2063
ISSN	0973-2063
DOI	10.6026/97320630016411
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: ViphyllinTM, a Standardized Black Pepper Seed Extract Exerts Antinociceptive Effects in Murine Pain Models via Activation of Cannabinoid Receptor CB2, Peroxisome Proliferator-Activated Receptor-Alpha and TRPV1 Ion Channels

Venkatakrishna K / Sundeep K / Sudeep HV / Gouthamchandra K / Shyamprasad K

Journal of Pain Research, Vol Volume 15, Pp 355-

2022 Volume 366

Abstract: Karempudi Venkatakrishna, Kuppam Sundeep, Heggar Venkataramana Sudeep, Kuluvar Gouthamchandra, Kodimule Shyamprasad R&D Center for Excellence, Vidya Herbs Pvt Ltd, Bangalore, 560 105, Karnataka, IndiaCorrespondence: Heggar Venkataramana Sudeep, Tel +91 ... ...

Abstract	Karempudi Venkatakrishna, Kuppam Sundeep, Heggar Venkataramana Sudeep, Kuluvar Gouthamchandra, Kodimule Shyamprasad R&D Center for Excellence, Vidya Herbs Pvt Ltd, Bangalore, 560 105, Karnataka, IndiaCorrespondence: Heggar Venkataramana Sudeep, Tel +91 80-42094158, Email research@vidyaherbs.comPurpose: Plant-based natural products as anti-nociceptors have enormous potential as safer alternatives to conventional opiates and NSAIDS. Piper nigrum (black pepper) is one of the major culinary spices with medicinal attributes.Methods: In the present study, the antinociceptive activity of a standardized black pepper seed extract (Viphyllin) containing not less than 30% β-caryophyllene (BCP) was evaluated using pain models in mice, namely acetic acid-induced writhing test, formalin-induced paw licking test, hot plate test and tail flick test. Further, the antagonists SR141716A (0.1 mg/kg i.p.), AM630 (5 mg/kg i.p.), capsazepine (0.1 mg/kg body weight i.p.), and GW6471 (1 mg/kg i.p.) were used to evaluate the involvement of cannabinoid receptors CB1 and CB2, TRPV1 ion channel and PPARα receptor, respectively. Molecular docking (AutoDock 4.2) was used to study the interaction of BCP with the agonist-binding sites of the selected pain receptors.Results: Viphyllin at 10 mg, 25 mg and 50 mg/kg (i.p.) significantly inhibited the writhings in mice as compared to untreated control group (p < 0.001). Further, Viphyllin at 50 mg/kg showed strong antinociceptive effect in formalin-induced paw licking test (p < 0.05). Pretreatment of mice with AM630 significantly reversed the antinociceptive activity of Viphyllin in both early and late phases of formalin test (p < 0.05). Administration of Viphyllin markedly increased the latency time of mice in hot plate test (p < 0.001). Further, Viphyllin markedly increased the latency time of tail flick compared to control group from 30 min to 90 min after treatment. AM630, Capsazepine, and GW6471 abolished the analgesic effect of Viphyllin. These findings clearly suggest the ...
Keywords	piper nigrum ; β-caryophyllene ; pain ; nociceptive receptors ; Medicine (General) ; R5-920
Subject code	616
Language	English
Publishing date	2022-02-01T00:00:00Z
Publisher	Dove Medical Press
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article: Oral and Topical Administration of a Standardized Saw Palmetto Oil Reduces Hair Fall and Improves the Hair Growth in Androgenetic Alopecia Subjects - A 16-Week Randomized, Placebo-Controlled Study.

Sudeep, Heggar Venkataramana / Rashmi, Sriram / Jestin, Thomas V / Richards, Aleksander / Gouthamchandra, Kuluvar / Shyamprasad, Kodimule

Clinical, cosmetic and investigational dermatology

2023 Volume 16, Page(s) 3251–3266

Abstract: Purpose: Androgenetic alopecia (AGA) is the most common type of hair loss in humans, affecting self-esteem and emotional well-being. This study aimed to assess the safety and efficacy of VISPO: Methods: In a double-blind, placebo-controlled, four-arm ...

Abstract	Purpose: Androgenetic alopecia (AGA) is the most common type of hair loss in humans, affecting self-esteem and emotional well-being. This study aimed to assess the safety and efficacy of VISPO Methods: In a double-blind, placebo-controlled, four-arm clinical study, 80 healthy male and female subjects aged 18-50 years were randomly allocated (1:1:1:1) to receive either 400 mg capsules of VISPO or 5 mL of a topical formulation containing 20% VISPO or the respective placebo once daily for 16 weeks. The primary endpoints included hair count (hair comb and hair pull tests) and the self-assessment of perceived efficacy. Objective evaluation was performed using the global photographic assessment score. Hair density, thickness, and anagen/telogen ratio were evaluated using phototrichogram analysis. Results: At the end of the study, oral and topical formulations of VISPO reduced hair fall by up to 29% ( Conclusion: VISPO formulations reduced hair fall and promoted hair regrowth and scalp appearance in AGA patients.
Language	English
Publishing date	2023-11-11
Publishing country	New Zealand
Document type	Case Reports ; Clinical Trial
ZDB-ID	2494852-4
ISSN	1178-7015
ISSN	1178-7015
DOI	10.2147/CCID.S435795
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Article ; Online: A standardized extract of

Sudeep, Heggar Venkataramana / Gouthamchandra, Kuluvar / Ramanaiah, Illuri / Raj, Amritha / Naveen, Puttaswamy / Shyamprasad, Kodimule

Pharmaceutical biology

2023 Volume 61, Issue 1, Page(s) 1211–1221

Abstract: Context: Preparations of : Objective: In this study, : Materials and methods: The standardized hydroalcoholic extract (4% chicoric acid) was prepared from the aerial parts of : Results: The SEP extract inhibited DPPH (IC50 = 106.7 µg/mL), ABTS!# ...

Abstract	Context: Preparations of Objective: In this study, Materials and methods: The standardized hydroalcoholic extract (4% chicoric acid) was prepared from the aerial parts of Results: The SEP extract inhibited DPPH (IC50 = 106.7 µg/mL), ABTS Conclusion: Our results strongly support SEP extract with 4% chicoric acid as a functional ingredient for immunomodulation.
MeSH term(s)	Mice ; Male ; Animals ; Echinacea/chemistry ; Nitric Oxide ; Cytokines ; Plant Extracts/pharmacology ; Plant Extracts/chemistry ; Macrophages ; Immunosuppression Therapy ; Immunity
Chemical Substances	chicoric acid (S4YY3V8YHD) ; Nitric Oxide (31C4KY9ESH) ; Cytokines ; Plant Extracts
Language	English
Publishing date	2023-08-15
Publishing country	England
Document type	Journal Article
ZDB-ID	1440131-9
ISSN	1744-5116 ; 1388-0209
ISSN (online)	1744-5116
ISSN	1388-0209
DOI	10.1080/13880209.2023.2244000
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Article: Molecular docking analysis of Withaferin A from Withania somnifera with the Glucose regulated protein 78 (GRP78) receptor and the SARS-CoV-2 main protease

Sudeep, H V / Gouthamchandra, K / Shyamprasad, K

Bioinformation

Abstract	Design and development of an effective compound to combat COVID-19 is clearly critical in the current circumstances. Therefore, it is of interest to document the molecular docking analysis data of the cellular receptor Glucose regulated protein 78 (GRP78) with Withaferin A from Withania somnifera in the context of COVID-19 pandemic for further consideration. Here, we report the optimal interaction features of withaferin A, artemisinin, curcumin and andrographolide with the GRP78 receptor having low binding energies (-8.7, -7.89, -6.21 and -6.17 kcal/mol respectively) in this report. In order to gain additional insights, the interaction pattern of compounds with SARS-CoV-2 main protease (Mpro) was studied.
Keywords	covid19
Publisher	WHO
Document type	Article
Note	WHO #Covidence: #729743
Database	COVID19

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Article: Viwithan, a Standardized

Sudeep, H V / Gouthamchandra, K / Venkatesh, B J / Prasad, K Shyam

Pharmacognosy magazine

2018 Volume 13, Issue Suppl 4, Page(s) S801–S806

Abstract: Background: Withania somnifera: Objective: In the present study, we have evaluated the antiproliferative activity of a standardized : Materials and methods: The cytotoxicity of Viwithan was determined using thiazolyl blue tetrazolium blue assay ... ...

Abstract	Background: Withania somnifera Objective: In the present study, we have evaluated the antiproliferative activity of a standardized Materials and methods: The cytotoxicity of Viwithan was determined using thiazolyl blue tetrazolium blue assay and crystal violet staining. The apoptotic changes in B16F1 cells following treatment with Viwithan were observed by acridine orange/ethidium bromide (AO/EB) staining and DNA fragmentation assay. The binding affinity of withanolides in Viwithan with antiapoptotic proteins B-cell lymphoma 2, B-cell lymphoma-extra large, and myeloid cell leukemia 1 (MCL-1) were studied using Results: The half maximal inhibitory concentration (IC50) values of Viwithan against liver hepatocellular carcinoma, Henrietta Lacks cervical carcinoma cells, human colorectal carcinoma cell line, and Ehrlich ascites carcinoma cells were 1830, 968, 2715, and 633 μg/ml, respectively. Interestingly, Viwithan was highly effective against B16F1 cells with an IC50 value of 220 μg/ml after 24 h treatment. The morphological alterations of apoptotic cell death were clearly observed in the AO/EB-stained cells after treatment with Viwithan. Viwithan induced late apoptotic changes in treated B16F1 cells as evident by the ladder formation of fragmented DNA in a time-dependent manner. The findings of molecular docking showed that withanolides present in Viwithan have a more binding affinity with the antiapoptotic proteins, particularly MCL-1. Conclusion: We have reported for the first time that Viwithan with 5% withanolides has a potent cytotoxic effect, particularly against B16F1 murine melanoma cells among the different cancer cell lines tested. Summary: The present study reports for the first time that Viwithan, a standardized 5%
Language	English
Publishing date	2018-01-31
Publishing country	India
Document type	Journal Article
ZDB-ID	2274976-7
ISSN	0976-4062 ; 0973-1296
ISSN (online)	0976-4062
ISSN	0973-1296
DOI	10.4103/pm.pm_121_17
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Article ; Online: A standardized black pepper seed extract containing β-caryophyllene improves cognitive function in scopolamine-induced amnesia model mice via regulation of brain-derived neurotrophic factor and MAPK proteins.

Sudeep, H V / Venkatakrishna, K / Amritharaj / Gouthamchandra, K / Reethi, B / Naveen, P / Lingaraju, H B / Shyamprasad, K

Journal of food biochemistry

2021 Volume 45, Issue 12, Page(s) e13994

Abstract: β-caryophyllene (BCP), a natural sesquiterpene present in plants, is a selective agonist of cannabinoid receptor type-2 (CB2) of the endocannabinoid system. In this study, we have prepared an extract from Piper nigrum (black pepper) seeds using ... ...

Abstract	β-caryophyllene (BCP), a natural sesquiterpene present in plants, is a selective agonist of cannabinoid receptor type-2 (CB2) of the endocannabinoid system. In this study, we have prepared an extract from Piper nigrum (black pepper) seeds using supercritical fluid extraction, standardized to contain 30% BCP (Viphyllin
MeSH term(s)	Amnesia/chemically induced ; Amnesia/drug therapy ; Animals ; Brain-Derived Neurotrophic Factor ; Cognition ; Male ; Mice ; Piper nigrum ; Plant Extracts/pharmacology ; Plant Extracts/therapeutic use ; Polycyclic Sesquiterpenes ; Scopolamine/toxicity
Chemical Substances	Brain-Derived Neurotrophic Factor ; Plant Extracts ; Polycyclic Sesquiterpenes ; caryophyllene (BHW853AU9H) ; Scopolamine (DL48G20X8X)
Language	English
Publishing date	2021-11-14
Publishing country	United States
Document type	Journal Article
ZDB-ID	433846-7
ISSN	1745-4514 ; 0145-8884
ISSN (online)	1745-4514
ISSN	0145-8884
DOI	10.1111/jfbc.13994
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Article ; Online: Kinetics and computational analysis of cholinesterase inhibition by REVERC3, a bisdemethoxycurcumin-rich extract

Sudeep HV / Amritha Raj / Gouthamchandra K / Chandrappa S / Shyamprasad K

SAGE Open Medicine, Vol

Relevance to the treatment of Alzheimer’s disease

2020 Volume 8

Abstract: Objectives: Cholinesterase inhibition is a common strategy to treat Alzheimer’s disease. In this study, we have investigated the cholinesterase inhibitory effects of a first-of-its-kind turmeric extract (REVERC3) having enriched content of ... ...

Abstract	Objectives: Cholinesterase inhibition is a common strategy to treat Alzheimer’s disease. In this study, we have investigated the cholinesterase inhibitory effects of a first-of-its-kind turmeric extract (REVERC3) having enriched content of bisdemethoxycurcumin as major active curcuminoid. Methods : The inhibition studies were performed using Ellman’s colorimetric assay. The kinetics of acetylcholinesterase and butyrylcholinesterase was determined in the presence of REVERC3 using the Lineweaver–Burk double reciprocal plots. Furthermore, we used AutoDock tools to predict the binding of bisdemethoxycurcumin with the active sites of cholinesterases. Results : REVERC3 showed 4.8- and 5.39-fold higher inhibitory potential of acetylcholinesterase and butyrylcholinesterase with IC50 values of 29.08 and 33.59 µg/mL, respectively, compared to the regular turmeric extract. The mode of binding of REVERC3 was competitive in the case of acetylcholinesterase while it was uncompetitive for the inhibition of butyrylcholinesterase. Docking analysis revealed that bisdemethoxycurcumin, the major constituent of REVERC3, has different preferences of binding in the active sites of acetylcholinesterase and butyrylcholinesterase. However, the best binding pose predictions are in line with the experimental binding mode of the cholinesterases. Conclusion : These results indicate that bisdemethoxycurcumin-enriched turmeric extract could improve the cholinergic functions via dual inhibition of cholinesterases. However, the predominant role of bisdemethoxycurcumin in REVERC3 must be further validated using preclinical studies and clinical trials.
Keywords	Medicine (General) ; R5-920
Subject code	500
Language	English
Publishing date	2020-11-01T00:00:00Z
Publisher	SAGE Publishing
Document type	Article ; Online
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Article: Viphyllin

Venkatakrishna, Karempudi / Sundeep, Kuppam / Sudeep, Heggar Venkataramana / Gouthamchandra, Kuluvar / Shyamprasad, Kodimule

Journal of pain research

2022 Volume 15, Page(s) 355–366

Abstract: Purpose: Plant-based natural products as anti-nociceptors have enormous potential as safer alternatives to conventional opiates and NSAIDS. : Methods: In the present study, the antinociceptive activity of a standardized black pepper seed extract ( ... ...

Abstract	Purpose: Plant-based natural products as anti-nociceptors have enormous potential as safer alternatives to conventional opiates and NSAIDS. Methods: In the present study, the antinociceptive activity of a standardized black pepper seed extract (Viphyllin) containing not less than 30% β-caryophyllene (BCP) was evaluated using pain models in mice, namely acetic acid-induced writhing test, formalin-induced paw licking test, hot plate test and tail flick test. Further, the antagonists SR141716A (0.1 mg/kg i.p.), AM630 (5 mg/kg i.p.), capsazepine (0.1 mg/kg body weight i.p.), and GW6471 (1 mg/kg i.p.) were used to evaluate the involvement of cannabinoid receptors CB1 and CB2, TRPV1 ion channel and PPARα receptor, respectively. Molecular docking (AutoDock 4.2) was used to study the interaction of BCP with the agonist-binding sites of the selected pain receptors. Results: Viphyllin at 10 mg, 25 mg and 50 mg/kg (i.p.) significantly inhibited the writhings in mice as compared to untreated control group ( Conclusion: In conclusion, Viphyllin could be a natural pain-relieving agent involving safer pain signaling mechanisms, unlike conventional opiates and NSAIDs.
Language	English
Publishing date	2022-02-05
Publishing country	New Zealand
Document type	Journal Article
ZDB-ID	2495284-9
ISSN	1178-7090
ISSN	1178-7090
DOI	10.2147/JPR.S351513
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Article: Efficacy of a Standardized Turmeric Extract Comprised of 70% Bisdemothoxy-Curcumin (REVERC3) Against LPS-Induced Inflammation in RAW264.7 Cells and Carrageenan-Induced Paw Edema.

Gouthamchandra, Kuluvar / Sudeep, Heggar Venkataramana / Chandrappa, Siddappa / Raj, Amrith / Naveen, Puttaswamy / Shyamaprasad, Kodimule

Journal of inflammation research

2021 Volume 14, Page(s) 859–868

Abstract: Objective: It is well known that regular turmeric extract with 95% curcuminoid is comprised of curcumin (70.07%), desmethoxycurcumin (20.28%), and bisdemethoxycurcumin (BDMC) (3.63%). In the current study for the first time, we have enriched about 3% of ...

Abstract	Objective: It is well known that regular turmeric extract with 95% curcuminoid is comprised of curcumin (70.07%), desmethoxycurcumin (20.28%), and bisdemethoxycurcumin (BDMC) (3.63%). In the current study for the first time, we have enriched about 3% of bisdemethoxycurcumin (BDMC) to 70% as well as named it as REVERC3 and compared anti-inflammatory activity with regular turmeric extract using in vitro and in vivo models of inflammation. Methods: To reveal the potential anti-inflammatory mechanism of action, we investigated nitric oxide (NO) scavenging, xanthine oxidase, and lipoxygenase inhibitory activity, further determined the level of pro-inflammatory cytokines, such as interleukin 6 (IL-6), tumor necrosis factor (TNF-α) and major inflammatory mediators like cyclooxygenase (COX-2) and inducible nitric oxide synthase (iNOS), inhibition in lipopolysaccharide (LPS) induced inflammation in RAW macrophage cells. In the other hand, a carrageenan-stimulated inflammatory rat model was carried out. Results: Our study findings exhibited a significant anti-inflammatory activity of REVERC3 together with nitric oxide (NO), xanthine oxidase, and lipoxygenase inhibition. Further, we attenuated the levels of cyclooxygenase (COX-2), inducible nitric oxide synthase (iNOS), interleukin (IL-6) and tumor necrosis factor (TNF-α) expressions in the LPS-elicited RAW macrophage cells. REVERC3 showed a potential anti-inflammatory activity by inhibiting carrageenan induced paw edema after 4 hr at the dose of 100mg/kg body weight. Conclusion: Thus, our findings collectively indicated that the REVERC3 could efficiently inhibit inflammation compared to regular turmeric extract. Since bisdemethoxycurcumin is a stable molecule it could be effectively used in the applications of health care and the nutraceutical industry, indeed which deserves further investigations.
Language	English
Publishing date	2021-03-12
Publishing country	New Zealand
Document type	Journal Article
ZDB-ID	2494878-0
ISSN	1178-7031
ISSN	1178-7031
DOI	10.2147/JIR.S291293
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