BDNF agonists(Brain-derived neurotrophic factor agonists), GDNF stimulants(Glial cell line-derived neurotrophic factors stimulants), Neurons stimulants

Therapeutic Areas

Nervous System DiseasesEndocrinology and Metabolic DiseaseOther Diseases+ [1]

Active Indication-

Inactive Indication

Amyotrophic Lateral SclerosisGlaucoma

Originator Organization

Phytopharm Plc

Active Organization-

Inactive Organization

Ixico PlcPhytopharm Plc

Drug Highest PhasePendingPhase 1

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC27H44O3

InChIKeyGMBQZIIUCVWOCD-WWASVFFGSA-N

CAS Registry126-19-2

100 Clinical Results associated with Sarsagenin

100 Translational Medicine associated with Sarsagenin

100 Patents (Medical) associated with Sarsagenin

577

Literatures (Medical) associated with Sarsagenin

03 May 2025·Journal of Biomolecular Structure and Dynamics

Natural sapogenins as potential inhibitors of aquaporins for targeted cancer therapy: computational insights into binding and inhibition mechanism

Article

Author: Adnan, Mohd ; Alwaili, Maha Abdullah ; Patel, Mitesh ; Alotaibi, Modhi O. ; Alshammari, Nawaf ; Alotaibi, Nahaa M.

Aquaporins (AQPs) are membrane proteins that facilitate the transport of water and other small molecules across biological membranes. AQPs are involved in various physiological processes and pathological conditions, including cancer, making them as potential targets for anticancer therapy. However, the development of selective and effective inhibitors of AQPs remains a challenge. In this study, we explored the possibility of using natural sapogenins, a class of plant-derived aglycones of saponins with diverse biological activities, as potential inhibitors of AQPs. We performed molecular docking, dynamics simulation and binding energy calculation to investigate the binding and inhibition mechanism of 19 sapogenins against 13 AQPs (AQP0-AQP13) that are overexpressed in various cancers. Our results showed that out of 19 sapogenins, 8 (Diosgenin, Gitogenin, Tigogenin, Ruscogenin, Yamogenin, Hecogenin, Sarsasapogenin and Smilagenin) exhibited acceptable drug-like characteristics. These sapogenin also exhibited favourable binding affinities in the range of -7.6 to -13.4 kcal/mol, and interactions within the AQP binding sites. Furthermore, MD simulations provided insights into stability and dynamics of the sapogenin-AQP complexes. Most of the fluctuations in binding pocket were observed for AQP0-Gitogenin and AQP4-Diosgenin. However, remaining protein-ligand complex showed stable root mean square deviation (RMSD) plots, strong hydrogen bonding interactions, stable solvent-accessible surface area (SASA) values and minimum distance to the receptor. These observations suggest that natural sapogenin hold promise as novel inhibitors of AQPs, offering a basis for the development of innovative therapeutic agents for cancer treatment. However, further validation of the identified compounds through experiments is essential for translating these findings into therapeutic applications.Communicated by Ramaswamy H. Sarma.

01 Apr 2025·Molecular Diversity

Betulin: a novel triterpenoid anti-cancerous agent targeting cervical cancer through epigenetic proteins

Article

Author: Sheoran, Sumit ; Pawar, Smita C ; Prabhu, Dhamodharan ; Perugu, Shyam ; Kour, Satbir ; Vuree, Sugunakar ; Arora, Swati ; Singh, Anjuvan ; Biswas, Indrani

Worldwide, cervical cancer (CCa) is a major killer of women. As the conventional drugs used to treat cervical cancer are expensive and expose severe side effects, there is a growing demand to search for novel modifications. Therefore, in the current investigation employing a bioinformatic approach, we explored triterpenoids for their anti-cancer efficacy by targeting cervical cancer epigenetic proteins, namely DNMT3A, HDAC4, and KMT2C. The study utilized molecular docking, ADMET assay, Molecular Dynamic simulation, and DFT calculation to unveil Betulin (BE) as the potential lead compound. Comparative analysis with that standard drug indicated that BE has a better glide score with the target protein KM2TC (- 9.893 kcal/mol), HDAC4 (- 9.720 kcal/mol), and DNMT3A (- 7.811 kcal/mol), which depicts that BE could be a potent inhibitor of these three epigenetic proteins and exhibits favorable pharmacokinetic, pharmacodynamics and toxicity properties. Molecular Dynamics simulation revealed noteworthy structural stability and compactness. DFT analysis revealed higher molecular activity of BE and showed the most increased kinetic stability (δE = 0.254647 eV). Further, we employed In vitro analysis through MTT assay and found that BE has IC₅₀ of 15 µg/ml. In conclusion, BE can potentially treat CCa upon further investigations using in vivo models for better understanding.

01 Apr 2025·Sugar Tech

Dual Function of Chaetomium globosum CGSR13: Antifungal Agent Against Wilt Caused by Fusarium sacchari and Promoter of Sugarcane Growth

Author: Singh, Dinesh ; Viswanathan, R. ; Chakdar, Hillol ; Singh, D. P. ; Gujjar, Ranjit Singh ; Kumar, Rajeev ; Singh, Shweta ; Yadav, Pooja ; Raj, Chandramani ; Goswami, Sanjay Kumar ; Choudhary, Prassan ; Singh, S. P.

Sugarcane wilt caused by Fusarium sacchari is a destructive and widespread disease globally.In the present era of intensive agriculture system, huge quantities of fungicides are being applied to manage diseases to get high crop yields.However, these fungicides have many non-target effects.For sustainable agriculture, there is a need for eco-friendly methods of growth promotion and crop protection.In this context, a total of 30 endophyte Chaetomium globosum isolates were isolated and evaluated for their antifungal potential against sugarcane wilt caused by Fusarium sacchari.The isolates of C. globosum showed large variations in colony color, growth rate, colony diameter, ascospore shape, sporulation of F. sacchari time, and ascomata hairs.The most promising CGSR13 strain inhibited colony diameter, spore germination, and sporulation by 66.39, 55.17, and 75.00, resp.The collective sett and soil treatment with CGSR13 showed 60.09 and 46.37% inhibition in wilt (F. sacchari) under greenhouse and field conditions during the 2022-2023 and 2023-2024 crop seasons.Apart from that, soil application and spraying also reduced the disease incidence.Also there was an increase in sett germination (14.49%), fresh shoot weight (6.47%), dry shoot weight (3.09%), FSW/DSW (3.44%), cane diameter (5.77%), fresh root weight (23.62%), dry root weight (44.44%), FRW/DRW (27.09%), internodes length (20.83%), number of internodes (35.52%), cane length (48.90%), and cane weight (68.79%) in CGSR13 treated F. sacchari infected plants than untreated control under field conditions.The liquid chromatog.-mass spectrometry (LC-MS) results showed that the methanolic extract of C. globosum CGSR13 contains plant growth regulator melatonin, cysteine, formononetin, and antagonistic scoulerine and sarsasapogenin.

100 Deals associated with Sarsagenin

External Link

KEGG	Wiki	ATC	Drug Bank
-	Sarsagenin	-	DB05126

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Amyotrophic Lateral Sclerosis	Phase 1	-	Ixico Plc	-
Amyotrophic Lateral Sclerosis	Phase 1	United Kingdom	Phytopharm Plc	-
Glaucoma	Phase 1	United Kingdom	Ixico Plc	-

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