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Flavopiridol, a synthetic flavonoid derived from rohitukine, stands out as a powerful cyclin-dependent kinase (CDK) inhibitor with significant anticancer properties. Its action mechanisms involve inducing cell cycle arrest, triggering apoptosis, and inhibiting transcription across various cancer types. Despite these promising effects, flavopiridol's clinical use has been hampered by issues related to toxicity and drug resistance. This study aims to comprehensively review flavopiridol's mechanisms of action, structure-activity relationships, synthetic derivatives, pharmacokinetics, and its potential role in clinical applications, with a focus on how combination therapies can enhance its efficacy and address resistance challenges in cancer treatment. A thorough analysis of key studies was performed, examining flavopiridol's anticancer properties, emphasizing its structure-activity relationships, synthetic modifications, and clinical outcomes. The anticancer effects of flavopiridol are primarily driven by its inhibition of CDKs, induction of apoptosis, promotion of oxidative stress, and antiangiogenic activity. Modifications in its chemical structure, especially in the D ring, have shown a significant impact on its CDK inhibitory potency. Several synthetic derivatives have also demonstrated enhanced anticancer activity. While preclinical models highlight flavopiridol's potential in treating cancers such as leukemia and solid tumors, clinical trials have brought attention to its limitations, particularly regarding toxicity and resistance. However, flavopiridol remains a promising candidate for cancer therapy, especially when used in combination with other treatments. Future research efforts should focus on refining its therapeutic profile, minimizing toxicity, and investigating synergistic treatment combinations, including those with immunotherapy. Understanding the mechanisms of resistance and discovering predictive biomarkers will be crucial for its effective integration into clinical practice., Competing Interests: Declarations. Ethics approval and consent to participate: Not applicable. Consent for publication: Not applicable. Competing interests: The authors declare no competing interests., (© 2024. The Author(s), under exclusive licence to Springer-Verlag GmbH Germany, part of Springer Nature.)

Background: Myrica esculenta is a notable therapeutic plant widely utilized in Indian system of medicine. Ayurvedic literature reported fruit and bark of this plant is used in gulma, jvara, arsa, grahani, pandu roga, hrillasa, mukha roga, kasa, svasa, agnimandhya, aruchi, meha, and kantharoga., Objective: The present study aimed to investigate the neuroprotective potential of "Himalayan Bayberry" (Myrica esculenta Buch.-Ham. ex D. Don) leaves methanol extract in Parkinson's disease induced by haloperidol., Materials and Methods: The present investigation was completed in wistar rats, in which Parkinson's disease (PD) was induced with haloperidol 1 mg/kg, intraperitoneally. The rats were randomly divided into six gatherings and the test animals received the methanolic extract of M. esculenta (MEME) at a dose of 50, 100 and 200 mg/kg, orally for one week. Various behavioural, biochemical and histopathological parameters were estimated in haloperidol exposed rats., Results: MEME demonstrated significant and dose-dependent increment in behavioural activity and improved muscle coordination. The significant diminution in malonaldehyde level while improved the level of antioxidant enzymes like catalase, superoxide dismutase and reduced glutathione in extract treated group were observed as compared to the control group. Histopathological changes revealed MEME significantly reduced haloperidol-induced damage in the substantia nigra and there was very little neuronal atrophy., Conclusion: The outcomes showed the defensive role of M. esculenta against PD. The mechanism of protection may be due to an escalation of cellular antioxidants., Competing Interests: Conflict of interest None, (Copyright © 2020 The Authors. Published by Elsevier B.V. All rights reserved.)

Background: Osteoarthritis (OA) ranks fifth among all forms of disability affecting 10% of the world population. Current treatments available are associated with multiple side effects and do not slow down the progression of the disease. Moreover, no such effective treatment is available to date in various systems of medicine to treat osteoarthritis. Curcumin and Arnica have shown evident clinical advances in the treatment of osteoarthritis., Objective: The aim of the present study was to design, optimize and characterize novel herbal transdermal patches of curcumin and Arnica montana using factorial design., Methods: A multiple factorial design was employed to investigate the effect of hydroxypropyl methyl cellulose, ethyl cellulose and jojoba oil on elongation and drug release. Transdermal patches were evaluated by FTIR, DSC, FESEM, ex vivo drug permeation, anti osteoarthritic activity and analgesic activity., Results: Independent variables exhibited a significant effect on the physicochemical properties of the prepared formulations. The higher values of drug release and elongation were observed with the higher concentration of hydroxypropyl methylcellulose and jojoba oil. Anti osteoarthritic activity was assessed by complete Freund's adjuvant arthritis model; using rats and analgesic activity by Eddy's hot plate method, using mice. Combination patch exhibited good anti osteoarthritic and analgesic activity as compare to individual drug patches., Conclusion: The design results revealed that the combination patch exhibited good physicochemical, anti osteoarthritic and analgesic activity for the treatment of osteoarthritis in animals. More plants and their combinations should be explored to get reliable, safe and effective formulations that can compete with synthetic drugs., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Background : Plant diversity is a basic source of food and medicine for local Himalayan communities. The current study was designed to assess the effect of different solvents (methanol, ethyl acetate, and water) on the phenolic profile, and the corresponding biological activity was studied. Methods : Antioxidant activity was investigated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2″-azino-bis(3-ethylbenzothiazoline-6-sulphonic) acid (ABTS) assay, while the antimicrobial activity was evaluated by disk diffusion method using various bacterial and fungal strains. Results : The outcomes demonstrated that methanol acted as the most effective solvent for polyphenols extraction, as strengthened by the liquid chromatography and mass spectroscopy (LC-MS) and fourier transform infrared spectroscopy (FTIR) analysis. M. esculenta methanol extract showed the highest DPPH and ABTS radical scavenger antioxidant activity with IC 50 values of 39.29 μg/mL and 52.83 μg/mL, respectively, while the ethyl acetate and aqueous extracts revealed minimum antioxidant potential. Methanol extract also revealed higher phenolic content, 88.94±0.24 mg of equivalent gallic acid (GAE)/g), measured by the Folin-Ciocalteu method, while the minimum content was recorded for aqueous extract (62.38±0.14 GAE/g). The highest flavonoid content was observed for methanol extract, 67.44±0.14 mg quercetin equivalent (QE)/g) measured by an aluminum chloride colorimetric method, while the lowest content was recorded for aqueous extract (35.77±0.14 QE/g). Antimicrobial activity findings also reveal that the methanol extract led to a higher inhibition zone against bacterial and fungal strains. FTIR analysis reveals the presence of various functional groups, viz. alkenes, amines, carboxylic acids, amides, esters, alcohols, phenols, ketones, carboxylic acids, and aromatic compounds. This FTIR analysis could serve as a basis for the authentication of M. esculenta extracts for future industrial applications. Compounds identified by LC-MS analysis were gallic acid, myricanol, myricanone, epigallocatechin 3- O -gallate, β -sitosterol, quercetin, p -coumaric acid, palmitic acid, n -pentadecanol, n -octadecanol, stigmasterol, oleanolic acid, n -hexadecanol, cis - β -caryophyllene, lupeol, and myresculoside. Conclusion: This study suggests that the methanolic extract from M. esculenta leaves has strong antioxidant potential and could be a significant source of natural antioxidants and antimicrobials for functional foods formulation., Competing Interests: The authors declare no conflict of interest.

Myrica esculenta (Myricaceae) is a popular medicinal plant most commonly found in the sub-tropical Himalayas. It is widely used in folk medicine to treat several ailments such as asthma, cough, chronic bronchitis, ulcers, inflammation, anemia, fever, diarrhea, and ear, nose, and throat disorders. Due to its multidimensional pharmacological and therapeutic effects, it is well recognized in the ayurvedic pharmacopeia. However, the recent upsurge in M. esculenta use and demand has led to illicit harvesting by the horticultural trade and habitat loss, pushing the plant to the brink of extinction. Thus, the present review aims to provide updated information on M. esculenta botany, ethnomedicinal uses, phytochemistry, pharmacological effects, toxicity, and conservation methods, as well as also highlight prospective for future research. Particular emphasis is also given to its antioxidant potential in health promotion. In-depth literature was probed by searching several sources via online databases, texts, websites, and thesis. About 57 compounds were isolated and identified from M. esculenta, and the available reports on physicochemical parameters, nutritional and high-performance thin-layer chromatography analysis of bioactive plant parts are portrayed in a comparative manner. Friendly holistic conservation approaches offered by plant biotechnology applications, such as micropropagation, germplasm preservation, synthetic seed production, and hairy root technologies are also discussed. Nonetheless, further studies are needed to propose the mechanistic role of crude extracts and other bioactives, and even to explore the structure-function relationship of active components., Competing Interests: The following abbreviations are used in this manuscript:

Background: Myrica esculenta (Family: Myricaceae) commonly known as Kaiphala or Katphala is a widely used medicinal plant in Ayurveda. In spite of its numerous medicinal attributes, no published work is available till date on pharmacognostical characterization and HPTLC analysis of its leaves., Objectives: To investigate the pharmacognostical, physicochemical, and HPTLC profiles of M. esculenta leaves., Materials and Methods: The measures taken for pharmacognostical characterization were organoleptic study, macroscopy, microscopy, powder microscopy, leaf constant, fluorescence analysis, preliminary phytochemical screening and HPTLC spectra profile., Results: Organoleptic and macroscopic studies found that leaves are lancoelate, thin, spirally arranged, dark green in color, with an astringent taste and acute apex. In transverse section, cuticularised epidermis having polygonal cells were found. Mesophyll cells were differentiated into single layered palisade cells on each surface and 2-3 layered spongy parenchyma, unicellular and uniseriate hollow trichomes, anomocytic stomata and bowl shaped vascular bundle in mid rib portion containing xylem and phloem tissues. Alkaloids, carbohydrates, flavonoids, glycosides, phenolic compounds and tannins were found present. Analysis on the leaf constants, powder microscopy, fluorescence characteristics and physical parameters resulted a valuable data to establish standards for the plant. HPTLC profile provides number of constituents present in the extracts with their respective Retention Factor (R f )., Conclusion: Present report on pharmacognostical characterization and HPTLC analysis of M. esculenta leaves provides a vital diagnostic tool for identification, authentication and development of quality parameters of the species. Data obtained by present study may be considered as standard for future studies., (Copyright © 2017 Transdisciplinary University, Bangalore and World Ayurveda Foundation. Published by Elsevier B.V. All rights reserved.)

Parkinson's disease (PD) is standout amongst the most common neurodegenerative malady with unpredictable dynamic pathology. At present, accessible traditional choices for PD have certain impediments of their own, and subsequently persistent consistence and fulfillment are low. Current contemporary treatment options just give symptomatic alleviation constrained control to anticipate malady progression, bringing about poor patient consistence and fulfilment. Numerous rising pharmacotherapies for PD are in various phases of medical improvement. Treatments incorporate adenosine A2A receptor antagonists, anti-apoptotic agents, monoamine oxidase inhibitors, glutamate receptor antagonists, and antioxidants for example, N-acetyl cysteine, edaravone, and coenzyme Q10. Other rising nonpharmacotherapies incorporate microRNAs, viral vector gene therapy, stem cells transglutaminases, RTP801, and glial derived neurotrophic factor (GDNF). Furthermore, surgeries including profound pallidotomy, deep brain stimulation, thalamotomy and gamma knife surgery have developed as elective mediations for cutting edge PD patients who have totally used common medications and still suffer from unrelenting motor symptoms. Complementary and Alternative medicine (CAM) modalities, such as Yoga, acupuncture, Tai Chi, Music therapies are highly practiced in several countries, offer some of the safer and effective treatment modalities for PD. While a few of these treatments hold much assurance in postponing the beginning of ailment and moderating its progression, more pharmacotherapies and careful mediations should be examined in various phases of PD. Therefore, the main objective of our review is to fill the gap between the researches and provide updated and productive information about the research reported in the last couple of years and can fulfil the most reassuring plausibility for encourage treatment of Parkinson Disease., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.)

Background: Melaleuca alternifolia (Myrtaceae) is a well-known, commonly used, tall shrub plant in Ayurvedic medicine. Traditionally, it is used for its antimicrobial potential to treat cutaneous infections. No attempts have been made regarding pharmacognostic investigation of the plant till date. So, the present study was aimed to establish standards with the help of different pharmacognostic parameters., Methods: Various pharmacognostic parameters (morphological, microscopic, physicochemical evaluations and preliminary phytochemical screening) were studied along with fluorescent and thin layer chromatographic analysis of the extract., Result: Morphologically Melaleuca alternifolia is a shrub having height of 7 m with layered and papery bark. Leaves have an arranged pattern, petiole is 1 mm in length; linear-acute with dimensions of 10-35 mm x 1 mm. Organoleptic features shows that leaves have characteristic odour and astringent taste. The transverse section of the leaf reveals the existence of epidermal layers, mesophyll tissues, vascular bundles and secretory cavities. The stomata are anomocytic and leaf constants such as stomatal number is 180-200-225, stomatal index is 3.8-4.4-5.9, vein islet number is 18.68 (average), veinlet termination number 20.3 (average) and palisade ratio is 5.5-6.4-6.9. The results of phytochemical screening showed the occurrence of different phytoconstituents (flavonoids, phenolic tannins, phytosterol and terpenoids)., Conclusion: The present study evaluated various pharmacognostic parameters which will help in quality control (standardization) of Melaleuca alternifolia leaves in crude form, in herbal formulation and also aid in the preparation of an herbal monograph for the species.

Background: Anogeissus pendula has various reported ethnomedicinal uses and is reported to contain phenolic compounds which have antioxidant potential., Aim: The present study was undertaken to evaluate the in vitro antioxidant potential and in vivo hepatoprotective activity along with the oxidative stress parameters of stem bark and leaves of Anogeissus pendula for the first time., Settings and Design: Albino rats were divided into seven groups of six animals each. Healthy control (Group I) and toxic control (Group II) received the vehicle. Group III, IV, V, VI and VII were treated with silymarin (100 mg/kg body weight, orally) and two hydro-alcoholic extracts i.e., APB (stem bark) and APL (leaves) at doses of 200 and 400 mg/kg b. w., orally, respectively. Hepatotoxicity was induced by allyl alcohol., Materials and Methods: Albino Wistar rats of either sex between 8-12 weeks old were used. The plant parts were collected from Sawai Madhopur (Rajasthan, India) and extracted with hydro-alcoholic solvent to get two extracts i.e., APB (stem bark) and APL (leaves) which were investigated for the in vitro antioxidant potential through DPPH radical and H 2 O 2 scavenging assay along with in vivo hepatoprotective potential through allyl alcohol induced hepatotoxicity., Statistical Analysis: Statistical comparisons between different groups were done by using one-way ANOVA followed by the Bonferroni test. P < 0.05 was considered significant., Results and Conclusions: APB showed more potent activity than APL in case of in vitro antioxidant potential with IC 50 of 44.29 μg/ml in DPPH radical scavenging activity and 53.09 μg/ml in hydrogen peroxide scavenging assay. Both the extracts revealed antioxidant and hepatoprotective potentials in a dose dependent manner but more significant results were obtained in case of APB at 400 mg/kg. More amounts of phytoconstituents might be the reason behind the more significant activity of extract of stem bark than that of the leaves., Competing Interests: There are no conflicts of interest.

Ethnopharmacological Relevance: The genus Anogeissus (axlewood tree, ghatti tree, button tree and chewing stick tree) belongs to Combretaceae, includes eight species that are distributed in Asia and Africa. Plants are used as an ethnomedicine in Asia and Africa to treat various ailments like diabetes, fever, diarrhoea, dysentery, tuberculosis, wound healing, skin diseases (eczema, psoriasis), snake and scorpion venom. Based on the traditional knowledge, different phytochemical and pharmacological activities have been at the focus of research. The aim of this review is to provide updated, comprehensive and categorized information on the ethnobotany, phytochemistry, pharmacological research and toxicity of Anogeissus species in order to identify their therapeutic potential and directs future research opportunities., Materials and Methods: The relevant data was searched by using the keyword "Anogeissus" in "Scopus", "Google Scholar", "Web of Science", "PubMed", and "ScienceDirect" databases. Plant taxonomy was validated by the databases "The Plant List" and A.J. Scott, 1979., Results: This review discusses the current knowledge of the ethnobotany, phytochemistry and in vitro as well as in vivo pharmacological evaluations carried out on the extracts and isolated main active constituents of Anogeissus genus. Among eight species, most of the phytochemical and pharmacological studies were performed on four species. About 55 secondary metabolites are isolated from the genus. Stem bark, leaf, seed, fruit, root of the plants are used for the treatment of several health disorders such as diabetes, fever, diarrhoea, dysentery, tuberculosis, wound healing, skin diseases (eczema, psoriasis), snake and scorpion venom. Gum ghatti obtained from Anogeissus latifolia is used after delivery as tonic and in spermatorrhoea. Many phytochemical investigations on this genus confirmed that it is rich in phenolic compounds. Modern pharmacology research has confirmed that the crude extracts or the isolated active compounds of the genus Anogeissus possess antioxidant, antimicrobial, wound healing, antiulcer, anti-inflammation, anti-diabetics, hepatoprotective, hypolipidemic, antiparasitic and neuroprotective effects., Conclusions: This review confirms that some Anogeissus species have emerged as a good source of the traditional medicine for wound healing, inflammation, skin diseases, microbial infection and diabetes. Many traditional uses of Anogeissus species have now been validated by modern pharmacology research. Intensive investigations of all the species of Anogeissus regarding phytochemical and pharmacological properties, especially their mechanism of action, safety and efficacy could be the future research interests before starting clinical trials., (Copyright © 2016 Elsevier Ireland Ltd. All rights reserved.)

Drug-polymer miscibility is one of the fundamental prerequisite for the successful design and development of amorphous solid dispersion formulation. The purpose of the present work is to provide an example of the theoretical estimation of drug-polymer miscibility and solubility on the basis of Flory-Huggins (F-H) theory and experimental validation of the phase diagram. The F-H interaction parameter, χ d-p, of model system, aceclofenac and Soluplus, was estimated by two methods: by melting point depression of drug in presence of different polymer fractions and by Hildebrand and Scott solubility parameter calculations. The simplified relationship between the F-H interaction parameter and temperature was established. This enabled us to generate free energy of mixing (ΔG mix) curves for varying drug-polymer compositions at different temperatures and finally the spinodal curve. The predicted behavior of the binary system was evaluated through X-ray diffraction, differential scanning calorimetry, and in vitro dissolution studies. The results suggest possibility of employing interaction parameter as preliminary tool for the estimation of drug-polymer miscibility.

In the present study an efficient strategy for the synthesis of thiazole and thiadiazole derivatives was developed and clubbed together both of the substituted nucleus to form the analogues of combretastatin A-4 (tubulin polymerization inhibitors.). Synthesis was started by the reaction of substituted benzoic acid with thionyl chloride followed by the reaction with hydrazine, p-chloro benzaldehyde and thioglycolic acid to form substituted thiazole derivatives. On the other side hydrazides were reacted with ammonium thiocyanate and strong acid to form substituted thiadiazole compounds. Finally thiazole and thiadiazole compounds were clubbed with the help of dioxan and triethylamine. All novel derivatives (TH01-TH40) were screened for their cytotoxicity activity using MTT assay against three cancer cell lines viz. A-549 (lung carcinoma), HT-29 (colon carcinoma), HeLa (cervix carcinoma). Compounds TH08 exhibited highest activity, due to the presence of trimethoxy substitution on phenyl ring. In QSAR study these results were correlated with physicochemical parameters and the correlation of XlogP, kaapa2, Quadrupole1 with cytotoxic activity on A-549 (lung carcinoma) was found highest (r2: 0.941; F: 99.103; Se: 0.0006). In docking study binding of active molecule (TH08) was found very well with α, β tubulin (PDB: 1SA0) protein.

A selective and sensitive, stability-indicating reverse phase high performance liquid chromatography method has been first developed and validated for the estimation of miglitol in bulk and tablet dosages form. Samples were separated on a prepacked, Inertsil amino C(18) column (150×4.6 mm i.d.) using a mobile phase comprised of acetonitrile and monobasic sodium phosphate pH 7.5 (80:20, v/v) delivered at 1.5 ml/min flow rate. Detection was performed on a SPD-20A prominence UV/Vis detector at 220 nm. The retention time for miglitol was 13.93±0.0367. The method was validated in terms of linearity, precision, accuracy, ruggedness, and specificity, limit of detection and limit of quantification. The linearity (r(2)) and percentage recoveries of miglitol were 0.9986 and 99.85%. This method is suitable for routine estimation of miglitol in bulk and tablet dosages form.