Current Topics in Medicinal Chemistry - Volume 21, Issue 20, 2021

Herbal remedies have been employed for the treatment and management of different diseases for ages. Herbal medicines are a promising choice over modern synthetic drugs because of their low side effects and are thus considered to be safe and effective in treating human diseases. Lagenaria siceraria (Mol.) Standley fruit (Bottle gourd) belongs to the Cucurbitaceae family that has been used in a different system of traditional medication to treat various diseases. This is a domestic plant that provides food as well as medication. This vegetable have low caloric values and high water contents. The edible portion of it contains phytochemicals like vitamins, proteins, choline, minerals, terpenoids, flavonoids, etc. Several bioactive compounds have been isolated from L. siceraria, including triterpenoids, sterols, cucurbitacins, flavones, C-glycosides and β-glycosides. Researchers have evaluated various parts of this plant viz. fruit, root, flowers, and leaves for pharmacological activities like antianxiety, antidepressant, diuretic, antimicrobial, cytotoxic, antihyperlipidemic, cardio protective, analgesic, anti-inflammatory, anthelmintic, anti-hyperglycemic, antihepatotoxic, anti-urolithiatic, antistress, antiulcer, anticancer, hepatoprotective, anthelmintic, immunomodulatory, and antioxidant. In this review, an attempt has been made to explore its phytochemical constituents, traditional, medicinal, and pharmacological uses to highlight the therapeutic importance of this well-known plant. This would be helpful in reviving its importance and will highlight its several promising aspects to encourage researchers for further research on L. siceraria.

Eugenol is a bioactive compound widely available in many herbs like clove, cinnamon, tulsi, pepper etc. The compound is known for its antioxidant, antimicrobial, anesthetic, anti-inflammatory, neuroprotective, anti-diabetic, and anti-cancer activities. In pharmaceutical analysis, eugenol is used as a marker for single drugs and drug products. Dental care, household, and personal hygiene products are other areas where it has established its potential. In the food industry, eugenol is used as a flavouring agent in non-alcoholic beverages, baked foods, and chewing gums. Considering the huge potential of eugenol, this review is an attempt to collate the regulatory information, physico-chemical properties, toxicity profile, marketed conventional and novel formulations, analytical methods, extraction procedures, recent patents and clinical trials of the moiety. Based on literature survey a schematic diagram of mechanism of action has also been made.

Background: The phosphatidyl inositol-3 kinase (PI3K)/protein kinase B (Akt)/mechanistic target of rapamycin (mTOR) signaling has been associated with many cellular physiological events, such as proliferation, maturation, survival, and metabolism. Besides its role in normal cells, the pathway is often upregulated in various cancers. Due to its prominent role in the cancer progression events, it is now being considered as a target for cancer therapy and cancer chemoprevention. Objectives: The present review provides a concise outline of the role of the PI3K/Akt/mTOR pathway in carcinogenesis and progression events, including metastasis, drug resistance and stemness. Further, emphasis needs to be placed on the PI3K/Akt/mTOR pathway inhibitory potentials of various food-derived bioactive components in cancer prevention. Methods: Data on the PI3K/Akt/mTOR inhibiting natural products and their bioactive compounds have been obtained from PubMed/Medline, Scopus, Eurekaselect, etc. Findings from the above citation databases from 2000-2021 are included in the manuscript. Results: Numerous compounds from plants have been isolated and identified as anticancer agents; among these, a predominant class is nutraceuticals. The PI3K pathway is the predominant target of these natural products, and many of these drug candidates are under various stages of drug development. These compounds have shown a significant inhibitory effect on the kinase activities of PI3K and Akt, resulting in the abrogation of cancer initiation and progression events. In addition, these compounds have been shown to reverse the resistance to chemotherapeutic drugs and also reduce the population of cancer stem cells. Conclusion: The nutraceuticals are promising candidates as anticancer agents by blocking PI3K signaling cascades. As the PI3K is a central pathway to various receptors signaling, the dietary intervention may prove to be highly effective.

Background: Today, the occurrence and recurrence of multidrug-resistant tuberculosis strains and comorbidities are the main reasons for long-term morbidity and mortality from tuberculosis from the nasty acid-fast pathogen Mycobacterium tuberculosis. Therefore, discovering and developing well-tolerated and non-toxic antituberculosis regimens are directly needed to defend the variants strains of M. tuberculosis and, alternatively, support WHO’s ‘END-TB’ campaign. Objective: Alternatively, phytochemicals from various common and medicinal plants have always been vital therapeutic agents since the primitive era. Thus, proper scientific documentation as diversity, potency, structure, drug-chemistry and overall critical analysis are essential tools to accelerate the phytochemical-based anti-TB drug development. Methods: In the present review, we have used some specific keywords such as ‘antituberculosis phytochemicals’, &; antituberculosis phytochemicals from plant source&; ‘natural products against tuberculosis’ in Google, PubMed, ScienceDirect sites to get more appropriate research publications. Further, based on lower minimum inhibitory concentration within fifty μ g/mL, a total of twohundred- twenty-one bioactive anti-TB phytochemicals were selected for critical drug-chemistry and structural activity relationship analyses to select most potential ‘lead candidate’ for anti-TB drug development. Results: Based on lower concentration, abietane, ethyl-p-methoxycinnamate, ergosterol peroxide, mono-O-methyl curcumin isoxazole, 7-methyljuglone, 12-demethylmulticaulin, 12-methyl-5- dehydroacetylhorminone, tryptanthrin, etc. are some of the potential anti-TB phytochemicals. Interestingly, existing and clinical drug pipelines for TB contain several active phytochemical pharmacophores illustrated from the structural analysis. Conclusion: Therefore, updated experimental documentation and structural-cum-critical drugchemistry analysis on isolated antituberculosis phytochemicals at the primary level are more beneficial for drug developers, R&D centres, and pharmaceutical companies to accelerate anti-TB drug development using phytochemicals.