Current Bioactive Compounds - Volume 19, Issue 4, 2023

Background: Herbal medicines have been derived from different parts of the plants including roots, bark, seeds, flowers, and leaf. Human beings have been using herbal medicine and their derived phytochemicals for the treatment of human health complications since ancient times. Presence of different classes of phytochemicals is responsible for different pharmacological activities of herbal drugs and their derived products. Methods: Numerous scientific literature data have been searched to collect all the needed scientific information of the present article. Scientific literature databases such as Google, Google Scholar, Science Direct, and PubMed have been searched in the present work to collect all the scientific information of swertisin. Medicinal importance and pharmacological activities of swertisin have been investigated in the present work through literature data analysis of different scientific research works. Therapeutic benefits of swertisin against cognitive impairment, diabetes, hepatitis B, pain and chromosomal damage have been investigated through literature data analysis of different scientific research works. Results: Literature data analysis of numerous scientific research works revealed the biological potential of swertisin in medicine as it is present in different medicinal plants i.e. Wilbrandia ebracteata, Swertia franchetiana, Swertia mussotii, Enicostemma hyssopifolium, and Iris tectorum. Scientific data analysis revealed the therapeutic effectiveness of swertisin against cognitive impairment, diabetes, hepatitis B, pain and chromosomal damage. Scientific data analysis signified the importance of different analytical techniques for qualitative and quantitative analysis of swertisin in different samples. Conclusion: Present study signified the biological importance and therapeutic benefit of swertisin in medicine.

Psoriasis is an autoimmune skin condition that is also inflammatory and proliferative. Psoriasis is caused by the activation of T-cells and is distinguished by prominent, drab-red, or peach-pink tight patches with silvery scales on the skin. In recent years, there have been some significant advances in the study of the etiology of inflammatory skin diseases such as psoriasis. The nanotechnology-based novel formulation provides a great occasion for enhancing the efficacy and safety of pharmacotherapeutic agents for psoriasis. The benefits of nanotechnological techniques to offer an effective drug concentration in the disease site and nanocarrier as innovative possibilities for drug delivery systems in psoriasis and other inflammatory chronic skin disorder are highlighted in this area. We have explored the mechanisms underlying the pathogenic aspects of psoriasis in this review, as well as phytoconstituents that are naturally occurring substances found in plants with anti-psoriatic properties. Anti-psoriatic action is attributed to phytochemicals that target cytokine signaling pathways. We also discussed the benefits of loading phytoconstituents as drugs in nanocarriers such as liposomes, niosomes, invasomes, phytosomes, transferosomes, and proniosomes for improved topical therapy and delivery of phytoconstituents with a better therapeutic profile and lower toxicity.

Background: A new series of malonic acid-based hydrazide derivatives (BPMPDH, 2HPMPDH, 3HPMPDH, 4HPMPDH, DMPDH) were successfully synthesized by the reaction of malonic ester hydrazide with various aldehydes like salicylaldehyde, benzaldehyde, 4-hydroxy benzaldehyde, 3-hydroxy benzaldehyde and formaldehyde. Objectives: Furthermore, metal complexes of prepared hydrazide derivatives were prepared using metals like Cu⁺², Zn⁺² and Ni⁺² in a mild efficient and convenient method. Methods: Newly synthesized compounds have been described by IR, NMR (¹H & ¹³C), UV/VIS and mass spectrometry. The presence of –C=N- peak at 1600-1700 cm^-1 with the absence of NH2 peak at 3500 cm^-1 in FTIR spectra and chemical change at 11.00-13.00 ppm for –OH protons, even chemical changes varying from 7.00-9.50 ppm for –NH verified synthesis of modern Dihydrazide derivatives. The presence of a C-OH sharp peak at 180-190 ppm, a C=O peak at 160-170 ppm and a C=N peak at 140-150 ppm have shown the development of compounds. The presence of molecular ion peaks at 308 m/z, 340 m/z and 156 m/z, respectively, provides a good indication of the synthesis of the possible Dihydrazide derivatives. Results: Synthesized compounds have also been analyzed for their antioxidant, antibacterial, antifungal, chymotrypsin and tyrosinase inhibition activities. The findings of activities revealed that the 2HPMPDH, 3HPMPDH, 4HPMPDH and their Cu⁺² and Zn⁺² metal complexes showed more successful inhibitions against standard drugs. Conclusion: In addition, structural behavior and metal complexes vs. ligand activity interaction were also discussed in this research, which indicated that the existence of electron-donating groups and transition metals improved the biological activities of the studied compounds.

Background: Nature-based pharmaceuticals are now becoming an integral aspect of toxic-free healthcare therapies. Diosgenin (DN), a unique phyto steroidal sapogenin, seems to be explicitly employed as a core ingredient in countless traditional and patented Chinese medicines owing to its epic multilayered therapeutic treasure. Objective: The prime intent of the current study was to probe the hepato- and nephro- ameliorating the impact of Diosgenin encapsulated chitosan nanoparticles (DN@CS-NPS) on 7,12- dimethylbenz(a)anthracene (DMBA) mediated rat mammary oncogenesis. Methods: A single dosage of DMBA (25 mg/kg body weight) was injected to induce breast cancer. Oral administration of DN (10 mg/kg body weight) and DN@CS-NPS (5 mg/kg body weight) was used to medicate DMBA administered tumor-bearing rats just after the emergence of a tumor. Following the experimental duration, biochemical and histopathological (H&E) analyses have been carried out. Results: Here, we noticed that there is an escalated level of liver and kidney biomarkers, phase-I detoxification enzymes, lipid peroxidative marker, total cholesterol (TC), phospholipids (PL), triglycerides (TG), and free fatty acids (FFA), low-density lipoprotein (LDL), very low-density lipoprotein (VLDL), total lipase (TL) as well as diminished levels of phase – II detoxification enzymes, enzymatic and non-enzymatic antioxidants, high-density lipoprotein (HDL), lipoprotein lipase (LPL) and lecithin acyltransferase (LCAT) in the plasma, liver and kidney tissues of DMBA-induced rats with renal and hepatic histopathological alterations. Conversely, oral treatment of DN@CS-NPS substantially reduced their tiers to near-normal levels. Conclusion: Thus, our observations suggested that DN@CS-NP is an impactful hepato- and nephro- therapeutic agent that might have a significant influence on breast cancer over free DN.

Background: Solidago virgaurea (Asteraceae) has been used for more than 700 years for treating cystitis, chronic nephritis, urolithiasis, rheumatism, and inflammatory diseases. However, the antidiabetic activity of Solidago virgaurea has been rarely studied. Methods: Three extracts of Solidago virgaurea were prepared, and their antidiabetic potentials were evaluated by various cell-free, cell-based, and in vivo studies. Results: We found that the Solidago virgaurea contained multiple bioactive phytochemicals based on the GC-MS analysis. The Solidago virgaurea extracts effectively inhibited the functions of the carbohydrate digestive enzyme (α-glucosidase) and protein tyrosine phosphatase 1B (PTP1B), as well as decreased the amount of advanced glycation end products (AGEs). In the L6 myotubes, the Solidago virgaurea methanolic extract remarkably enhanced the glucose uptake via the upregulation of glucose transporter type 4 (GLUT4). The extract also significantly downregulated the expression of PTP1B. In the streptozotocin-nicotinamide induced diabetic mice, the daily intraperitoneal injection of 100 mg/kg Solidago virgaurea methanolic extract for 24 days, substantially lowered the postprandial blood glucose level with no obvious toxicity. The extract’s anti-hyperglycemic effect was comparable to that of the glibenclamide treatment. Conclusion: Our findings suggested that the Solidago virgaurea extract might have great potential in the prevention and treatment of diabetes.

Background: Coccidiosis is a common infection among birds that is caused by Eimeria spp. (Protozoa, Phylum Apicomplexa). Eimeria is transmitted fecal-orally and replicated in the intestines. Coccidiosis causes economic losses and increases birds’ susceptibility to other diseases. Methods: In this study, the broilers were experimentally infected by Eimeria tenella and then treated with Sulfaclozine and Iberogol. Birds were randomly divided into 5 groups (21 birds each); I: negative control, II: positive control, III: treated by Iberogol, IV: treated by Sulfaclozine, and V: treated by Iberogol+Sulfaclozine. Twenty-one-day-old chickens were infected by 10000 oocysts/ ml/chicken of E. tenella. Treatments were started 1 day after oocyst observation in thirtyday- old chickens. Treatments continued for 3 days, stopped for 2 days, and again continued for the next 2 days. Results: The results were compared for OPG (oocyst per gram), AW (average weight), FCR (feed conversion ratio), and mortality rate among different groups. According to statistical analysis, the worst results were observed in the Iberogol group (III) among other treatment groups (IV and V), and the most effective treatment was reported in the Iberogol+Sulfaclozine group (V). Conclusion: Complex herbal medications, such as Iberogol, can have different activities, but in coccidiosis, its antioxidant and anti-inflammatory effects are more than the anticoccidial effect. Therefore, Iberogol can be used with Sulfaclozine to increase its efficiency.

Aim: The present study aimed to investigate the bioavailability of curcumin conjugated with isoleucine. Background: Curcumin has various health beneficiary properties; however, it is poorly bioavailable because of its insolubility in water, poor absorption and quick systemic elimination. Hence, any approach that could improve bioavailability is necessary. Objective: The objective of the present study is to examine whether the bioavailability and biodistribution of curcumin is improved upon derivatisation with isoleucine than that of native curcumin. Methods: About 0.1 g/kg bw of curcumin and its isoleucine-derivative were administered to fasting rats. Then the blood and tissue samples were collected at different time intervals (0, 1800, 3600, 7200, 14400, 28800, 43200, 86400, and 172800 seconds) and processed for the extraction of curcumin and its derivative with methanol. The processed samples were subjected to HPLC analysis and compared with the standard curcumin and its derivative. The results were analysed using the software, PKSolver, for determining the bioavailability and biodistribution. Further, the docking studies were carried out to better understand the results obtained. Results: We found that isoleucine-curcumin conjugates have better bioavailable in plasma, ovary and uterus in the experimental rats. The curcumin and its isoleucine-derivative was detected to be maximum at 14400 seconds. However, the concentration of isoleucine-derivative of curcumin was significantly high at Tmax compared to native curcumin. Further, curcumin and its derivative were found in the reproductive organs only at 28800 seconds, 43200 seconds and 86400 seconds. The binding energy of isoleucine-derivative of curcumin with p-glycoprotein transporter was found to be more compared to the native form. This may be the reason for the increased bioavailability of isoleucine-derivative of curcumin. Conclusion: The isoleucine-curcumin conjugate has better bioavailability compared to curcumin both in plasma and reproductive organs.

Psoriasis is a multifaceted inflammatory dermatological skin disease characterized by Tcell (T-lymphocyte) activation, hyperproliferation, and abnormal epidermal keratinocyte differentiation. Natural bioactive agents from plants including Psoralea corylifolia, Nigella sativa, Curcuma longa, Capsicum annum, Smilax china, Woodfordia fructicosa, and others have recently gained a lot of attention for their anti-psoriatic properties. However, inadequate drug absorption, lack of specificity in drug release, and unintended skin reactions largely restrict their clinical efficacy. Nanoformulations improve the pharmacodynamic characteristics that overcome drug delivery challenges and enhance the anti-psoriatic activity. Nanostructured systems such as liposome, ethosome, liposphere, and others have been reported to improve plant extract solubility, penetration, bioavailability, bioactivity, and minimize undesirable effects, providing the way for the development of herbal nanoformulation. This review enlights the therapeutic efficacy of lead phytocompounds and its nanoformulations in managing psoriasis.