Active Chemical Constituents Research Articles

Carica papaya L. Latex Mediated Green Synthesis of Zno Nanoparticles for its Antimicrobial Activity

Zinc oxide nanoparticles have gained potential recognition because of their distinctive characteristics and wide utilizatrion in various fields. Therefore, development of novel biological techniques is significant for the biosynthesis of ZnO nanoparticles using the latex of Carica papaya L. Plant latex is a natural product produced by a number of plant species which are used by different tribal communities in India as a folk medicinal treatment on natural wounds or cuts. Plant latex has a huge demand as herbal products in an aspect of clinical, therapeutical and also in agricultural sectors. Natural latex is composed of different important biomolecules like, tannins, flavonoids, glycosides, sterols, saponins etc. These different active chemical constituents have versatile medicinal activities against different pathogens such as bacteria, fungi, viruses and protozoans etc. This study reports on the biosynthesis of ZnO nanoparticles (Zn NPs)using latex of C. papaya as an effective reducing agent. Green synthesis of nanoparticles has advantageous over conventional methodsbecause it does not require the use of toxic chemicals and therefore environmentally sustainable. The elemental composition of C. papaya latex was also analysed using X-ray Fluorescence (XRF) technique. Properties of synthesized ZnO NPs were characterized using various methods such as ultra violet visible spectrophotometer (UV-Vis), scanning electron microscopy and Fourier transform infrared spectroscopy. Green synthesized ZnO nanoparticles also assessed for its antimicrobial activity against selected bacterial and fungal species.

Ethnopharmacology and current conservational status of Cordyceps sinensis.

Cordyceps sinensis, known as the caterpillar fungus, constitutes an invaluable and irreplaceable part of traditional Chinese medicine (TCM) and is now gaining widespread global recognition and dedicated attention owing to both highly promising characteristics as well as grave dangers that are suggestive of an impending doom. C.sinensis possibly holds the key to the treatment of many human ailments with minimal side effects due to a wide array of biologically active chemical constituents. The powerful potential harbored by this fungus has led to a meteoric rise in its prices in the domestic and international markets which has caused the involvement of an increasing number of harvesters, traders, and buyers and unchecked overexploitation of this bioresource thus threatening its long-term survival in its natural habitat of the Himalayan region. This review focuses on the ethnopharmacology of C.sinensis, and various aspects related to its conservation, such as natural distribution, sale and revenue, decline in population density, and conservational practices prevalent in the current scenario of fungal depletion. The paper concludes with a comprehensive evaluation of the discrete therapeutic capabilities possessed by C.sinensis, the mechanistic insights into the remarkable treatment of chronic ailments using the fungus or its derivatives, and a suggested strategic roadmap that may be adopted for fruitful conservation of this natural miracle.

Exploratory research on the effective chemical basis of tanreqing injection for treating acute lung injury: In vivo, in vitro and in silico

Ethnopharmacological relevanceSepsis-induced acute lung injury (ALI) presents with significant morbidity and mortality in clinical settings. Tanreqing Injection (TRQI) has been clinically recommended for the treatment of ALI; however, the specific active chemical constituents remain unidentified. Aim of the studyThis study aimed to elucidate the potential pharmacologically active components and the underlying mechanisms of TRQI in the treatment of sepsis-induced ALI. Materials and methodsHigh-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) techniques were employed to identify the effective chemical constituents of TRQI. Additionally, an in vitro study was conducted using Raw264.7 macrophage cells stimulated with lipopolysaccharide (LPS) to evaluate the inhibitory effects of TRQI. An acute lung injury model produced by LPS was intraperitoneal injection in mice to assess the ALI-inhibitory effect of TRQI. The lung's pathological characteristics were examined using hematoxylin and eosin staining. Enzyme-linked immunosorbent assay (ELISA) and QPCR were performed to confirm the pharmaceutical effect. Network pharmacology was employed for mechanistic exploration, incorporating GO, and PPI analyses of targets. Src inhibitor and JNK agonist used to investigate the dependence of associated signaling pathways. ResultsCombining pharmacokinetic characteristics, lung first-pass effect and anti-inflammatory effects, the main components of TRQI for treating sepsis induced ALI were narrowed down to seven compounds: chlorogenic acid, scutellarin, wogonoside, oroxyloside, oroxylin A and baicalein. Network pharmacology indicated that Src/JNK signaling pathway, may be the main regulatory pathway for treatment of actue lung injury. Next by using Src inhibitor, Src inhibition partly diminished the protective effects of TRQI in LPS-injected mice. Pretreatment with JNK agonist anisomycin abolished the protective effects of lung injury in vivo. ConclusionsTRQI is injected, the seven compounds could be presented in vivo, which can improve ALI by inhibiting Src-JNK signaling.

Study on the mechanism of ischemic stroke treatment based on network pharmacology and Raman spectroscopy in the larval zebrafish model, Calculus Bovis as a case

Calculus Bovis (C. bovis) is a precious traditional Chinese medicine of animal origin, and it is one of the traditional medicines for treating cerebral inflammatory diseases such as stroke. However, the pharmacological action of C. bovis on ischemic stroke (IS) and its mechanism are still unclear. The purpose of this study was to investigate the potential mechanism to treat IS. Chemical constituents of different varieties of C. bovis were analyzed and confirmed by HPLC-MS/MS technique. We constructed a component and corresponding target network and drug-disease target protein–protein interaction (PPI) network. GO and KEGG enrichment analysis were performed. The molecular docking of the main compound with the target protein. Subsequently, the potential mechanism of therapy for IS was verified in vivo by zebrafish model. We introduced Raman spectroscopy to detect changes in the biochemical composition of zebrafish. 13 active chemical constituents and 129 potential targets were selected. 122 KEGG signaling pathways were obtained. The binding energy of the main compounds is less than −4.5. The results of animal experiments showed that C. bovis could significantly improve Ponatinib-induced IS, decrease the aggregation degree of brain macrophages, reduce the number of macrophage migrations, and significantly increase the expression level of NR3C1. Raman information indicated that the biochemical composition in the brain of the Ponatinib-induced group shifted to the control group. The mechanism may be related to anti-inflammatory process and regulation of lipid metabolism. This study demonstrates that Raman spectroscopy has great potential as a drug evaluation tool in living larval zebrafish.

Alleviation of favipiravir-induced hepatotoxicity using hepatoprotective herbal extracts in wistar rats

Teratogenicity and hyperuricaemia are the main side effects of favipiravir, an antiviral drug recently found its use to treat mild to moderate coronavirus (COVID-19) infections. This study investigated the beneficial effect of herbal extracts like Picrorrhiza kurroa (PK) and Scutellaria baicalensis (SB) and their active chemical constituents (baicalin and baicalein) on favipiravir-induced hepatotoxicity in rats. The formulation combinations included favipiravir, favipiravir + PK extract, favipiravir + pure baicalin, favipiravir + pure baicalein, and favipiravir + SB extract designated as F1, F2, F3, F4 and F5 respectively that were administered to rats orally for 21 days. Favipiravir caused increased levels of SGOT, SGPT, ALP, total bilirubin, and uric acid and decreased liver weight which was alleviated when alloherbal formulation of favipiravir and baicalein combination and favipiravir and SB extract was used. This paper highlights an attractive proposition to ameliorate favipiravir-induced hepatotoxicity using hepatoprotective agents.

The Potential of Grape Polyphenols Additive in Pig Nutrition: Chemical Structure, Bioavailability and Their Effect on Intestinal Health of Pigs

The recognition of the necessity for employing natural additives in animal feed has grown alongside the ban on antibiotics in the animal feed sector. Grapes, as well as by-products of the wine-making industry (grape marc and seed extracts), possess biologically active chemical constituents that can be used to improve animal production by incorporating them into animal feed. Grapes are a valuable resource of polyphenols, especially flavonoids, stilbenes and phenolic acids, most of them showing therapeutic or health-promoting properties. The purpose of this review is to elucidate the impact of polyphenols on animal gut health. The first section of the review discusses the chemical structure of the major polyphenols in grapes and the polyphenols’ bioavailability and metabolism in pigs. The second and major part of the review reviews the results of investigations into the antioxidant, antimicrobial and prebiotic effects of grape polyphenols in pig diets, as well as their regulation of intestinal barrier functions through signalling pathways and intestinal responses. All of this is supported by previous research, findings and conclusions. There are fewer recorded pig studies, but the inclusion of up to 9% grape by-products resulted in improved performance with an increased mean daily gain. Ultimately, this analysis concluded that supplementation of pigs with grape phenolic compounds as natural feed additives enhanced their antioxidant capacity, improved humoral and cellular immune responses, and promoted gut ecosystem biodiversity and the overall production performance in pigs.

Headspace analysis of volatiles from commercial seeds of Trigonella foenum-graecum L. obtained from four Middle Eastern countries

ABSTRACT Trigonella foenum-graecum L. commonly known as fenugreek, is an important economic and medicinal plant cultivated in various regions of the world. Fenugreek produces several important active chemical constituents that determine its pharmacological properties. The aim of this research was to analyze the volatile constituents spontaneously emitted by eight samples of fenugreek seeds purchased from different Middle Eastern drugstores, including Saudi Arabia, Yemen, Egypt, and Iran. A total of 70 constituents belonging to different chemical classes, including monoterpene hydrocarbons, oxygenated monoterpenes, sesquiterpene hydrocarbons, phenylpropanoids, apocarotenes, nitrogen/sulfur derivatives, and non-terpene derivatives, were characterized in the volatile emissions of the eight samples, some components with significant olfactory properties were detected such as γ-nonalactone, cumin aldehyde, (E)-cinnamaldehyde, p-anisaldehyde, and eugenol. PCA showed two macro-clusters; the first comprised two sub-groups, while the second included only Yemeni samples. The findings of this study demonstrate that the significant variation for volatile profiles in fenugreek samples which are prone to variations in the geographical origin of these samples.

Effects of Rauwolfa vomitoria (Akata) and Olax subscorpioidea (Asaja) Roots on Hematology of Chicken Type II Collagen-Freund’s Adjuvant-induced Rheumatoid Arthritis in Albino Rats

This study evaluated the effects of ethanol and aqueous root extracts of Rauwolfia vomitoria and Olax subscorpioidea on Chicken type II collagen in Complete Freund’s Adjuvant-induced arthritis in albino rats. A total of 225 albino rats, weighing between 120-200 g, were used and divided into 15 groups of 15 rats each. Rheumatoid Arthritis (RA) was induced by administering 0.1 ml of Chicken type II-Complete Freund’s Adjuvant into the left hind paw. The study duration was 32 days, during which the arthritic rats were treated with Rauwolfia vomitoria and Olax subscorpioidea root extracts at doses of 400 mg, 600 mg, and 800 mg/kg body weight. The sub-lethal toxicity study revealed significant increases (P<0.05) in WBC, platelet, and differential counts, along with significant reductions (P<0.05) in RBC count, PCV, and HB in the adjuvant induced arthritic rats compared to the negative control group. However, treatment with the plant extracts (groups 4-15) significantly reversed these trends towards normal levels compared to the untreated arthritis group (group 2) within the 32-day period. The ameliorative effects of the extracts were both time- and dose dependent (P<0.05). This study concludes that the ethanol and aqueous root extracts of Rauwolfia vomitoria and Olax subscorpioidea effectively ameliorate arthritis symptoms in albino rats, potentially due to the presence of active chemical constituents. These findings provide scientific evidence supporting the therapeutic use of these plant extracts in managing arthritis.

Butea monosperma as a collective phytomedicine, including environmentally sustainable, conservative and beneficial plant

Nature exists as a golden spot and supplies the remedies to treat all diseases of mankind. Plant kingdom stand for plethora of natural compounds, well known for utilized in therapeutic applications and might act the way for expansion of novel mediators having decent efficiency in many pathological disorders in future. In India and throught the world herbs becoming principle and popular medicine. Recognized green medicines are better than synthetic one with less side effects. From ancient periods plants have been intended for their medicinal properties for treating various health ailments because of their lesser side effects, availability of the agent, their cost and potential effectiveness. Medicinal value of plants comes from various vegetative parts of the plant including flowers, fruit, bark, roots, leaves, seeds and its modified parts. The Indian forests are the major repository of remedial and aromatic medicinal plants, which are composed for production of plethora remedies against various diseases. Butea monosperma is one of traditional ayurvedic medicinal plant considered as rich source of ingredients which can be used in drug development as home remedies to treat various diseases such as diarrhea, constipation, hypertension, dehydration, bronchial asthma, leucorrhea, infection, liver, stomach disorders including cancer. The seed powder known for having specific pharmaceutical and insecticidal activities. This study highlights the traditional ayurvedic importance of a eminent medicinal plant Butea monosperma, with its active chemical constituents, pharmacological importance, environmentally sustainable, ecological, and economical importance of the plant. This plant can be planted everywhere to make use of its versatile applications.

UPLC-Q-TOF-MS Analysis of Chemical Constituents of the Kadsura coccinea Extract with Effect of Attenuating Lipid Accumulation in Vitro

Objective/Background: This study aims to explore the Kadsura coccinea extract (KCE)'s effect on lipid accumulation in vitro and its chemical components characterizations, aiming at developing a new alternative plant medicinal resource to fight against non-alcoholic fatty liver disease (NAFLD). Methods: After toxicological evaluation of KCE on HepG2 cells, Oil red O staining model and intracellular TGs quantification kit were used to examine the effects of KCE on lipid accumulation in vitro. The chemical components characterizations and potential active chemical constituents of the bioactive KCE were analyzed using ultra-high-performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS) technology. Results: Among the chosen non-toxic concentrations of KCE (5, 10, 20 μg/mL), KCE can reduce the number and volume of lipid droplets in the oleic acid induced HepG2 cells in a dose-dependent manner, and the results of TGs quantification were almost consistent with the results of the oil red O staining experiment. These data indicate the KCE has ameliorative effect on lipid accumulation in vitro. In addition, a total of 26 compounds from the KCE were tentatively identified, dibenzocyclooctadiene lignans (DCLs) including Kadsulignan L and Gomisin J could be the main supposed components. Conclusion: These findings support further investigation into Kadsura coccinea containing DCLs as a new alternative medicinal arsenal to battle against NAFLD.

Study of the antitumor activity of the combination baicalin and epigallocatechin gallate in a murine model of vincristine-resistant breast cancer

Background: Breast cancer is one of the primary causes of death in women worldwide. Yearly, a quarter of cancer cases in women are breast cancer. The problem is aggravated by the emergence of chemotherapeutic resistance. One of the practices to overcome this problem is using natural products along with chemotherapy. Epigallocatechin Gallate (EGCG) is the main efficient catechin in green tea. Baicalin is the main active chemical constituent of Scutellaria baicalensis. Both natural products have anti-cancer and improving resistance activities. Therefore, a combination of EGCG and baicalin may afford a possible way out to overcome chemotherapeutic resistance. Methods: EGCG and baicalin were tested on Vincristine-sensitive (EMT-6/P) and Vincristine-resistant (EMT-6/V) mouse mammary cell lines. Antiproliferative and apoptotic effects were assessed for EGCG, baicalin, their combination, and Vincristine in vitro using MTT and caspase-3 assays. An in vivo study was conducted to assess the effect of EGCG, baicalin, their combination, vincristine, vincristine along with the combination in both EMT-6/P and EMT-6/V mouse mammary cell lines. The safety profile was also considered using liver enzymes and creatinine assays. Results: in vitro, EGCG and baicalin had synergistic effects in both cell lines. The combination of baicalin and EGCG as 140 and 100 µM respectively, caused an apoptotic effect higher than the single treatment of baicalin 175 µM or EGCG 125 µM, in vincristine-resistant cell lines. In vivo, the combination along with vincristine significantly enhanced the reduction of tumour size in mice implanted with EMT-6/P and EMT-6/V cell lines. According to the safety profile, the combinations of EGCG and baicalin are safe. Conclusion: The combination of baicalin and EGCG can be optimistic in improving vincristine-resistant cells to treatments.

An integrated network pharmacology approach to discover therapeutic mechanisms of Commiphora wightii for the treatment of Bell’s palsy

Bell’s palsy (BP) can result in facial paralysis. Inflammation or injury to the cranial nerves that regulate the facial muscles is primarily responsible for that disease. Commiphora wightii remains recognized as a cure for a few human ailments. This study focused on therapeutic phenomena of C. wightii for the treatment of Bell’s palsy, utilizing the network drug discovery and molecular docking techniques. Active biological constituents of C. wightii were retrieved from literature and independent databases. Potential therapeutic targets (431) of 13 bioactive phytochemicals were fetched via SwissTargetPrediction tool. Putative intersecting targets (855) of Bell’s palsy were computed through the DisGeNET and GeneCards datasets. Subsequently, by the analysis of potential shared targets (87) of C. wightii and Bell’s palsy, a Venn diagram was drawn. DAVID database was used to evaluate gene functional annotations and enriched pathways that are involved in Bell’s palsy. STRING database was used for generating the protein–protein relationship complex. Visual presentations of the interactions of potential targets to active chemical constituents were done by the Cytoscape. Whereas, the conformational research sorted out 10 key targets through the protein–protein interactions network. Moreover, the capacity of therapeutic ingredients to interact with a target inhibiting Bell’s palsy was confirmed by molecular docking, which might ratify the findings of network pharmacology. In the molecular complex of AKT1–cholesterol, a 100-ns simulation unveiled a graceful stability, with a minimal 0.167 Å ligand shift and resilient hydrogen bonds (ASN54 and SER205). The final 20 ns showcased a P1 motif pirouette, gracefully forming aromatic bonds with H165 and W186, underscoring the complex’s dynamic finesse. This study evaluated compound–target interactions and their impact on disease-related genes. It revealed that five genes (AKT1, TNF, MAPK3, EGFR and SRC) of C. wightii might be useful therapeutic targets for the treatment of Bell’s palsy, as well as helping in lowering down the blood pressure. Communicated by Ramaswamy H. Sarma

Pharmacological Review of Celosia Argentea

Medicinal plants are used in all traditional system of medicine from thousands of year to treat and to prevent disease. The active metabolites possess the efficiency to treat the disorders. Based on therapeutic effect we select the plant Celosia argentea. Plant Celosia argentea belong to family-Amaranthaceae is used in various medicinal products. Various part extract are used for formulation of medicine. We mentioned the various therapeutic effects shown by drug Celosia argentea. It contain active chemical constituent are mainly phenols, flavonoids, steroids, tannins, carbohydrates, lipids, amino acids, peptides, phenolic acids, cardiac glycosides, , phytosterols, , amino acids, carbohydrates

Molecular mechanisms of Codonopsis pilosula in inhibiting hepatocellular carcinoma growth and metastasis

BackgroundLiver cancer, one of the most common types of cancer worldwide, accounts for millions of cases annually. With its multi-target and wide-ranging therapeutic effects, traditional Chinese medicine has emerged as a potential approach for treating various tumors. Codonopsis pilosula, a traditional herb, is known for its anti-inflammatory and antioxidant properties. In this study, we investigated the potential molecular mechanisms of Codonopsis pilosula in regulating the inhibition of CDK1 and the modulation of PDK1/β-catenin, which are involved in hepatocellular carcinoma growth and metastasis. Study Design/MethodsFirstly, we screened the active chemical constituents of Codonopsis pilosula and identified their respective target proteins using the Herb database. Then, we applied the GeneCards database and transcriptome sequencing analysis to screen for critical genes associated with the occurrence and development of liver cancer. The intersection of the target proteins and disease-related genes was used to determine the potential targets of Codonopsis pilosula in hepatocellular carcinoma. Protein-protein interaction analysis and GO/KEGG analysis were subsequently performed to uncover the pathways through which Codonopsis pilosula acts on liver cancer. The Huh-7 cell line, exhibiting the highest sensitivity to Codonopsis pilosula polysaccharide solution (CPP) intervention, was chosen for subsequent studies. Cell viability was evaluated using the CCK-8 assay, colony formation assay was conducted to determine cell proliferation capacity, flow cytometry was used to analyze cell cycle, TUNEL staining was performed to assess cell apoptosis, scratch assay was carried out to evaluate cell migration ability, the expression of EMT-related proteins was detected and analyzed, and cell sphere formation assay was conducted to investigate cell stemness. Finally, a liver cancer animal model was established, and different doses of CPP were administered via gavage the next day. The expression levels of CDK1, PDK1, and β-catenin in mouse liver tissues were detected and analyzed, immunohistochemistry staining was performed to assess the expression of tumor cell proliferation-related proteins Ki67 and PCNA in mouse xenografts, and TUNEL staining was carried out to evaluate cell apoptosis in mouse liver tissues. After intervention with CDK1 expression, the expression levels of CDK1, PDK1, and β-catenin proteins and mRNA in each group of cells were detected using Western blot and RT-qPCR. ResultsThrough network pharmacology analysis, transcriptome sequencing, and bioinformatics analysis, 35 target genes through which Codonopsis pilosula acts on liver cancer were identified. Among them, CDK1, with the highest degree in the PPI network, was considered an essential target protein for Codonopsis pilosula in treating liver cancer. In vitro cell experiments revealed that CPP could inhibit the expression of CDK1/PDK1/β-catenin signaling axis factors, suppress cell proliferation, decrease cell migration ability, influence the EMT process, and reduce cell stemness by inhibiting CDK1 and affecting the PDK1/β-catenin signaling axis. Similarly, in vivo experiments demonstrated that CPP could regulate the CDK1/PDK1/β-catenin signaling axis, inhibit tumor growth, and induce cell apoptosis. ConclusionCodonopsis pilosula may inhibit hepatocellular carcinoma growth by suppressing CDK1 and affecting the PDK1/β-catenin signaling axis, limiting cell EMT and reducing cell stemness. These findings provide insights into the potential therapeutic role of Codonopsis pilosula in liver cancer.

Indian Medicinal Plants for the Management of Endometriosis: A Comprehensive Review on their phytopharmacology

Endometriosis is a chronic gynecological disorder characterized by the aberrant growth of endometrial tissue outside the uterus, resulting in severe pain and infertility. Conventional treatments often come with limitations and side effects, prompting a quest for alternative therapies. Medicinal plants, integral to traditional medicine systems, have emerged as potential solutions. This review delves into the phytopharmacology and chemistry of medicinal plants employed in endometriosis treatment. An exhaustive search revealed pertinent studies concerning medicinal plant use in endometriosis treatment. These studies were scrutinized for their phytopharmacological attributes and active chemical constituents. Numerous medicinal plants exhibited anti-inflammatory, analgesic, antioxidant, immunomodulatory, and hormone-regulating properties, pivotal in endometriosis management. Mechanisms encompassed the suppression of inflammatory mediators, modulation of estrogen signaling, mitigation of oxidative stress, and enhancement of immune function. Furthermore, key chemical constituents responsible for these effects were pinpointed and classified into classes such as flavonoids, terpenoids, alkaloids, and phenolic compounds. These bioactive agents elicited their actions via diverse molecular targets, including cyclooxygenase enzymes, estrogen receptors, nuclear factor-kappa B, and reactive oxygen species. The findings underscore the potential of medicinal plants as adjunct therapies for endometriosis. Nonetheless, additional preclinical and clinical investigations are imperative to substantiate their efficacy, safety, and optimal dosing. Grasping the phytopharmacology and chemistry of medicinal plants in endometriosis treatment lays the groundwork for novel therapeutic agent development, spotlighting the capacity of natural products to combat this intricate gynecological ailment.

Antibacterial activity of Seaweed extracts against human pathogenic bacteria

Seaweeds are screened extensively for their activity against human bacterial pathogens. In the present study, the petroleum ether, butanol, chloroform, acetone and methanol extracts of seaweed species, viz., Caulerpa racemosa, Padina gymnospora, Sargassum wightii and Ulva fasciata were investigated for their antibacterial properties by well diffusion method against human pathogenic bacteria (Bacillus subtilis, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Salmonella typhimurium, Staphylococcus aureus and Streptococcus mutans). Preliminary qualitative analysis on the chemical constituents of the twenty seaweed crude extracts revealed the predominant presence of phenols and tannins. Antibacterial activity of the seaweed extracts were represented by zone of inhibition. The order of maximum antibacterial activity (represented by very strong zone of inhibition) was exhibited by Padina gymnospora petroleum ether extract against Staphylococcus aureus (23.6mm) and Pseudomonas aeruginosa (21.6mm), and its butanol extract against Pseudomonas aeruginosa (20.5mm). From the overall results of the present study, it was observed that Padina gymnospora extracts exhibited maximum antibacterial activity, attributed to the presence of the active chemical constituents, especially phenols and tannins. Further in depth studies are recommended, as Padina gymnospora extracts could serve as an additional implement to natural antibacterial agents.

Density functional theory, molecular docking, In vitro and In vivo anti-inflammatory investigation of lapachol isolated from Fernandoaadenophylla

Medicinal plants are the main source of active chemical constituents responsible for curing or mitigating various ailments. To discover new, safe, and effective drug candidates the isolation and screening of natural products are essential. In the current research work, lapachol was isolated from Fernandoa adenophylla, which was evaluated for anti-inflammatory effect followed by molecular docking. The isolated compound was tested for anti-inflammatory effects using in vitro (HRBC assay) and in vivo (xylene-induced ear edema) experimental models. Various concentrations of lapachol demonstrated anti-inflammatory effects with a percent potential of 77.96 at 100 μM. Different concentrations of Lapachol demonstrated a dose-dependent anti-edematous effect with a maximum percent effect of 77.9 % at a higher dose. The histopathological study revealed that the application of xylene led to a significant increase in ear thickness, along with clear signs of ear edema and infiltration of inflammatory cells, as well as epidermal hyperplasia of the dermis when compared to the control group. However, treatment with the investigated compound showed a significant reduction in ear thickness and pathological differences comparable to those observed in the group treated with diclofenac. Density functional theory calculations are accomplished to gain insight into structural and spectroscopic properties. Geometry optimization, FMO, and MEP analyses are performed. Overall, the molecular docking results indicate that lapachol has potential as a COX inhibitor by binding to the active sites of both COX-1 and COX-2 enzymes.

Effects of total flavones of Abelmoschus manihot (L.) on the treatment of diabetic nephropathy via the activation of solute carriers in renal tubular epithelial cells

As a traditional Chinese medicine, Huangkui capsule (HKC) has been used to treat patients with kidney diseases, including diabetic nephropathy (DN). We have recently demonstrated that HKC could re-regulate the activities of solute carriers (SLC)s in proximal and distal convoluted tubules of kidneys in regression of the development of DN. The main active chemical constituents of HKC are the flavones of Abelmoschus manihot (L.). The current study aims to further evaluate the efficacy of total flavones of A. manihot (TFA) in the regression of DN by analyzing SLC activities in proximal and distal convoluted tubules of kidneys. TFA (0.076 g/kg/d) or vehicle was administered in db/db mice, the animal model of type 2 diabetes and DN, daily via oral gavage for four weeks. Blood glucose levels and urinary albumin-to-creatinine ratio (UACR) were measured and used for the determination of T2D and DN. Ten SLCs, including slc2a2, slc4A1, slc5a2, slc5A3, slc5a8, slc6a20, slc27a2, slc12a3, slc34a1 and slc38a2 were highly expressed in proximal and distinct convoluted tubules of kidneys. Their expression at mRNA and protein levels before and after TFA treatment were analyzed with real-time RT-PCR and immunohistochemistry. Data showed that UACR in the db/db mice after TFA treatment was significantly decreased. Compared with the group of non-diabetic control, slc2a2, slc4A1, slc5a2, slc5A3, slc5a8, slc6a20, slc27a2, slc12a3, slc34a1 and slc38a2 in the group of DN were down-regulated but up-regulated after TFA treatment. Further analyses of whole kidney sections indicated that the numbers and structures of the nephron in db/db mice was increased and improved after TFA treatment. Thereby, the current study provides further evidence that the flavones in A. manihot have pharmacological effects on the treatment of DN by improving the biological function of SLCs in kidneys.

Topical Mosquito Repellent Formulations for Enhanced Repellency Time and Reduced Toxicity.

Mosquito-borne diseases such as dengue, malaria, yellow fever, chikungunya and Zika virus affect millions of people worldwide each year. Vector control and personal protection are very important to minimize the spread of diseases, and the use of repellent is an economic practice to prevent them. The application of repellent, which acts on the skin to form a vapor layer with a repellent odor to mosquitos, is recommended as an economic prevention and practice. The natural botanical product Citronella is an effective mosquito repellent due to the high concentrations of active chemical constituents present, notably terpenic alcohols. However, citronella tends to evaporate quickly from the skin surface, resulting in a rapid loss of activity. Strategies to increase repellency time, while at the same time minimizing toxicity, are major focuses of research and development in natural repellent products. Here we highlight the role of extended-release systems (ERS) of citronella oil in this approach.

GC-MS analysis and in silico docking of constituents of Cinnamomum malabatrum against CYP450 17α and CYP450 19 (Aromatase)- Key targets for hyperandrogenism.

Poly cystic ovary syndrome (PCOS) is considered as one of the common hormonal disorders affecting 6-20% of women in their reproductive age with characteristic features include anovulatory infertility, hyperandrogenism, cystic follicles and insulin resistance. The gene CYP play an important role in pathophysiology of hyperandrogenism associated with PCOS. An elevated androgens are reported in PCOS condition due to overexpression of the enzyme CYP450 17 α: . As well as diminished levels of aromatase (CYP450 19) were observed in several hyperandrogenic PCOS patients. The powdered leafy material of Cinnamomum malabatrum was subjected to Soxhlet extraction. The plant extract was subjected to Gas chromatography-MS analysis (GC-MS), and the chromatogram obtained revealed the presence of active chemical constituents like 1(10),9(11)-B-Homolanistadiene for the first time and other potential compounds. Hypothesis has raised to interpret the efficiency of phytoconstituents of Cinnamomum malabatrum on these enzyme targets and which may be a novel drug candidate for the treatment and maintenance of hyperandrogenism associated with PCOS. Thus, the results obtained from the in-silico study of Cinnamomum malabatrum leaf extract using computational approaches indicate that the phytoconstituents have good affinities for the selected two key targets. ADME and PASS studies has been performed for active phytoconstituents homolanistadiene, β-sitosterol, cycloartenol and a pyrazole derivative, and results revealed the Lipinski drug-likeness and pharmacological potential. In conclusion, this work throws a new insight into the possibility of the active phytoconstituents on binding the two active CYP45017 α and CYP45019 aromatase enzymes which facilitates development of novel compounds for hyperandrogenism associated with PCOS.