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A study was designed to investigate the presence of nanoferrites in Cryptolepis buchanani. In this study, various leaves and stem organic extracts were prepared separately using the solvents viz., n-hexane, ethyl acetate, ethanol and water. Different phytochemical tests for alkaloids, carbohydrates, oils, amino acids and others were performed to determine their presence in the extracts. These plant extracts were used for screening of sample via UV and HPLC techniques to compare the wavelength and absorbance, and retention time on chromatogram by extracts, respectively. The results showed the presence of alkaloids, carbohydrates and proteins in all the samples. However, other compounds were present randomly. Spectroscopy showed highest peaks with ethyl acetate extracts and the lowest with water. The surface properties and size of nickel-zinc nano ferrites were evaluated by Energy-dispersive X-ray spectroscopy (EDX) and Scanning Electron Microscopy (SEM). The former, showed the presence of nickel (Ni) and zinc (Zn) weighing 4.27⁒ of N ,6.89⁒ of C and 35.5⁒ of O in the sample which confirmed the presence of nano ferrites in leaves and stem of C. buchanani.

The material medica has over 25000 plant species having therapeutic value, and more than 500 are used in indigenous systems of medicine. Sariva is one such drug having multifaceted activities widely used as coolant, blood purifier. In Ayurvedic classics two varieties have been mentioned, Shweta and Krishna. Regarding the botanical identity of both the varieties, Shweta Sariva is unanimously accepted as Hemidesmus indicus, where as for Krishna Sariva is accepted as both Ichnocarpus frutescens, Cryptolepis buchnani. In the market, by the name of Sariva Decalepis hamiltonii is usually sold. Hence all the four sources were collected from their natural habitat, subjected for phytochemical analysis, including its morphological features and HPTLC was carried out. In this research work it was found that the four sources of Sariva have match with standards mentioned in quality standards of Indian medicinal plants, published by ICMR, New Delhi. Further these sources should be subjected for pharmacological evaluations pertaining Sariva as to confirm the genuine source and best substitute.

Cryptolepis oblongifolia (Meisn.) Schltr. — Habit: Shrub. Habitat: LMWF, LMDF; up to 2 300 m. Distribution: II. Voucher: Northeast Mount Kenya, Meru, Balbo 16 (FT). References: Goyder et al. (2012)., Published as part of Zhou, Ya-Dong, Mwachala, Geoffrey, Hu, Guang-Wan & Wang, Qing-Feng, 2022, Annotated checklist of the vascular plants of Mount Kenya, East Africa, pp. 1-108 in Phytotaxa 546 (1) on page 76, DOI: 10.11646/phytotaxa.546.1.1, http://zenodo.org/record/6550464, {"references":["Goyder, D., Harris, T., Masinde, S., Meve, U. & Venter, J. (2012) Apocynaceae (Part 2). In: Beentje, H. J. (Ed.) Flora of Tropical East Africa. Royal Botanic Gardens, Kew, London, 416 pp."]}

The ongoing global pandemic caused by the human coronavirus, severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has infected millions of people and claimed hundreds of thousands of lives. The absence of approved therapeutics to combat this disease threatens the health of all persons on earth and could cause catastrophic damage to society. New drugs are therefore urgently required to bring relief to people everywhere. In addition to repurposing existing drugs, natural products provide an interesting alternative due to their widespread use in all cultures of the world. In this study, alkaloids from Cryptolepis sanguinolenta have been investigated for their ability to inhibit two of the main proteins in SARS-CoV-2, the main protease and the RNA-dependent RNA polymerase, using in silico methods. Molecular docking was used to assess binding potential of the alkaloids to the viral proteins whereas molecular dynamics was used to evaluate stability of the binding event. The results of the study indicate that all 13 alkaloids bind strongly to the main protease and RNA-dependent RNA polymerase with binding energies ranging from -6.7 to -10.6 kcal/mol. In particular, cryptomisrine, cryptospirolepine, cryptoquindoline, and biscryptolepine exhibited very strong inhibitory potential towards both proteins. Results from the molecular dynamics study revealed that a stable protein-ligand complex is formed upon binding. Alkaloids from Cryptolepis sanguinolenta therefore represent a promising class of compounds that could serve as lead compounds in the search for a cure for the corona virus disease.

Malaria is one of the life-threatening parasitic diseases that is endemic in tropical areas. The increased prevalence of malaria due to drug resistance leads to a high incidence of mortality. Drug discovery based on natural products and secondary metabolites is considered as alternative approaches for antimalarial therapy. Herbal medicines have advantages over modern medicines, including fewer side effects, cost-effectiveness, and affordability encouraging the herbal-based drug discovery. Several naturally occurring, semisynthetic, and synthetic antimalarial medications are on the market. For example, chloroquine is a synthetic medication for antimalarial therapy derived from quinine. Moreover, artemisinin, and its derivative, artesunate with sesquiterpene lactone backbone, is an antimalarial agent originated from Artemisia annua L. A. annua traditionally has been used to detoxify blood and eliminate fever in China. Although the artemisinin-based combination therapy against malaria has shown exceptional responses, the limited medicinal options demand novel therapeutics. Furthermore, drug resistance is the cause in most cases, and new medications are proposed to overcome the resistance. In addition to conventional therapeutics, this review covers some important genera in this area, including Artemisia, Cinchona, Cryptolepis, and Tabebuia, whose antimalarial activities are finely verified.

Following the high treatment gap and massive impact of epilepsy on global health particularly in low- and middle-income countries, our study aims to investigate cryptolepine, the major alkaloid of Cryptolepis sanguinolenta as well as its solid-lipid nanoparticle formulation for potential antiseizure activity. Cryptolepine was isolated and a solid-lipid formulation was prepared. Antiseizure activity of Solid-Lipid Nanoparticle formulation of cryptolepine (SLN-CRYP) was investigated using Pentylenetetrazole (PTZ)-induced model of seizure-like behaviors in Zebrafish with 2.5 and 5 mg/kg each of cryptolepine and SLN-CRYP. Drug receptor binding and permeability of the compound across the Blood Brain Barrier (BBB) were also assessed. SLN formulation of cryptolepine increased its permeability to the BBB from 0.32 × 10−6 cm/s to 10.81 × 10−6 cm/s. 2.5 and 5 mg/kg of SLN-CRYP significantly reduced mean seizure score (P = 0.0018; F(6, 63) = 23.52) and significantly increased (P

Background The object of the present study is to evaluate the effect of alcoholic extracts of Cissus quadrangularis (CQ), Cryptolepis buchanani (CB), and Sardinella longiceps (SL) either alone or in the combination (100 mg/kg) in the management of femur bone healing of Wistar albino rats for 8 weeks. After the period of treatment, femur bones were examined by using biochemical, radiographical, and histopathological studies. Result Biochemical evaluation results reveal that there is a steep increase of serum calcium level in the experimental animals during the entire period of treatment which led to an adequate supply of serum calcium to the fractured bone for healing and increases the thickness of the femur bones soon compared to control group. It had been estimated by a calibrated ocular micrometer. Radiographical images of the bones also disclose that the complete bridging of fractured bone occurred in the experimental animals after the treatment of natural compound extracts. In addition to that, all the organs of animals were safe in the experimental animals during the entire study. Conclusion The present study strongly recommended that these ethanolic extracts (CQCBSL) either alone or in the combination restoring the strength of the bone and reduced bone repairing period due to the rich content of calcium and other natural phytochemicals presents with them. Graphical abstract

Cryptolepine, the principal constituent of the West African climbing shrub Cryptolepis sanguinolenta, continues to be of interest as a lead to new therapeutic agents, especially for the treatment of protozoal infections and cancer. This contribution reviews the research published in the last decade, highlighting new synthesis routes to cryptolepine and to analogs of this alkaloid, as well as their pharmacology. Studies relating to the use of C. sanguinolenta as an herbal medicine for the treatment of malaria are discussed, as well as the development of analogs of cryptolepine as leads to new agents for the treatment of malaria, trypanosomiasis, and cancer with an emphasis on the pharmacological mechanisms involved. Other potential therapeutic applications include antimicrobial, antidiabetic, and anti-inflammatory activities; the pharmacokinetics and toxicity of cryptolepine are also reviewed.

BackgroundDiverse signalling pathways are involved in carcinogenesis and one of such pathways implicated in many cancers is the interleukin 6/signal transducer and activator of transcription 3 (IL-6/STAT3) signalling pathway. Therefore, inhibition of this pathway is targeted as an anti-cancer intervention. This study aimed to establish the effect of cryptolepine, which is the main bioactive alkaloid in the medicinal plantCryptolepis sanguinolenta, on the IL-6/STAT3 signalling pathway.MethodsFirst, the effect of cryptolepine on the IL-6/STAT3 pathway in human hepatoma cells (HepG2 cells) was screened using the Cignal Finder Multi-Pathway Reporter Array. Next, to confirm the effect of cryptolepine on the IL-6/STAT3 signalling pathway, the pathway was activated using 200 ng/mL IL-6 in the presence of 0.5–2 μM cryptolepine. The levels of total STAT3, p-STAT3 and IL-23 were assessed by ELISA.ResultsCryptolepine downregulated 12 signalling pathways including the IL-6/STAT3 signalling pathway and upregulated 17 signalling pathways. Cryptolepine, in the presence of IL-6, decreased the levels of p-STAT3 and IL-23 in a dose-dependent fashion.ConclusionOur results demonstrated that cryptolepine inhibits the IL-6/STAT3 signalling pathway, and therefore cryptolepine-based remedies such asCryptolepis sanguinolentacould potentially be used as an effective immunotherapeutic agent for hepatocellular carcinoma and other cancers.

Human babesiosis is a CDC reportable disease in the United States and is recognized as an emerging health risk in multiple parts of the world. The current treatment for human babesiosis is suboptimal due to treatment failures and unwanted side effects. Although Babesia duncani was first described almost 30 years ago, further research is needed to elucidate its pathogenesis and clarify optimal treatment regimens. Here, we screened a panel of herbal medicines and identified Cryptolepis sanguinolenta, Artemisia annua, Scutellaria baicalensis, Alchornea cordifolia, and Polygonum cuspidatum to have good in vitro inhibitory activity against B. duncani in the hamster erythrocyte model. Furthermore, we found their potential bioactive compounds, cryptolepine, artemisinin, artesunate, artemether, and baicalein, to have good activity against B. duncani, with IC50 values of 3.4 μM, 14 μM, 7.4 μM, 7.8 μM, and 12 μM, respectively, which are comparable or lower than that of the currently used drugs quinine (10 μM) and clindamycin (37 μM). B. duncani treated with cryptolepine and quinine at their respective 1×, 2×, 4× and 8× IC50 values, and by artemether at 8× IC50 for three days could not regrow in subculture. Additionally, Cryptolepis sanguinolenta 90% ethanol extract also exhibited no regrowth after 6 days of subculture at doses of 2×, 4×, and 8× IC50 values. Our results indicate that some botanical medicines and their active constituents have potent activity against B. duncani in vitro and may be further explored for more effective treatment of babesiosis.

Aqueous root extract of Cryptolepis sanguinolenta has been used traditionally to treat many upper respiratory tract disorders. Besides its well-known broad spectrum antimicrobial activity, we had reasoned that cryptolepine can directly attenuate the symptoms of asthma. Therefore, this study evaluates cryptolepine, the main compound of the aqueous extract of Cryptolepis sanguinolenta, on early and late-phase symptoms of asthma attack. In the early phase study, isolated cryptolepine was evaluated on its ability to reverse histamine-induced bronchoconstriction and reduce histamine release from mast cells and bronchial mucus secretion. In the late phase study, cryptolepine was evaluated on its ability to affect airway inflammation and hypersensitivity as well as its ability to attenuate airway remodeling induced by ovalbumin. In the early asthma phase study, Cryptolepine (10–100 mg/kg) significantly and dose dependently inhibited Histamine-induced bronchoconstriction in guinea pigs. The protection lasted beyond 24 h. It also decreased the volume and optical density of bronchial secretions in mice. Cryptolepine (10–100 µg /mL) stabilized mesentery mast cells in vitro against Compound 48/80 -induced degranulation. In the late phase study, cryptolepine (10–100 mg/kg) prevented ovalbumin-induced airway obstruction and basal membrane smooth muscle hypertrophy. It significantly reduced systemic leukocytosis and inflammatory cell infiltration into airways in antigen-sensitized animals. Using the skin prick test, cryptolepine reduced the hypersensitivity to allergen challenge in antigen-sensitized animals. Cryptolepine's effects in the late phase was similar to dexamethasone (1 mg/kg) used as standard drug. Cryptolepine attenuates both early and late phase symptoms of asthma. It reduces bronchospasms, bronchial secretions, airway remodeling and hypersensitivity. This gives scientific credence to the traditional usage of cryptolepis extracts in upper respiratory tract disorders.

The ongoing global pandemic caused by the human coronavirus, severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has infected millions of people and claimed hundreds of thousands of lives. The absence of approved therapeutics to combat this disease threatens the health of all persons on earth and could cause catastrophic damage to society. New drugs are therefore urgently required to bring relief to people everywhere. In addition to repurposing existing drugs, natural products provide an interesting alternative due to their widespread use in all cultures of the world. In this study, alkaloids from Cryptolepis sanguinolenta have been investigated for their ability to inhibit two of the main proteins in SARS-CoV-2, the main protease and the RNA-dependent RNA polymerase, using in silico methods. Molecular docking was used to assess binding potential of the alkaloids to the viral proteins whereas molecular dynamics was used to evaluate stability of the binding event. The results of the study indicate that all 13 alkaloids bind strongly to the main protease and RNA-dependent RNA polymerase with binding energies ranging from -6.7 to -10.6 kcal/mol. In particular, cryptomisrine, cryptospirolepine, cryptoquindoline, and biscryptolepine exhibited very strong inhibitory potential towards both proteins. Results from the molecular dynamics study revealed that a stable protein-ligand complex is formed upon binding. Alkaloids from Cryptolepis sanguinolenta therefore represent a promising class of compounds that could serve as lead compounds in the search for a cure for the corona virus disease.

The present paper reports duration of different developmental stages as well as fecundity, longevity, oviposition periods, sex ratio, etc. of Tetranychus sayedi Baker & Pitchard on two medicinal plants, viz. Cryptolepis buchanani Roem & Schult and Justicia adhatoda L. under laboratory condition at 27.5 °C and 65% R.H. during February-March, 2016. The two hosts in which the life cycle was studied form two new records of hosts for this mite. It appears that C. buchanani is better host among the two hosts as because the life cycle (egg to adult) was completed in shorter time, recording high fecundity and longer longevity.

Aim This study aimed to compare the efficacy of a topical Cryptolepis buchanani oil formulation (CBO) with indomethacin, a topical non-steroidal anti-inflammatory drug, in the symptomatic treatment of osteoarthritis (OA) of the knee. Study design This study was a randomized, double-blind, active-controlled trial. Methods One hundred and sixty-nine patients with OA of the knee were randomly assigned to receive either a 1% indomethacin solution or CBO formulation, which were applied topically, four times a day for a period of four weeks. Clinical assessments included a visual analog scale (VAS) assessment of joint pain, VAS assessment of stiffness, Lequesne’s functional index (LI), time taken to climb up 10 steps, and patient’s and physician’s opinions of overall improvement. Results After four weeks of treatment, there were no statistically significant differences between the two groups in mean changes from baseline of the VAS assessment of total pain (p = 0.92), VAS assessment of total stiffness (p = 0.57), LI (p = 0.44), and time taken to climb up 10 steps (p = 0.61). Additionally, the mean VAS of patient’s and physician’s opinions of overall improvement did not differ significantly (p = 0.77 and p = 0.77, respectively). The percentages of responders in the CBO and the indomethacin groups were also comparable (67.44% versus 69.88%, p = 0.86). Treatments were generally well tolerated, with reports of pruritus and rash at the application site occurring significantly more frequently in the indomethacin than CBO group (28.92% versus 10.47%, p = 0.005 and 21.69% versus 8.14%, p = 0.024, respectively). Conclusion CBO was as effective as indomethacin solution for the symptomatic treatment of OA of the knee, but had a significantly lower rate of adverse skin reactions.

Gautam AK, Avasthi S. 2017. Short Communication: Some additions to powdery mildews (Erysiphales: Fungi) of Northwestern Himalayas. Nusantara Bioscience 9: 52-56. During the regular mycological collections, between October to December 2015 in North-West Himalayas of Himachal Pradesh, four powdery mildews parasitic on higher plants were gathered. After study they were found to be Pseudoidium cryptolepidis on Cryptolepis buchanani, Erysiphe trifoliorum on Trifolium repentis, Podosphaera xanthii on Coreopsis lanceolata and Podosphaera euphorbiae-hirtae on Euphorbia hirta. All the powdery mildew fungi are additions to Himachal Pradesh as well as north-west Himalayas.

Regimens of current drugs for tuberculosis are lengthy and are associated with many adverse effects. Currently, the emergence of different resistant strains has been observed. This urges a need for the discovery and development of novel drugs. The main sources of drug lead candidates are based on natural products. Zanthoxylum leprieurii, Lantana camara, and Cryptolepis Sanguinolenta are among the plants that have antimycobacterial activity. Recent technological methods, such as metabolomics, can rapidly detect and identify active compounds from medicinal plants. In this review, we aim to provide an overview and discussion of the antimycobacterial activity, phytochemical analysis and toxicity profile of these plants and their products as well as the potential of metabolomic fingerprinting of medicinal plants with a given activity on microbes, in the search for the potential drug hit molecules. The information for this review was extracted from databases such as Excerpta Medica Database, Google Scholar, Springer, and PubMed Central. Primary studies, using a combination of the keywords antimycobacterial medicinal plant, multidrug-resistant tuberculosis, phytochemistry, toxicity, Zanthoxylum leprieurii, Lantana camara, Cryptolepis sanguinolenta, and plant metabolomics/metabolic fingerprinting of plant extracts, have been considered. The above-mentioned plant species showed antimycobacterial activity against drug-resistant strains of M. tuberculosis. They may provide potential candidates for novel drugs against multidrug-resistant tuberculosis. However, extensive work is still needed. To our knowledge, there is no or limited literature that reports the metabolic fingerprints of these plants. The analysis of the metabolite fingerprints of medicinal plants with similar antimicrobial activity could be important to determine whether the activity results from common metabolites within different plant species. This review shows that these plants are potential candidates to provide drug hits against multidrug-resistant tuberculosis strains. Future studies of compound optimization, in vivo safety and efficacy, as well as of the specific mechanisms of action are however required.

Ethnopharmacological relevance Acanthosicyos naudininus, Gomphocarpus fruticosus, and Cryptolepis decidua are, according to the knowledge of traditional healers, used in Namibia to treat inflammatory disorders such as pain, fever and skin rashes. Aim of the study: The present study was conducted to evaluate the immunomodulatory effects and the possible underlying mechanisms of action of the plant extracts on peripheral blood mononuclear cells (PBMCs) such as T-lymphocytes. Materials and methods Methanolic and EtOAc extracts of A. naudinianus, G. fruticosus and C. decidua were analysed for their immunomodulatory potential. PBMCs were isolated from the blood of healthy donors and incubated with the plant extracts at concentrations 100, 30, 10, 3, 1 and 0.3 μg/mL. Effects on proliferation and viability of activated human lymphocytes were assessed in comparison to ciclosporin A by flow cytometry using carboxyfluorescein succinimidyl ester (CFSE) and WST-1 assay. Flow cytometry by annexin V/propidium iodide (PI) staining was performed to investigate the necrotic/apoptotic effect of the plant extracts on mitogen-activated human lymphocytes. In addition, analysis of the influence of plant extracts on the regulatory mechanisms of T-lymphocytes was performed using activation marker and cytokine production assays. An HPLC-PDA-ELSD-ESIMS profile was recorded for each of the extracts. Results T-lymphocyte proliferation was inhibited in a dose-dependent manner by the extracts of A. naudinianus, G. fruticosus, and C. decidua in concentrations not causing apoptosis or necrosis. This effect was mediated by inhibition of lymphocyte activation, specifically the suppression of CD25 and CD69 surface receptor expression. Moreover, the extracts suppressed effector functions, as indicated by reduced production of IFN-γ and IL-2. Based on the HPLC profile, possible responsible compound classes could be identified for the extracts of A. naudinianus (cucurbitacins) and C. decidua (indole alkaloids), but not for G. fruticosus. Conclusions The data show that the extracts of A. naudinianus, G. fruticosus and C. decidua have in vitro immunomodulatory activity and they interfere with the function of immunocompetent cells, suggesting an anti-inflammatory mode-of-action. The present chemical determination and pattern recognition results explain the therapeutic potency. However, further studies to investigate the therapeutic potential of the plants in inflammatory disorders should be done.

Background The effects of methanol extract of Parquetina nigrescens were studied on histomorphometry and protein expression (SDS-PAGE) from the ovaries and uteri of wistar rats. Methods 30 sexually matured rats were used for the study with 10 each in the control and treatment 100 mgkg−1 and 400 mgkg−1 groups. The extract was orally administered for 14 days. Histological sections of tissues collected presented no abnormalities. Results An increase in the number of developing and matured follicles were observed during the study in the treated groups compared to the control in the follicular and the luteal phases. The corpora lutea in the treated groups were fewer in number to that of the control in the follicular phase and in the luteal phase. Sections of the uterine horns showed significant narrowing in the lumen diameter and increases in epithelial height with increased laydown of the lamina propria in the treated groups. The expression of protein bands fractionated during the study, confirm the presence of proteins expressed repeatedly from the ovary and uterine horns in the follicular and luteal phases at the 70 kDa and 63 kDa regions. Conclusions The study concluded that the methanol extract of the plant increased folliculogenesis on the ovary, secretory activity in the nuclei of the epithelium and the fibroplasia of the lamina propria while narrowing the lumen of the uterine horns which are similar to the effects of oestrogen or oestrogen-like substances on these reproductive organs and may have an effect on the abundance of protein expressed in the follicular phase.

India is enriched in diversity of flora since ages. The ancient professionals have kept records of their work related to the plants. These works are a source of research today. Sariva is a well known herb since it is most commonly used in Ayurveda for its various therapeutic uses. Later on controversies erupt as locals in different parts of India used different plant species are considered in the name Sariva across India. From the data available, four species are being used as sariva in different regions. Hemidesmus indicus is a botanical name of true sariva. Cryptolepis buchanani and Ichnocarpus are also collectively known as Sariva in ayurveda. In south India Decalepis hamiltonii is being used as true Sariva. Sariva is a widely used herbal drug in the management of cognitive disorders from the times of Aacharya Charaka till today. Hemidesmus indicus, also known in ancient Ayurvedic medicine as "Sugandi" or "Sariva", has been revealed for its medicinal properties since nearly a thousand years. True Sariva traditionally used in various preparations. There is a greater chance of real material been adulterated or substituted by similar looking, cheaper material. Therefore present study is launched to carry out a complete pharmacognostic evaluation of Hemidesmus indicus and its possible adulterants or substitutes which are being used as true sariva in different regions of India. These diagnostic characters will be useful to screen out original crude drug material at the point purchasing.

Background Increasing resistance to current anti-malarial therapies requires a renewed effort in searching for alternative therapies to combat this challenge, and combination therapy is the preferred approach to address this. The present study confirms the anti-plasmodial effects of two compounds, cryptolepine and xylopic acid and the relationship that exists in their combined administration determined. Methods Anti-plasmodial effect of cryptolepine (CYP) (3, 10, 30 mg kg−1) and xylopic acid (XA) (3, 10, 30 mg kg−1) was evaluated in Plasmodium berghei-infected male mice after a 6-day drug treatment. The respective doses which produced 50% chemosuppression (ED50) was determined by iterative fitting of the log-dose responses of both drugs. CYP and XA were then co-administered in a fixed dose combination of their ED50s (1:1) as well as different fractions of these combinations (1/2, 1/4, 1/8, 1/16 and 1/32) to find the experimental ED50 (Zexp). The nature of interaction between cryptolepine and xylopic acid was determined by constructing an isobologram to compare the Zexp with the theoretical ED50 (Zadd). Additionally, the effect of cryptolepine/xylopic acid co-administration on vital organs associated with malarial parasiticidal action was assessed. Results The Zadd and Zexp were determined to be 12.75 ± 0.33 and 2.60 ± 0.41, respectively, with an interaction index of 0.2041. The Zexp was significantly (P

Background Khaya grandifoliola (C.D.C.) stem bark, Cymbopogon citratus (Stapf) and Cryptolepis sanguinolenta (Lindl.) Schltr leaves are used in Cameroonian traditional medicine for the treatment of inflammatory diseases. Several studies have been performed on the biological activities of secondary metabolites extracted from these plants. However, to the best of our knowledge, the anti-neuro inflammatory and protective roles of the polysaccharides of these three plants have not yet been elucidated. This study aimed at investigating potential use of K. grandifoliola, C. sanguinolenta and C. citratus polysaccharides in the prevention of chronic inflammation. Methods Firstly, the composition of polysaccharide fractions isolated from K. grandifoliola stem bark (KGF), C. sanguinolenta (CSF) and C. citratus (CCF) leaves was assessed. Secondly, the cytotoxicity was evaluated on Raw 264.7 macrophages and U87-MG glioblastoma cell lines by the MTT assay. This was followed by the in vitro evaluation of the ability of KGF, CSF and CCF to inhibit lipopolysaccharides (LPS) induced overproduction of various pro-inflammatory mediators (NO, ROS and IL1β, TNFα, IL6, NF-kB cytokines). This was done in Raw 264.7 and U87-MG cells. Finally, the in vitro protective effect of KGF, CSF and CCF against LPS-induced toxicity in the U87-MG cells was evaluated. Results CCF was shown to mostly contain sugar and no polyphenol while KGP and CSP contained very few amounts of these metabolites (≤ 2%). The three polysaccharide fractions were non-toxic up to 100 μg.mL− 1. All the polysaccharides at 10 μg/mL inhibited NO production, but only KGF and CCF at 12.5 μg/mL down-regulated LPS-induced ROS overproduction. Finally, 100 μg/mL LPS reduced 50% of U87 cell viability, and pre-treatment with the three polysaccharides significantly increased the proliferation. Conclusion These results suggest that the polysaccharides of K. grandifoliola, C. citratus and C. sanguinolenta could be beneficial in preventing/treating neurodegenerative diseases in which neuroinflammation is part of the pathophysiology.

Parquetina nigrescens is a medicinal herb with recognized antioxidant properties and potential to alleviate conditions associated with oxidative stress, including gastric ulcers. We investigated the protective potential of methanol extract of Parquetina nigrescens (MEPN) against ischemia-reperfusion injury in the intestine of rats. Thirty (30) male Wistar albino rats were randomly assigned into five groups with Group I made up of control rats and Group II consisting of rats experimentally subjected to ischemia and reperfusion (IR) by clamping of the superior mesenteric artery (SMA) for 30 minutes and 45 minutes, respectively. Groups III and IV rats also had IR, but were initially pre-treated with MEPN at 500 mg/kg and 1000 mg/kg respectively, for seven days. Rats in Group V were also pre-treated with Vitamin C, for seven days, before induction of IR. The results showed marked reduction in intestinal epithelial lesions in groups treated with MEPN, compared to the IR group which had severe villi erosion, inflammatory cell infiltration and hemorrhages. There were significant increases in Malondialdehyde (MDA) and significant reductions in reduced glutathione (GSH) and Glutathione S-transferase (GST) activity with IR injury, while pre-treatment with either MEPN or Vitamin C prevented these effects. Increases in Glutathione peroxidase (GPX), Catalase (CAT) and Superoxide dismutase (SOD) with IR provided evidence for adaptive responses to oxidative injury during IR and preservation of enzyme activity by MEPN and Vitamin C. Taken together, Parquetina nigrescens provided considerable alleviation of intestinal injury produced by IR, at values much as effective as that offered by Vitamin C.

Objective To screen the effect of 28 medicinal plants on inhibition of pancreatic lipase and evaluate the phytochemical contents of extracts. Methods The ethanolic extracts of 28 traditional Thai herbal medicines were assayed for their in vitro activities against porcine pancreatic lipase using p -nitrophenyl butyrate as a substrate. Quantitative estimation of flavonoids, phenolics, and alkaloids was done. Results Extracts from four herbs, Memecylon edule Roxb., Garcinia vilersiana Pierre, Cryptolepis elegans Wall. and Phyllanthus chamaepeuce Ridl., at a concentration of 100 μg/mL, strongly inhibited porcine pancreatic lipase by 90.97%, 92.04%, 94.64% and 95.38%, respectively. There was a significant positive correlation between phenolic content and inhibition activity. Inhibition activity was significantly correlated with flavonoid and with alkaloid contents. Conclusions From this result, it could be concluded that herbs represent a rich of anti-pancreatic lipase compounds, in particular, Cryptolepis elegans Wall. and Phyllanthus chamaepeuce Ridl. It is suggested that the phytochemical compounds from these plants may be applied for the prevention and treatment of obesity or hyperlipidemia.

Cryptospirolepine is the most structurally complex alkaloid discovered and characterized thus far from any Cryptolepis specie. Characterization of several degradants of the original, sealed NMR sample a decade after the initial report called the validity of the originally proposed structure in question. We now report the development of improved, homodecoupled variants of the 1,1- and 1,n-ADEQUATE (HD-ADEQUATE) NMR experiments; utilization of these techniques was critical to successfully resolving long-standing structural questions associated with crytospirolepine.

New approaches in probing for antimicrobial metabolites require genome and chemical investigation. The rapid identification of known compounds, i.e. dereplication, is strategically crucial in bioprospecting microbes for novel metabolites. An endophytic fungal strain, CBR-18, was isolated from Cryptolepis buchanani Roem. and identified as Phomopsis liquidambaris by molecular analysis. Biosynthetic polyketide synthase (PKS) genes of CBR-18 were investigated using three sets of degenerate primers, amplified with LC1–LC2c primers. Type I PKS gene-based and chemical investigation by a chromatography-guided approach furnished a broad-spectrum antimicrobial metabolite which was identified as oblongolide Y. Minimum inhibitory concentration values of the compound against test pathogens ranged between 25 and 100 µg/ml. The present study highlights the utility of strain CBR-18 as a promising source of potential polyketide antimicrobial agents which could be exploited for industrial purposes. This approach enabled di...

We recently reported that potent N10,O11-bis-alkylamine indolo[3,2- b ]quinoline antimalarials act as hemozoin (Hz) growth inhibitors. To improve access and binding to the target we have now designed novel N10,N11-di-alkylamine bioisosteres. 3-Chloro derivatives ( 10a – f ) showed selectivity for malaria parasite compared to human cells, high activity against Plasmodium falciparum chloroquine (CQ)-resistant strain W2 (IC 50 s between 20 and 158 nM), good correlation with β-hematin inhibition and improved vacuolar accumulation ratios, thus suggesting inhibition of Hz growth as one possible mechanism of action for these compounds. Moreover, our studies show that Hz is a valid target for the development of new antimalarials able to overcome CQ resistance.

Parquetina nigrescens is commonly used to treat diseases in humans and animals in developing countries, including Nigeria. This study evaluates the effects of its polyphenol-rich fraction (prf) on dichlorvos-induced cardio- and renal toxicity. There were several factors assessed during this study, including cardiac and renal markers, serum myeloperoxidase and xanthine oxidase, and electrocardiograph (ECG) changes. The changes in electrocardiograph (ECG) were recorded. Immunohistochemistry of cardiac and renal p38 and nitrotyrosine was determined. Dichlorvos exposure caused a significant decrease in L-glutathione (reduced glutathione) and other antioxidant enzymes with increases in malondialdehyde, myeloperoxidase, advanced oxidation protein products, and protein carbonyl levels. It also brought about alterations in microanatomy of the heart and kidneys accompanied by increases in serum creatinine and urea levels. Exposure to dichlorvos induced prolonged QRS interval and shortened QT durations in rats. Immunohistochemistry revealed lower expressions of cardiac nitrotyrosine and renal p38 (mitogen-activated protein kinase; MAPK) in rats treated with prf of P. nigrescens. Combining all, prf of P. nigrescens demonstrated antioxidant as well as protective properties in the heart and kidneys of rats exposed to dichlorvos. It ameliorated dichlorvos-induced cardio- and nephrotoxicity giving credence to its use in ethnomedicine.

‘Pinda oil ’ is an Ayurvedic medicinal oil use in dermatological and inflammatory conditions, prepared from Rubia cordifolia, Glycyrrhiza glabra and Cryptolepis buchnani . Qualitative and quantitative analysis of plant secondary metabolites incorporated in the oil is important in the standardization of the oil. T he oil has a deep wine red colo r due to the incorporation of anthraquinones from Rubia cordifolia . The major anthraquinones present in ‘Pinda oil’ were identified to be alizarin, xanthopurpurin, purpurin and ru biadin . A method was developed to quantitatively extract the anthraquinones by a solid phase extraction method using polyamide and to qua n tify them by HPLC. The precision of the method for alizarin , xanthopurpurin, purpurin and rubiadin are 6.5, 4.5, 4.0 a nd 4.8 % CV (n = 7) respectively. Analysis of market samples of the oil showed a wide variation in the values obtained indicating the need to standardize the manufacturing procedure. The Log P values of these compounds were determined by the HPLC method an d gave values in the range 2. 8 - 4.3 . These are reported her e for the first time.

An endophytic fungus Phomopsis liquidambaris CBR-15, was isolated from Cryptolepis buchanani Roem. (Asclepiadaceae) and identified by its characteristic culture morphology and molecular analysis of the ITS region of rDNA and intervening 5.8S rRNA gene. The impact of different culture media on biosynthesis of antimicrobial metabolites was tested by disc diffusion assay. Polyketide synthase gene (PKS) of the endophytic fungus was investigated using three pairs of degenerate primers LC1–LC2c, LC3–LC5c and KS3–KS4c by PCR. TLC-bioautography method was employed to detect the antimicrobial metabolites. Antimicrobial metabolites fractionated with ethyl acetate extract showed significant antimicrobial activity against the test bacteria and fungi. Biosynthesis of antimicrobial metabolites was optimum as depicted by zone of inhibition from ethyl acetate extract cultured in potato dextrose broth. Strain CBR-15 was identified as Phomopsisliquidambaris and PKS genes of the fungus were amplified with LC3–LC5c and KS3–KS4c sets of degenerate primers. These findings suggest that endophytic P.liquidambaris CBR-15 harbor iterative type I fungal PKS gene domain which indicates the biosynthetic potential of endophytic fungi as producers of natural antimicrobial metabolites. The study also demonstrates the utilization and optimization of different culture media which best supports for the biosynthesis of the antimicrobial metabolites from P.liquidambaris. Electronic supplementary material The online version of this article (doi:10.1007/s13205-014-0204-2) contains supplementary material, which is available to authorized users.

Asclepiadaceae is an economically important family species which are the source of fiber, rubber and dyes. In this study, genetic variability has been determined in three species, that is, Tylophora hirsuta, Wattakaka volubilis and Cryptolepis buchananii. The aim of present study was to understand the extent and pattern of genetic diversity among the individuals of same and different species of Asclepiadaceae. To asses the level of polymorphism within the species and members of different species, randomly amplified polymorphic DNA (RAPD) markers were used. Sixty RAPD primers of OPA, OPC, OPF and OPG series were used; only eight primers of OPC series gave amplification. Maximum polymorphism at interspecific and intraspecific levels was shown by OPC 09 and minimum polymorphism was observed in OPC 05. The data was analyzed using software numerical taxonomy system (NTSYS) cluster analysis PC version 2.20. In total 190 monomorphic and 78 polymorphic bands were produced from all primers. Therefore, out of 322 amplified products, 59% were monomorphic and 24.22% were polymorphic. Low genetic diversification was found both at intraspecific and interspecific level. Mixed pattern of grouping in the analyses indicated the close affinities of species with each other. Key words: Comparative assessment, genetic diversity, Asclepiadaceous species, randomly amplified polymorphic DNA (RAPD) markers on Asclepiadaceae.

Cryptolepis buchananiRoem. & Schult. is widely used in folk medicine in Southeast Asia for treating muscle tension and arthritis. This study aimed to investigate an analgesic activity of the methanol extract ofC. buchanani(CBE) in acetic acid-induced writhing response in mice, and to examine its anti-inflammatory activity in ethyl phenylpropiolate- (EPP-) induced ear edema and carrageenan-induced paw edema in rats. Its effects on cartilage degradation induced by interleukin-1β(IL-1β) in porcine cartilage explant culture were also determined. This study demonstrated that CBE significantly reduced acetic acid-induced writhing response. It also inhibited edema formation in both EPP-induced ear edema and carrageenan-induced paw edema models. In cartilage explant culture, CBE significantly reduced the sulfated glycosaminoglycan and hyaluronan released into culture media while it reserved the uronic acid and collagen within the cartilage tissues. It also suppressed the matrix metalloproteinase-2 activity with no effect on cell viability. In conclusion, CBE shows analgesic, anti-inflammatory, and chondroprotective effects in this preliminary study. Therefore, CBE may be useful as an alternative treatment for osteoarthritis.

Cryptolepis sanguinolenta and its bioactive alkaloid, cryptolepine have shown anti-inflammatory activity. However, the underlying mechanism of anti-inflammatory action in neuronal cells has not been investigated. In the present study we evaluated an extract of C. sanguinolenta (CSE) and cryptolepine (CAS) on neuroinflammation induced with IL-1β in SK-N-SH neuroblastoma cells. We then attempted to elucidate the mechanisms underlying the anti-neuroinflammatory effects of CAS in SK-N-SH cells. Cells were stimulated with 10 U/ml of IL-1β in the presence or absence of different concentrations of CSE (25–200 μg/ml) and CAS (2.5–20 μM). After 24 h incubation, culture media were collected to measure the production of PGE2 and the pro-inflammatory cytokines (TNFα and IL-6). Protein and gene expressions of cyclooxygenase (COX-2) and microsomal prostaglandin synthase-1 (mPGES-1) were studied by immunoblotting and qPCR, respectively. CSE produced significant (p < 0.05) inhibition of TNFα, IL-6 and PGE2 production in SK-N-SH cells. Studies on CAS showed significant and dose-dependent inhibition of TNFα, IL-6 and PGE2 production in IL-1β-stimulated cells without affecting viability. Pre-treatment with CAS (10 and 20 μM) was also found to inhibit IL-1β-induced protein and gene expressions of COX-2 and mPGES-1. Further studies to determine the mechanism of action of CAS showed inhibition of NF-κBp65 nuclear translocation, but not IκB phosphorylation. At 10 and 20 μM, CAS inhibited IL-1β-induced phosphorylation of p38 MAPK. Studies on the downstream substrate of p38, MAPK-activated protein kinase 2 (MAPKAPK2) showed that CAS produced significant (p < 0.05) and dose dependent inhibition of MAPKAPK2 phosphorylation in IL-1β-stimulated SK-N-SH cells. This study clearly shows that cryptolepine (CAS) inhibits neuroinflammation through mechanisms involving inhibition of COX-2 and mPGES-1. It is suggested that these actions are probably mediated through NF-κB and p38 signalling.

Literature survey revealed one HPLC method for quantification of 2-hydroxy-4-methoxybenzaldehyde in the root of Hemidesmus indicus [13], another for simultaneous analysis of 2-hydroxy-4-methoxybenzaldehyde and 2-hydroxy-4-methoxybenzoic acid in root tissues of the same plant [14], and a GC–MS method for determination of the chemical composition of volatile oil of H. indicus [15]. Gas chromatographic assay of 2hydroxy-4-methoxybenzaldehyde in dry and fresh root of Decalepis hamiltonii and H. indicus has also been reported [16]. No suitable HPTLC method is available. HPTLC has been widely used as quality-control tool for phytochemical evaluation of herbal drugs. In this work a precise and accurate HPTLC method has been established for rapid and accurate analysis of 2-hydroxy-4-methoxybenzaldehyde in H. indicus dried root powder and its extract. One important reason for selection of this marker was its absence from the plants commonly used as substitutes for H. indicus. It has been reported [17] that the roots of Ichnocarpus frutescens (Linn.) R.Br. (Apocyanaceae), Decalepis hamiltonii Wight and Arn. (Asclepiadaceae), and Cryptolepis buchnani Roem. & Schult. (Asclepiadaceae) are used as substitutes for H. indicus. Because there are no reports of the presence of this marker in the roots of I. frutescens and C. buchnani, substitution by the roots of these plants can be easily revealed by use of this HPTLC method. A study [18] of the essential oil (0.33%) of D. hamiltonii discovered the 2-hydroxy-4-methoxybenzaldehyde content of the oil was 37.45%. The amount of this marker in H. indicus is much higher. Sircar et al. [14] have reported the content to be 3.2 ± 0.2 mg g –1 of the mature roots of H. indicus and 2.6 ± 0.3 mg g –1 of the young roots. Thus even in this case, substitution of H. indicus by D. hamiltonii can be detected easily. Thus quantification of this marker will aid the detection of adulteration or substitution by common substituents because they either lack this marker or the content is less than in H. indicus.

Lectotypes are selected for the following names in the Apocynaceae from the Arabian Peninsula: Adenium arabicum Balf.f., Adenium obesum (Forssk.) Roem. & Schultes, Caralluma adenensis (Deflers) A.Berger, Cryptolepis intricata (Balf.f.) Venter, Cryptolepis volubilis (Balf.f.) O.Schwartz, Kanahia laniflora (Forssk.) R.Br., Leptadenia arborea (Forssk.) Schweinf., Marsdenia robusta Balf.f., Rhazya stricta Decne. and Tylophora yemensis Deflers. For Secamone socotrana Balf.f., it is noted that a previous citation of a holotype is rather an effective designation of a lectotype. Neotypes are selected for Caralluma hexagona var. septentrionalis Lavranos & L.E.Newton, Glossonema boveanum (Decne.) Decne., Leptadenia pyrotechnica (Forssk.) Decne. and Orbea chrysostephana (Deflers) Bruyns.

Factors leading to endemism, and the evolutionary implications of endemism, can be explored by studying closely related taxa with variously restricted distributions. Such a model is provided by Carex section Ceratocystis (Cyperaceae); Carex cryptolepis, Carex sp. nov., and C. lutea are North American endemics with broad, restricted, and highly restricted distributions, respectively. The prediction that levels of genetic diversity are a consequence of distribution size was tested within a phylogenetic context using population level genetic variation at 18 allozyme loci. In contrast to expectations, mean proportion of loci polymorphic, number of alleles per polymorphic locus, and expected heterozygosity were significantly greater in C. lutea than either C. cryptolepis or Carex sp. nov. Although the possibility of a shift in breeding system, past introgression, or progenitor-derivative relationships could explain the relatively high levels of variation observed in C. lutea, these were dismissed on the basis of allozyme and nuclear ribosomal sequence data. We conclude that C. lutea maintains levels of genetic diversity typical of caespitose carices despite its narrow endemism and that the low levels of genetic variation in C. cryptolepis and Carex sp. nov. are likely the result of population fluctuations during Pleistocene glacial-interglacial cycles.

A new species of Cryptolepis is described from Kenya and Tanzania. It is a tropical forest climber and its unique second corona whorl of deeply cleft lobes distinguishes it from all other Cryptolepis species. © 2008 The Linnean Society of London, Botanical Journal of the Linnean Society, 2008, 157, 343–346.

The relationship between construction materials used and longevity of traditional houses in three parishes adjacent to Kibale National Park in western Uganda was explored. Based on (i) resistance to termite attack, (ii) resistance to insect borers, (iii) rot resistance, (iv) wood that splits well, (v) the wood fibre not entangled, (vi) easy workability, (vii) weight, (viii) straight poles, (ix) availability within 2 km radius and (x) durability, 67 species were recorded, of which 43 are trees, nine climbers, ten shrubs and five herbs. Durable wood resistant to fungal attack, termites and woodborers is preferred in addition to being hard, straight and easy to work with a machete. Ranked high among the wild species are Harrisonia abyssinica Oliver, Millettia dura Dunn., Blighia unijugata Baker and Aegelopsis eggelingii M. R. F. Taylor. The commonly extracted pole sizes are between 5 and 12 cm dbh. Preferred wild ropes to fasten wattle, that are resistant to termites, include Cryptolepis sanguinoleta R. Br., Motandra sp., Urera trinervis (Hochst.) Friis & Imm., Paullinia pinnata L. and Cissus rotundifolia (Forssk.) Vahl. Longevity of houses greatly depended on the wall finishing by plastering with sand/wood ash and cow dung as well as the thatch material used: with the average life span of 14.7 years for grass-thatched, 20 years for papyrus and 29.9 years for iron-roofed houses.